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Cat. No.: HY-14983

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PI3Kα/mTOR-IN-2

Benzothiazole Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors.

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

CAS No.: 1112980-86-5
Formula: C₂₀H₁₄ClFN₄O₃S₂
Molecular Weight:476.93

Storage:

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

PI3Kα/mTOR-IN-2 Chemical Structure

CAS No.: 1112980-86-5

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Use of MCE Products

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

Biological Activity
- Description
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
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Biological Activity

Description

Benzothiazole Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors

Cellular Effect

Cell Line	Type	Value	Description	References
A549	ED₅₀	0.28 mg/kg Compound: 82	Antitumor activity in po dosed mouse xenografted with human A549 cells expressing KRAS mutant gene Antitumor activity in po dosed mouse xenografted with human A549 cells expressing KRAS mutant gene	[PMID: 21332118]
A549	IC₅₀	0.2 μM Compound: A	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 24878359]
A549	IC₅₀	0.41 μM Compound: A	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 26321603]
HCT-116	ED₅₀	0.53 mg/kg Compound: 82	Antitumor activity in po dosed mouse xenografted with human HCT116 cells expressing PI3Kalpha/KRAS mutant gene Antitumor activity in po dosed mouse xenografted with human HCT116 cells expressing PI3Kalpha/KRAS mutant gene	[PMID: 21332118]
HCT-116	IC₅₀	0.44 μM Compound: A	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay	[PMID: 26321603]
HCT-116	IC₅₀	0.51 μM Compound: A	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 24878359]
MCF7	IC₅₀	0.23 μM Compound: A	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 23871904]
MCF7	IC₅₀	0.43 μM Compound: A	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay	[PMID: 26321603]
MCF7	IC₅₀	0.52 μM Compound: A	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 24878359]
PC-3	IC₅₀	47 nM Compound: 82	Antiproliferative activity against PTEN-deficient human PC3 cells by ATP-based cell viability assay Antiproliferative activity against PTEN-deficient human PC3 cells by ATP-based cell viability assay	[PMID: 21332118]
U-87MG ATCC	ED₅₀	0.26 mg/kg Compound: 1	Antitumor activity against human U87MG cells xenografted in po dosed mouse assessed as tumor growth inhibition Antitumor activity against human U87MG cells xenografted in po dosed mouse assessed as tumor growth inhibition	[PMID: 21612232]
U-87MG ATCC	ED₅₀	0.26 mg/kg Compound: 82	Antitumor activity against PTEN-deficient human U87MG cells xenografted in po dosed mouse Antitumor activity against PTEN-deficient human U87MG cells xenografted in po dosed mouse	[PMID: 21332118]
U-87MG ATCC	IC₅₀	0.44 μM Compound: A	Antiproliferative activity against human U87MG cells incubated for 72 hrs by MTT assay Antiproliferative activity against human U87MG cells incubated for 72 hrs by MTT assay	[PMID: 26321603]
U-87MG ATCC	IC₅₀	2.79 μM Compound: A	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay	[PMID: 24878359]
U-87MG ATCC	IC₅₀	6.3 nM Compound: 1	Inhibition of PI3Kalpha-mediated Akt phosphorylation at Ser 473 in human U87MG cells Inhibition of PI3Kalpha-mediated Akt phosphorylation at Ser 473 in human U87MG cells	[PMID: 21612232]
U-87MG ATCC	IC₅₀	6.3 nM Compound: 1	Inhibition of PI3K-mediated Akt phosphorylation at Ser 473 in human U87MG cells after 2 hrs by alphascreen assay Inhibition of PI3K-mediated Akt phosphorylation at Ser 473 in human U87MG cells after 2 hrs by alphascreen assay	[PMID: 21714526]
U-87MG ATCC	IC₅₀	68 nM Compound: 82	Antiproliferative activity against PTEN-deficient human U87MG cells by ATP-based cell viability assay Antiproliferative activity against PTEN-deficient human U87MG cells by ATP-based cell viability assay	[PMID: 21332118]

Chemical Information

CAS No. 1112980-86-5
Molecular Weight 476.93
Formula C₂₀H₁₄ClFN₄O₃S₂
SMILES

O=C(NC1=NC=2C=CC(=CC2S1)C=3C=NC(Cl)=C(C3)NS(=O)(=O)C4=CC=C(F)C=C4)C
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]. Discovery and Optimization of a Series of Benzothiazole Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors J. Med. Chem., Article ASAP Publication Date (Web): February 18, 2011

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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.

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100 mg

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