Idelalisib (Synonyms: CAL-101; GS-1101)

Name: Idelalisib
Brand: MedChemExpress
SKU: HY-13026
Rating: 5.0 (46 reviews)

Cat. No.: HY-13026 Purity: 99.58%: FAQs
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Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC₅₀ of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.

For research use only. We do not sell to patients.

Idelalisib Chemical Structure

CAS No. : 870281-82-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 61	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 40	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 88	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
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Based on 46 publication(s) in Google Scholar

Other Forms of Idelalisib:

Idelalisib-d₅ Get quote

43 Publications Citing Use of MCE Idelalisib

Proliferation Assay

: Idelalisib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Aug 16;7(33):53515-53525. [Abstract]; PI3KD/V-IN-01 affects autophagy HeLa cells are treated with different concentrations of PI3KD/V-IN-01, VPS34-IN-1, GDC-0941 or CAL-101 for 16 hours before they are fixed and stained for the autophagy marker LC3B.

: Idelalisib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 May 31;7(22):32641-51. [Abstract]; The well-established PI3Kδ specific inhibitor, CAL-101, shows similar effects as PI3KD-IN-015 with an EC₅₀ of 2.3 nM against PI3Kδ and over 1000-fold less potent against the other three isoforms. Determination of CAL-101 inhibitory activities against PI3Kα, β, δ and γ in cellular background.

: Idelalisib purchased from MedChemExpress. Usage Cited in: Br J Haematol. 2015 Jul;170(1):134-8. [Abstract]; Treatment of CXCR4^WT and CXCR4^S338X BCWM.1 and MWCL-1 cells with PCI-32765 or Idelalisib induced caspase-3 and PARP cleavage at 6 h. Caspase-3 and PAPR cleavage following PCI-32765 (IB), Idelalisib (ID), ABT-199 (ABT), in the presence of absence of CXCL12 (SDF) and AMD3100 (AMD).

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View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
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Purity & Documentation
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Description

IC₅₀ & Target^[1]

p110δ

2.5 nM (IC₅₀)

p110γ

89 nM (IC₅₀)

p110β

565 nM (IC₅₀)

p110α

820 nM (IC₅₀)

hVps34

978 nM (IC₅₀)

