PI3Kα-IN-5

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PI3Kα-IN-5 (compound 6 ab) is a potent PI3Kα/mTOR inhibitor, with an IC₅₀ of 0.7 nM and 3.3 nM, respectively. PI3Kα-IN-5 can be used for the research of colorectal cancer.

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

PI3Kα-IN-5 Chemical Structure

CAS No. : 2237953-19-2

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mTOR mTORC1 mTORC2

Biological Activity
Purity & Documentation
References
Customer Review

Description

PI3Kα-IN-5 (compound 6 ab) is a potent PI3Kα/mTOR inhibitor, with an IC₅₀ of 0.7 nM and 3.3 nM, respectively. PI3Kα-IN-5 can be used for the research of colorectal cancer^[1].

IC₅₀ & Target^[1]

PI3Kα

0.7 nM (IC₅₀)

mTOR

3.3 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.218 μM Compound: 6ab	Antiproliferative activity against human A431 cells harboring wild type EGFR mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human A431 cells harboring wild type EGFR mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34971874]
BaF3	IC₅₀	0.217 μM Compound: 6ab	Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34971874]
CNE-2	IC₅₀	0.07 μM Compound: 6ab	Antiproliferative activity against human CNE-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human CNE-2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
HCT-116	IC₅₀	0.11 μM Compound: 6ab	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
HeLa	IC₅₀	13.44 μM Compound: 6ab	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
HepG2	IC₅₀	15.14 μM Compound: 6ab	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
L02	IC₅₀	> 100 μM Compound: 6ab	Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
MCF7	IC₅₀	2.22 μM Compound: 6ab	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
MDA-MB-231	IC₅₀	6.48 μM Compound: 6ab	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 34971874]
NCI-H1975	IC₅₀	0.217 μM Compound: 6ab	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by celltiter-glo assay	[PMID: 34971874]

Molecular Weight

601.66

Formula

C₃₀H₃₅N₉O₅

CAS No.

2237953-19-2

SMILES

O=C([C@H]1N(C(C2=CC=C(NC(NC3=CC=C(C4=NC(N5CCOCC5)=NC(N6CCOCC6)=N4)C=C3)=O)C=C2)=O)CCC1)N

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]. Wu CF, et, al. Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer. Eur J Med Chem. 2022 Feb 5;229:114055. [Content Brief]

PI3Kα-IN-5 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:

PI3Kα-IN-52237953-19-2PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycincolorectalcancerInhibitorinhibitorinhibit

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