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509226 PI 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).

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: GDC0941, 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

Primary Target: PI 3-K
509226
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Aperçu

Replacement Information

Tableau de caractéristiques principal

CAS #Empirical Formula
957054-30-7C₂₃H₂₇N₇O₃S₂

Products

RéférenceConditionnement Qté
5092260001 Flacon en verre 10 mg
Description
OverviewA 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 Number509226
Brand Family Calbiochem®
SynonymsGDC0941, 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
References
ReferencesTabe, 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 number957054-30-7
FormWhite solid
Hill FormulaC₂₃H₂₇N₇O₃S₂
Chemical formulaC₂₃H₂₇N₇O₃S₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetPI 3-K
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
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 InstructionsFollowing 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
Référence GTIN
5092260001 04055977241693

Documentation

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

Titre

Fiche de données de sécurité des matériaux (FDS) 

Références bibliographiques

Aperçu de la référence bibliographique
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.
Fiche technique

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.

Revision14-February-2014 JSW
SynonymsGDC0941, 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
DescriptionA 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.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number957054-30-7
Chemical formulaC₂₃H₂₇N₇O₃S₂
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (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 InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesTabe, 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.