DNA-PK

6729 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A498	GI₅₀	1.1 μM Compound: Idelalisib	Antiproliferative activity against human A498 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human A498 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
A549	IC₅₀	0.33 μM Compound: CAL-101	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	10.1039/C5MD00364D
B-cell	IC₅₀	0.0061 μM Compound: 74, GS-1101, CAL-101	Inhibition of PI3Kdelta in B-cells by proliferation assay Inhibition of PI3Kdelta in B-cells by proliferation assay	[PMID: 22924688]
Bel-7402	IC₅₀	66.23 μM Compound: CAL-101	Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35191698]
CAKI-1	GI₅₀	20.5 μM Compound: Idelalisib	Antiproliferative activity against human Caki1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human Caki1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
CCRF-CEM	GI₅₀	22.3 μM Compound: Idelalisib	Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human CCRF-CEM cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
DOHH-2	IC₅₀	0.86 μM Compound: Idelalisib	Cytotoxicity against human DOHH-2 cells expressing BTK and PI3kdelta assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay Cytotoxicity against human DOHH-2 cells expressing BTK and PI3kdelta assessed as inhibition of cell growth incubated for 72 hrs by celltiter-glo assay	[PMID: 35247756]
HCC 2998	GI₅₀	38.5 μM Compound: Idelalisib	Antiproliferative activity against human HCC2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HCC2998 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
HCT-116	IC₅₀	> 10 μM Compound: Idelalisib	Antiproliferative activity against human HCT116 cells by MTT assay Antiproliferative activity against human HCT116 cells by MTT assay	[PMID: 31434616]
HCT-116	IC₅₀	2.96 μM Compound: 1	Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
HEK293	IC₅₀	> 20 μM Compound: Idelalisib	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability by MTS assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability by MTS assay	[PMID: 32784091]
HeLa	IC₅₀	0.15 μM Compound: CAL-101	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	10.1039/C5MD00364D
Hep 3B2	IC₅₀	77.55 μM Compound: CAL-101	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35191698]
HepG2	IC₅₀	0.92 μM Compound: CAL-101	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	10.1039/C5MD00364D
HepG2	IC₅₀	89.5 μM Compound: CAL-101	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 35191698]
HOP-62	GI₅₀	> 100 μM Compound: Idelalisib	Antiproliferative activity against human HOP62 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HOP62 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
HOP-92	GI₅₀	14.1 μM Compound: Idelalisib	Antiproliferative activity against human HOP92 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human HOP92 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
Hs-578T	GI₅₀	6 μM Compound: Idelalisib	Antiproliferative activity against human Hs578T cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human Hs578T cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
HT	IC₅₀	> 10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human HT cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human HT cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
HUVEC	IC₅₀	38.22 μM Compound: 1	Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay Cytotoxicity against HUVEC cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
IGROV-1	GI₅₀	4.8 μM Compound: Idelalisib	Antiproliferative activity against human IGROV1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human IGROV1 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
JeKo-1	IC₅₀	0.12 μM Compound: Idelalisib	Antiproliferative activity against human JeKo-1 assessed as reduction in cell growth by MTS assay Antiproliferative activity against human JeKo-1 assessed as reduction in cell growth by MTS assay	[PMID: 32784091]
Jurkat	IC₅₀	7.9 μM Compound: Idelalisib	Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human Jurkat cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
KARPAS-422	GI₅₀	0.68 μM Compound: CAL-101	Growth inhibition of human KARPAS422 cells by CCK8 assay Growth inhibition of human KARPAS422 cells by CCK8 assay	[PMID: 28835805]
KARPAS-422	IC₅₀	8.1 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human KARPAS422 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human KARPAS422 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
KM12	IC₅₀	0.96 μM Compound: 1	Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human KM12 cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
KM12	GI₅₀	1.2 μM Compound: Idelalisib	Antiproliferative activity against human KM12 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human KM12 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
L02	IC₅₀	> 20 μM Compound: Idelalisib	Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTS assay Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTS assay	[PMID: 32784091]
LOUCY	IC₅₀	8.4 μM Compound: Idelalisib	Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human Loucy cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
LOX IMVI	GI₅₀	33.5 μM Compound: Idelalisib	Antiproliferative activity against human LOXIMVI cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human LOXIMVI cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
M14	GI₅₀	37.8 μM Compound: Idelalisib	Antiproliferative activity against human M14 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human M14 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
MCF7	IC₅₀	> 10 μM Compound: Idelalisib	Antiproliferative activity against human MCF7 cells by MTT assay Antiproliferative activity against human MCF7 cells by MTT assay	[PMID: 31434616]
MCF7	IC₅₀	0.78 μM Compound: CAL-101	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	10.1039/C5MD00364D
MDA-MB-231	GI₅₀	42.3 μM Compound: Idelalisib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
MOLM-13	GI₅₀	1.7 μM Compound: 1; CAL-101	Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MOLM-14	IC₅₀	3.6 μM Compound: Idelalisib	Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human MOLM14 cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
MOLM-14	GI₅₀	6.4 μM Compound: 1; CAL-101	Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MOLT-4	IC₅₀	> 10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human MOLT4 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human MOLT4 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
