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PI3Kα-IN-5

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.

CAS No.: 2237953-19-2
Formula: C₃₀H₃₅N₉O₅
Molecular Weight:601.66

Storage:

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

Data Sheet (267 KB)

PI3Kα-IN-5 Chemical Structure

CAS No.: 2237953-19-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

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)

All PI3K Isoforms :

All mTOR Isoforms :

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]

Chemical Information

CAS No. 2237953-19-2
Molecular Weight 601.66
Formula C₃₀H₃₅N₉O₅
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (267 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Purity & Documentation
References

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PI3Kα-IN-5

All PI3K Isoforms

All mTOR Isoforms