Pictilisib (dimethanesulfonate)
Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold) .
Product Specifications
CAS Number
[957054-33-0]
Product Name Alternative
GDC-0941 (dimethanesulfonate) ; GDC-0941 (2 MeSO3H salt)
UNSPSC
12352005
Target
Apoptosis; Autophagy; PI3K
Type
Reference compound
Related Pathways
Apoptosis; Autophagy; PI3K/Akt/mTOR
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/GDC-0941-dimethanesulfonate.html
Purity
99.72
Solubility
DMSO : 7.14 mg/mL (ultrasonic; warming) |H2O : 7.14 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
O=S(N1CCN(CC1)CC2=CC3=C(S2)C(N4CCOCC4)=NC(C5=CC=CC6=C5C=NN6)=N3)(C)=O.O=S(O)(C)=O.O=S(O)(C)=O
Molecular Formula
C25H35N7O9S4
Molecular Weight
705.85
References & Citations
[1]Wallin JJ, et al. GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of RP-56976 in human breast cancer models by increasing cell death in vitro and in vivo.Clin Cancer Res. 2012 Jul 15;18 (14) :3901-11. Epub 2012 May 14.|[2]Wullschleger S, et al. Quantitative MRI establishes the efficacy of PI3K inhibitor (GDC-0941) multi-treatments in PTEN-deficient mice lymphoma.Anticancer Res. 2012 Feb;32 (2) :415-20.|[3]Zou ZQ, et al. The novel dual PI3K/mTOR inhibitor GDC-0941 synergizes with the MEK inhibitor U0126 in non-small cell lung cancer cells.Mol Med Report. 2012 Feb;5 (2) :503-8.|[4]Burrows N, et al. GDC-0941 inhibits metastatic characteristics of thyroid carcinomas by targeting both the phosphoinositide-3 kinase (PI3K) and hypoxia-inducible factor-1α (HIF-1α) pathways.J Clin Endocrinol Metab. 2011 Dec;96 (12) :E1934-43. Epub 2011 Oct|[5]Folkes AJ, et al. The identification of 2- (1H-indazol-4-yl) -6- (4-methanesulfonyl-piperazin-1-ylmethyl) -4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer . J Med Chem. 2008 Sep 25;51 (18) :5522-32.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ
Citation 01
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