MOLT-4	IC₅₀	10.6 μM Compound: Idelalisib	Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human MOLT4 cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
MRC5	IC₅₀	> 100 μM Compound: 1; 6c	Cytotoxicity against human MRC5 cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as inhibition of cell viability measured after 48 hrs by MTT assay	[PMID: 34332211]
MV4-11	GI₅₀	> 10 μM Compound: 1; CAL-101	Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
MV4-11	IC₅₀	6.3 μM Compound: Idelalisib	Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells after 3 days by CellTiter-Glo assay	[PMID: 27774127]
NALM-6	GI₅₀	> 10 μM Compound: 1; CAL-101	Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
NAMALVA	IC₅₀	> 10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human NAMALWA cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human NAMALWA cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
Neutrophil	IC₅₀	0.07 μM Compound: Idelalisib	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation by measuring superoxide oxide dismutase inhibitable reduction of ferricytochrome c incubated for 5 mins Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced superoxide anion generation by measuring superoxide oxide dismutase inhibitable reduction of ferricytochrome c incubated for 5 mins	[PMID: 28648460]
Neutrophil	IC₅₀	0.07 μM Compound: Idelalisib	Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of superoxide generation preincubated for 5 mins followed by cytochalasin B and FMLP stimulation for 3 mins and 10 mins respectively by ferricytochrome c reduction b Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of superoxide generation preincubated for 5 mins followed by cytochalasin B and FMLP stimulation for 3 mins and 10 mins respectively by ferricytochrome c reduction b	[PMID: 27142697]
Neutrophil	IC₅₀	0.1 μM Compound: CAL-101	Antiinflammatory activity in human neutrophils assessed as inhibition of FMLP/cytochalasin B-induced superoxide anion generation by measuring superoxide dismutase-inhibitable reduction of ferricytochrome c preincubated for 5 mins followed by FMLP/cytochal Antiinflammatory activity in human neutrophils assessed as inhibition of FMLP/cytochalasin B-induced superoxide anion generation by measuring superoxide dismutase-inhibitable reduction of ferricytochrome c preincubated for 5 mins followed by FMLP/cytochal	[PMID: 27525452]
Neutrophil	IC₅₀	0.3 μM Compound: Idelalisib	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release incubated for 5 mins in presence of MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release incubated for 5 mins in presence of MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide	[PMID: 28648460]
Neutrophil	IC₅₀	0.3 μM Compound: CAL-101	Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as elastase substrate preincubated for 5 mins followed by fMLP/CB-induction Antiinflammatory activity in human neutrophils assessed as inhibition of fMLP/CB-induced elastase release using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as elastase substrate preincubated for 5 mins followed by fMLP/CB-induction	[PMID: 27525452]
Neutrophil	IC₅₀	0.3 μM Compound: Idelalisib	Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of elastase release preincubated for 5 mins followed by FMLP/CB stimulation for 10 mins using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate Anti-inflammatory activity in FMLP/CB-stimulated human neutrophils assessed as inhibition of elastase release preincubated for 5 mins followed by FMLP/CB stimulation for 10 mins using MeO-Suc-Ala-Ala-Pro-Val-p-nitroanilide as substrate	[PMID: 27142697]
OCI-Ly10	IC₅₀	> 10 μM Compound: Idelalisib	Antiproliferative activity against human OCILY10 assessed as reduction in cell growth by MTS assay Antiproliferative activity against human OCILY10 assessed as reduction in cell growth by MTS assay	[PMID: 32784091]
OCI-Ly10	IC₅₀	31.9 nM Compound: 1; CAL-101	Anticancer activity against human OCILY10 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay Anticancer activity against human OCILY10 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay	[PMID: 33297683]
OCI-Ly3	IC₅₀	5.2 μM Compound: Idelalisib	Antiproliferative activity against human OCILY3 assessed as reduction in cell growth by MTS assay Antiproliferative activity against human OCILY3 assessed as reduction in cell growth by MTS assay	[PMID: 32784091]
OVCAR-3	GI₅₀	17.7 μM Compound: Idelalisib	Antiproliferative activity against human OVCAR3 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human OVCAR3 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
PF-382	GI₅₀	> 10 μM Compound: 1; CAL-101	Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay	[PMID: 30053721]
Pfeiffer	GI₅₀	0.74 μM Compound: CAL-101	Growth inhibition of human Pfeiffer cells by CCK8 assay Growth inhibition of human Pfeiffer cells by CCK8 assay	[PMID: 28835805]
Pfeiffer	IC₅₀	6.8 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human Pfeiffer cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human Pfeiffer cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
Raji	IC₅₀	> 10 μM Compound: Idelalisib	Antiproliferative activity against human Raji cells by MTT assay Antiproliferative activity against human Raji cells by MTT assay	[PMID: 31434616]
Raji	IC₅₀	9.95 nM Compound: Idelalisib	Antiproliferative activity against human Raji cells after 72 hrs by MTT assay Antiproliferative activity against human Raji cells after 72 hrs by MTT assay	[PMID: 28325601]
Raji	IC₅₀	9.95 μM Compound: 1; CAL-101	Antiproliferative activity against human Raji cells after 72 hrs by MTT assay Antiproliferative activity against human Raji cells after 72 hrs by MTT assay	[PMID: 29534936]
Ramos	IC₅₀	> 10 nM Compound: Idelalisib	Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay	[PMID: 28325601]
Ramos	IC₅₀	> 10 μM Compound: 1; CAL-101	Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay Antiproliferative activity against human Ramos cells after 72 hrs by MTT assay	[PMID: 29534936]
Ramos	IC₅₀	> 10 μM Compound: Idelalisib	Antiproliferative activity against human Ramos cells by MTT assay Antiproliferative activity against human Ramos cells by MTT assay	[PMID: 31434616]
