GDC-0941 dimethanesulfonate |CAS:957054-33-0 Probechem Biochemicals

Chemical Structure : GDC-0941 dimethanesulfonate

CAS No.: 957054-33-0

GDC-0941 dimethanesulfonate (Pictilisib dimethanesulfonate)

Catalog No.: PC-45782Not For Human Use, Lab Use Only.

Pictilisib dimethanesulfonate (GSC-0941) is a potent, selective, orally bioavailable inhibitor of class I PI3Ks with IC50 of 3/33/3/75 nM for p110α/β/γ/δ, respectively.

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25 mg	$188	In stock
50 mg	$288	In stock
100 mg	$458	In stock
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Biological Activity

Pictilisib dimethanesulfonate (GSC-0941) is a potent, selective, orally bioavailable inhibitor of class I PI3Ks with IC50 of 3/33/3/75 nM for p110α/β/γ/δ, respectively.

Pictilisib (GSC-0941) shows similar activity for mutant p110α E545K and H1047R (IC50=3 nM), weak or little activity for C2α, Vps34, DNA-PK, and mTOR (IC50>500 nM).

Pictilisib (GSC-0941) inhibits Akt (Ser473) phosphorylation in U87MG, PC3, and MDA-MB-361 cells with IC50s of 46, 37, and 28 nM, respectively, and respective GI50 is 0.95, 0.28, and 0.72 uM.

Pictilisib (GSC-0941) exhibits tumor growth inhibition in U87MG human glioblastoma xenografts.

Physicochemical Properties

M.Wt	705.8469
Formula	C25H35N7O9S4
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Thieno[3,2-d]pyrimidine, 2-(1H-indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-, methanesulfonate (1:2)

References

1. Folkes AJ, et al. J Med Chem. 2008 Sep 25;51(18):5522-32.

2. Junttila TT, et al. Cancer Cell. 2009 May 5;15(5):429-40.

3. Raynaud FI, et al. Mol Cancer Ther. 2009 Jul;8(7):1725-38.

GDC-0941 dimethanesulfonate (Pictilisib dimethanesulfonate)

Biological Activity

Physicochemical Properties

References

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