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			96-Well Plate

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509226 Sigma-AldrichPI 3-K Inhibitor XXI, GDC-0941 - CAS 957054-30-7 - Calbiochem

A cell-permeable, potent, ATP-competitive inhibitor of class IA (IC₅₀ = 3 nM/p110α, 33 nM/p110&beta, 3 nM/p110δ) and IB PI 3-kinases (IC₅₀ = 75 nM/p110γ).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
参考
Data Sheet

同义词: 2-(1H-Indazol-4-yl)-6-(4-methylsulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2- d]pyrimidine, 4-(2-(1H-Indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine, GDC0941

Primary Target: PI 3-K

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
957054-30-7	C₂₃H₂₇N₇O₃S₂

价格及供货情况

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Description
Overview	A cell-permeable thienopyrimidine compound that acts as a potent, ATP-competitive inhibitor against class IA (IC₅₀ = 3 nM/p110α, 33 nM/p110β, 3 nM/p110δ) & IB (IC₅₀ = 75 nM/p110γ) PI 3-K kinases, including the two known p110α hot spot mutants E454K & H1047R (IC₅₀ = 3 nM), while exhibiting much reduced or little potency against more than 200 other kinases, including TrkA, class II C2β, class IV mTOR & DNA-PK (IC₅₀ = 2.85, 0.67, 0.58, and 1.23 µM, respectively) and class III Vps34 (IC₅₀ >10 µM). Effectively inhibits cellular Akt S473 phosphorylation (IC₅₀ = 28 to 46 nM) as well as proliferation in cancer cultures in vitro (GI₅₀ = 280 to 950 nM) and completely prevents the expansion of U87MG glioblastoma xenograft in mice in vivo (by 83%; 75 mg/kg/d p.o. for 21 days). Oral bioavailability is reported in human, dog, mouse, and rat.
Catalogue Number	509226
Brand Family	Calbiochem®
Synonyms	2-(1H-Indazol-4-yl)-6-(4-methylsulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2- d]pyrimidine, 4-(2-(1H-Indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine, GDC0941

References
References	Tabe, Y., et al. 2014. Acta Haematol. 131, 59. Ware, J.A., et al. 2013. Mol. Pharm. 10, 4047. Junttila,.T., et al. 2009. Cancer Cell 15, 429. Raynaud, F.I., et al. 2009. Mol Cancer Ther. 8, 1725. Folkes, A. J., et al. 2008. J. Med. Chem. 51, 5522.

Product Information
CAS number	957054-30-7
Form	White solid
Hill Formula	C₂₃H₂₇N₇O₃S₂
Chemical formula	C₂₃H₂₇N₇O₃S₂
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	PI 3-K
Purity	≥99% by HPLC

Physicochemical Information
Cell permeable	Y

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
Storage	+2°C to +8°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
5.09226.0001	04055977241693

Documentation

PI 3-K Inhibitor XXI, GDC-0941 - CAS 957054-30-7 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

参考

参考信息概述
Tabe, Y., et al. 2014. Acta Haematol. 131, 59. Ware, J.A., et al. 2013. Mol. Pharm. 10, 4047. Junttila,.T., et al. 2009. Cancer Cell 15, 429. Raynaud, F.I., et al. 2009. Mol Cancer Ther. 8, 1725. Folkes, A. J., et al. 2008. J. Med. Chem. 51, 5522.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	14-February-2014 JSW
Synonyms	2-(1H-Indazol-4-yl)-6-(4-methylsulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2- d]pyrimidine, 4-(2-(1H-Indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine, GDC0941
Description	A cell-permeable thienopyrimidine compound that acts as a potent, ATP-competitive inhibitor against class IA (IC₅₀ = 3 nM/p110α, 33 nM/p110β, 3 nM/p110δ) & IB (IC₅₀ = 75 nM/p110γ) PI 3-K kinases, including the two known p110α hot spot mutants E454K & H1047R (IC₅₀ = 3 nM), while exhibiting much reduced or little potency against more than 200 other kinases, including TrkA, class II C2β, class IV mTOR & DNA-PK (IC₅₀ = 2.85, 0.67, 0.58, and 1.23 µM, respectively) and class III Vps34 (IC₅₀ >10 µM). Effectively inhibits cellular Akt S473 phosphorylation (IC₅₀ = 46 nM/U87MG, 37 nM/PC3, and 28 nM/MDA-MB-361) as well as proliferation in cancer cultures in vitro (GI₅₀ = 950/U87MG, 280/PC3, and 720 nM/MDA-MB-361) and greatly prevents the expansion of U87MG glioblastoma xenograft in mice in vivo (by 83%; 75 mg/kg/d p.o. for 21 days). Oral bioavailability is reported in human, dog, mouse, and rat.
Form	White solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	957054-30-7
Chemical formula	C₂₃H₂₇N₇O₃S₂
Structure formula
Purity	≥99% by HPLC
Solubility	DMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity	Standard Handling
References	Tabe, Y., et al. 2014. Acta Haematol. 131, 59. Ware, J.A., et al. 2013. Mol. Pharm. 10, 4047. Junttila,.T., et al. 2009. Cancer Cell 15, 429. Raynaud, F.I., et al. 2009. Mol Cancer Ther. 8, 1725. Folkes, A. J., et al. 2008. J. Med. Chem. 51, 5522.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Phosphatidylinositol 3-Kinase (PI 3-kinase) Inhibitors

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