Ramos	IC₅₀	0.004 μM Compound: 1; CAL-101, GS-1101	Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in antihuman IgM-stimulated AKT phosphorylation at Ser473 residue preincubated for 60 mins followed by antihuman IgM stimulation and measured after 15 mins Inhibition of PI3Kdelta in human Ramos cells assessed as reduction in antihuman IgM-stimulated AKT phosphorylation at Ser473 residue preincubated for 60 mins followed by antihuman IgM stimulation and measured after 15 mins	[PMID: 31033293]
RAW264.7	IC₅₀	0.337 μM Compound: 1; CAL-101, GS-1101	Inhibition of PI3Kgamma in rat RAW264.7 cells assessed as reduction in C5a-stimulated AKT phosphorylation at Ser473 residue preincubated for 30 mins followed by C5a-stimulation and measured after 5 mins Inhibition of PI3Kgamma in rat RAW264.7 cells assessed as reduction in C5a-stimulated AKT phosphorylation at Ser473 residue preincubated for 30 mins followed by C5a-stimulation and measured after 5 mins	[PMID: 31033293]
RPMI-8226	IC₅₀	5.49 μM Compound: 1; CAL-101	Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTT assay	[PMID: 29534936]
RXF 393	GI₅₀	1.4 μM Compound: Idelalisib	Antiproliferative activity against human RXF393 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human RXF393 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
Sf21	IC₅₀	0.002 μM Compound: 1; CAL-101, GS-1101	Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence po Inhibition of N-terminal His6-tagged recombinant full length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence po	[PMID: 31033293]
Sf21	IC₅₀	0.293 μM Compound: 1; CAL-101, GS-1101	Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence pol Inhibition of N-terminal His6-tagged recombinant full length human p110beta/untagged recombinant full length human p85alpha expressed in baculovirus infected Sf21 insect cells using PIP2 as substrate measured after 80 mins by transcreener fluorescence pol	[PMID: 31033293]
Sf21	IC₅₀	154 nM Compound: 1	Inhibition of His6-tagged recombinant full length human N-terminal PI3Kbeta expressed in baculovirus infected Sf21 cells using lipid substrate incubated for 2 hrs by ADP-Glo assay Inhibition of His6-tagged recombinant full length human N-terminal PI3Kbeta expressed in baculovirus infected Sf21 cells using lipid substrate incubated for 2 hrs by ADP-Glo assay	[PMID: 30878826]
SNB-75	GI₅₀	1.2 μM Compound: Idelalisib	Antiproliferative activity against human SNB75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human SNB75 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
SUD4	IC₅₀	1.6 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human SU-DHL4 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human SU-DHL4 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
SU-DHL-1	IC₅₀	> 10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human SU-DHL1 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human SU-DHL1 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
SU-DHL10	IC₅₀	> 10 μM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human SU-DHL10 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human SU-DHL10 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
SU-DHL-6	GI₅₀	0.02 μM Compound: 1	Antiproliferative activity against human SU-DHL6 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human SU-DHL6 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 30996859]
SU-DHL-6	IC₅₀	0.033 μM Compound: Idelalisib	Antiproliferative activity against human SUDHL6 cells by MTT assay Antiproliferative activity against human SUDHL6 cells by MTT assay	[PMID: 31434616]
SU-DHL-6	GI₅₀	0.042 μM Compound: CAL-101; 1	Growth inhibition of human SU-DHL6 cells by CellTiter-Glo assay Growth inhibition of human SU-DHL6 cells by CellTiter-Glo assay	[PMID: 29601991]
SU-DHL-6	IC₅₀	0.053 μM Compound: 1	Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human SU-DHL-6 cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
SU-DHL-6	IC₅₀	0.12 μM Compound: Idelalisib	Antiproliferative activity against human SU-DHL-6 assessed as reduction in cell growth by MTS assay Antiproliferative activity against human SU-DHL-6 assessed as reduction in cell growth by MTS assay	[PMID: 32784091]
SU-DHL-6	IC₅₀	0.65 μM Compound: 1; CAL-101	Antiproliferative activity against human SUDHL6 cells after 72 hrs by CCK8 assay Antiproliferative activity against human SUDHL6 cells after 72 hrs by CCK8 assay	[PMID: 29534936]
SU-DHL-6	IC₅₀	117.6 nM Compound: 1; CAL-101; GS-1101	Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by alamar blue assay Antiproliferative activity against human SUDHL6 cells measured after 72 hrs by alamar blue assay	[PMID: 27846451]
SU-DHL-6	GI₅₀	124 nM Compound: 1	Growth inhibition of human SU-DHL6 cells incubated for 72 hrs by CellTiter-Glo assay Growth inhibition of human SU-DHL6 cells incubated for 72 hrs by CellTiter-Glo assay	[PMID: 30878826]
SU-DHL-6	IC₅₀	22.5 nM Compound: 1; CAL-101	Anticancer activity against human SUDHL-6 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay Anticancer activity against human SUDHL-6 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay	[PMID: 33297683]
SU-DHL-6	GI₅₀	34 nM Compound: Idelalisib	Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32078865]
T47D	IC₅₀	0.51 μM Compound: 1	Antiproliferative activity against human T47D cells incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells incubated for 72 hrs by CCK-8 assay	[PMID: 36182802]
T47D	GI₅₀	5.2 μM Compound: Idelalisib	Antiproliferative activity against human T47D cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human T47D cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
TMD8	IC₅₀	7.3 nM Compound: 1; CAL-101	Anticancer activity against human TMD8 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay Anticancer activity against human TMD8 assessed as inhibition of ATP level measured after 96 hrs by CellTiter-Glo reagent assay	[PMID: 33297683]
U-251	GI₅₀	53.2 μM Compound: Idelalisib	Antiproliferative activity against human U251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay Antiproliferative activity against human U251 cells assessed as cell growth inhibition measured after 48 hrs by SRB assay	[PMID: 32212730]
Vero	IC₅₀	> 20 μM Compound: Idelalisib	Cytotoxicity against monkey Vero cells assessed as reduction in cell viability by MTS assay Cytotoxicity against monkey Vero cells assessed as reduction in cell viability by MTS assay	[PMID: 32784091]

