PI3Kδ-IN-10

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PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC₅₀ of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models.

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

PI3Kδ-IN-10 Chemical Structure

CAS No. : 2409725-49-9

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•Related Small Molecules:

•Related Proteins:

View All PI3K Isoform Specific Products:

View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All Akt Isoform Specific Products:

View All Isoforms

Akt Akt1 Akt2 Akt3

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

PI3Kδ

2 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
Bel-7402	IC₅₀	1.36 μM Compound: 9x	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]
Hep 3B2	IC₅₀	1.09 μM Compound: 9x	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	0.53 μM Compound: 9x	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]

In Vitro

PI3Kδ-IN-10 (compound 9x) (0-10 μM; 72 hours) has cell proliferation inhibitory effects in HCC cell lines with IC₅₀ of 0.53 - 1.36 μM^[1].
PI3Kδ-IN-10 (0-50 μM; 24 hours) markedly enhances expression level of cleaved PARP and cleaved caspase-3, also reduces the level of Akt phosphorylation at Ser473 and Thr308 in a dose-dependent manner^[1].

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

Cell Proliferation Assay

Cell Line:	Bel-7402, HepG2, Hep3B^[1]
Concentration:	0-10 μM
Incubation Time:	72 hours
Result:	Showed cell proliferation inhibitory effects in HCC cell lines with IC₅₀ of 0.53 - 1.36 μM.

Western Blot Analysis

Cell Line:	Bel-7402, HepG2^[1]
Concentration:	0 μM, 1.56 μM, 3.12 μM, 6.25 μM, 12.5 μM, 50 μM
Incubation Time:	24 hours
Result:	Markedly enhanced expression level of cleaved PARP and cleaved caspase-3, also reduced the level of Akt phosphorylation at Ser473 and Thr308 in a dose-dependent manner.

In Vivo

PI3Kδ-IN-10 (5 mg/kg for PO, 1 mg/kg for IV, single) exhibits an acceptable half-life (T_1/2), a moderate distribution volume, and acceptable oral bioavailability^[1].
PI3Kδ-IN-10 (40 and 20 mg/kg; IV, for 12 days) effectively suppress the growth of live cancer xenografts with inhibition ratios of 76.02% and 59.15% at 40 mg/kg and 20 mg/kg^[1].
Pharmacokinetic Parameters of PI3Kδ-IN-10 in female Balb/c (nu/nu) mice^[1].

	PO (5 mg/kg)	IV (1 mg/kg)
T_1/2 (h)	2.502	1.131
AUC (h·μg/L)	3067.94	2791.37
Vz/F (L/kg)	6.15	0.587
T_max (h)	3	0.083
F (%)	22.0

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

Animal Model:	Female Balb/c (nu/nu) mice^[1]
Dosage:	5 mg/kg or 1 mg/kg
Administration:	PO and IV, single (Pharmacokinetic Analysis)
Result:	Exhibited an acceptable half-life (T_1/2), a moderate distribution volume, and acceptable oral bioavailability.

Animal Model:	Female Balb/c (nu/nu) mice (6 weeks)^[1]
Dosage:	40 and 20 mg/kg
Administration:	IV, for 12 days
Result:	Effectively suppressed the growth of live cancer xenografts with inhibition ratios of 76.02% and 59.15% at 40 mg/kg and 20 mg/kg.

Molecular Weight

405.84

Formula

C₁₉H₁₆ClN₉

CAS No.

2409725-49-9

SMILES

N#CC1=C(N[C@H](C2=NN(C3=CC=CN=C3)C4=C2C=CC(Cl)=C4)C)N=C(N)N=C1N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Qi J, Wang W, Tang Y, et al. Discovery of Novel Indazoles as Potent and Selective PI3Kδ Inhibitors with High Efficacy for Treatment of Hepatocellular Carcinoma. J Med Chem. 2022;65(5):3849-3865. [Content Brief]

PI3Kδ-IN-10 Related Classifications

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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:

PI3Kδ-IN-102409725-49-9PI3KAktApoptosisPhosphoinositide 3-kinasePKBProtein kinase BPI3KδAKTHepatocellular carcinomaOrally activeBel-7402HepG2Inhibitorinhibitorinhibit

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