In Vitro

Idelalisib (CAL-101; GS-1101) is a highly selective and potent p110δ inhibitor (EC₅₀=8 nM). Greater selectivity (400- to 4000-fold) is seen against related kinases C2β, hVPS34, DNA-PK, and mTOR, whereas no activity is observed against a panel of 402 diverse kinases at 10 μM. CAL-101 reduces PDGF-induced pAkt by only 25% at 10 μM. Idelalisib (CAL-101) inhibits LPA-induced pAkt with an EC₅₀ of 1.9 μM. Idelalisib (CAL-101) blocks Fc?RI p110δ-mediated CD63 expression with an EC₅₀ of 8 nM, whereas formyl-methionyl-leucyl-phenylalanine activation of p110γ is inhibited with an EC₅₀ of 3 μM. Thus, in cell-based assays, CAL-101 has 240- to 2500-fold selectivity for p110δ over the other class I PI3K isoforms^[1]. CAL-101Idelalisib (CAL-101)-induced apoptosis of chronic lymphocytic leukemia (CLL) cells is significant compare with vehicle treatment alone (P<0.001). Idelalisib (CAL-101) induces selective cytotoxicity in CLL cells independent of IgVH mutational status or interphase cytogenetics^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

A significant reduction is observed in the CD11b⁺Ly6G⁺ neutrophils from brain homogenates of bothp110δ^D910A/D910A mice and Idelalisib (CAL-101) (40 mg/kg, i.v.) post-treated mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

415.42

Formula

C₂₂H₁₈FN₇O

CAS No.

870281-82-6

Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C2=CC=CC=C2)C([C@@H](NC3=C4N=CNC4=NC=N3)CC)=NC5=C1C(F)=CC=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : ≥ 59.7 mg/mL (143.71 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4072 mL	12.0360 mL	24.0720 mL
5 mM	0.4814 mL	2.4072 mL	4.8144 mL
10 mM	0.2407 mL	1.2036 mL	2.4072 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.78%

Select Batch:

Data Sheet (287 KB) SDS (393 KB)

COA (257 KB) LCMS (120 KB) Elemental Analysis Report (115 KB)

Handling Instructions (2659 KB)

References

[1]. Lannutti BJ, et al. CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood, 2011, 117(2), 591-594. [Content Brief]

[2]. Herman SE, et al. Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood, 2010, 116(12), 2078-2088. [Content Brief]

[3]. Low PC, et al. PI3Kδ inhibition reduces TNF secretion and neuroinflammation in a mouse cerebral stroke model. Nat Commun. 2014 Mar 14;5:3450. [Content Brief]

[4]. Cooney J, et al. Synergistic targeting of the regulatory and catalytic subunits of PI3Kδ in mature B cell malignancies. Clin Cancer Res. 2018 Mar 1;24(5):1103-1113. [Content Brief]

Cell Assay ^[2]	MTT assays are performed to determine cytotoxicity. Briefly, 1×10⁵ cells (CLL B cells or healthy volunteer T cells or NK cells) are incubated for 48 hours with different concentrations of Idelalisib (CAL-101) (0.1 μM, 1 μM, 5 μM, 10 μM), 25 μM LY294002, or vehicle control. MTT reagent is then added. DMSO is added, and absorbance is measured by spectrophotometry at 540 nm in a Labsystems plate reader. Cell viability is also measured at various time points with the use of annexin/PI flow cytometry. Data are analyzed with Expo-ADC32 software package. At least 10,000 cells are counted for each sample. Results are expressed as the percentage of total positive cells over untreated control. Experiments examining caspase-dependent apoptosis included the addition of 100 μM Z-VAD. Experiments examining survival signals include the addition of 1 μg/mL CD40L, 800 U/mL IL-4, 50 ng/mL BAFF, 20 ng/mL TNF-α, or coculturing on fibronectin or stromal (HS-5 cell line) coated plates. Stromal coculture is done by plating a 75-cm2 flask (80%-100% confluent) per 6-well plate 24 hours before the addition of CLL cells^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice^[3] For Idelalisib (CAL-101) treatment, wild-type C57BL/6 mice are administered either 40 mg/kg Idelalisib (CAL-101) or vehicle DMSO, by 25 μL infusion into the femoral vein, 15 min before I/R (pre-treatment), or 3 and 6 h after initiation of reperfusion (post-treatment). Controls and animals treated with Idelalisib (CAL-101) underwent cerebral blood flow (CBF) measurements using a laser Doppler perfusion monitor. The CBF measurements obtained immediately before and after MCAO and again at 3 h after reperfusion showed an ~90-95% reduction in the blood flow to the MCAO infarct region, which does not differ between groups. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Lannutti BJ, et al. CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood, 2011, 117(2), 591-594. [Content Brief] [2]. Herman SE, et al. Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood, 2010, 116(12), 2078-2088. [Content Brief] [3]. Low PC, et al. PI3Kδ inhibition reduces TNF secretion and neuroinflammation in a mouse cerebral stroke model. Nat Commun. 2014 Mar 14;5:3450. [Content Brief] [4]. Cooney J, et al. Synergistic targeting of the regulatory and catalytic subunits of PI3Kδ in mature B cell malignancies. Clin Cancer Res. 2018 Mar 1;24(5):1103-1113. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4072 mL	12.0360 mL	24.0720 mL	60.1801 mL
	5 mM	0.4814 mL	2.4072 mL	4.8144 mL	12.0360 mL
	10 mM	0.2407 mL	1.2036 mL	2.4072 mL	6.0180 mL
	15 mM	0.1605 mL	0.8024 mL	1.6048 mL	4.0120 mL
	20 mM	0.1204 mL	0.6018 mL	1.2036 mL	3.0090 mL
	25 mM	0.0963 mL	0.4814 mL	0.9629 mL	2.4072 mL
	30 mM	0.0802 mL	0.4012 mL	0.8024 mL	2.0060 mL
	40 mM	0.0602 mL	0.3009 mL	0.6018 mL	1.5045 mL
	50 mM	0.0481 mL	0.2407 mL	0.4814 mL	1.2036 mL
	60 mM	0.0401 mL	0.2006 mL	0.4012 mL	1.0030 mL
	80 mM	0.0301 mL	0.1505 mL	0.3009 mL	0.7523 mL
	100 mM	0.0241 mL	0.1204 mL	0.2407 mL	0.6018 mL

Idelalisib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Idelalisib870281-82-6CAL-101 GS-1101CAL101CAL 101GS1101GS 1101GS-1101PI3KAutophagyPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Idelalisib (Synonyms: CAL-101; GS-1101)

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