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Pictilisib dimethanesulfonate (GDC-0941 2 MeSO3H salt) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $30 | In Stock | |
25 mg | $40 | In Stock | |
50 mg | $50 | In Stock | |
1 mL x 10 mM (in DMSO) | $33 | In Stock |
Description | Pictilisib dimethanesulfonate (GDC-0941 2 MeSO3H salt) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold). |
Targets&IC50 | p110δ:3 nM, DNA-PK:1.23 μM, p110γ:75 nM, p110α:3 nM, p110α-E545K:3 nM, mTOR:0.58 μM (Ki), p110α-H1047R:3 nM, p110β:33 nM |
In vitro | Pictilisib (GDC-0941) demonstrates high efficacy in inhibiting cell growth, inducing G0-G1 arrest, and promoting apoptosis, especially when used in combination with U0126. It shows increased sensitivity in H460 cells harboring PIK3CA mutations over A549 cells with wild-type PIK3CA, by diminishing PI3K pathway activity as evidenced by reduced pAK levels. Pictilisib significantly lowers VEGF secretion in the medium following hypoxic/anoxic conditions across all tested cell lines. In breast cancer cell model systems, Pictilisib, alongside RP-56976, considerably decreases tumor cell viability by 80% or more, surpassing the effects of single-agent treatments. It effectively inhibits Akt phosphorylation and affects downstream targets including pPRAS40 and pS6 in various tumor models such as Hs578T1.2 (PI3Kα wild-type), MCF7-neo/HER2 (PI3Kα-mutant), and MX-1 (PTEN-null). Furthermore, Pictilisib reduces the duration of RP-56976-induced mitotic arrest, leading to apoptosis, and exhibits strong antitumor activity against ZD1839-resistant NSCLC cell lines, A549 and H460, highlighting its potential as a therapeutic agent in cancer treatment. |
In vivo | Pictilisib (GDC-0941)-treated mice display substantial, non-linear tumor shrinkage that reverses upon cessation of treatment, indicating a dependency on continuous administration for sustained efficacy. At doses of 25 or 50 mg/kg, Pictilisib effectively diminishes tumor growth and inhibits the PI3K and HIF-1 pathways in eGFP-FTC133 tumor-bearing mice. Additionally, a higher dose of 150 mg/kg administered orally achieves tumor stasis in MCF7-neo/HER2 model animals. The combination of Pictilisib with RP-56976 facilitates tumor regression and enhances antitumor responses during the treatment regimen, suggesting a synergistic interaction between the two compounds. |
Alias | GDC-0941 dimethanesulfonate, GDC-0941 2 MeSO3H salt |
Molecular Weight | 705.85 |
Formula | C25H35N7O9S4 |
Cas No. | 957054-33-0 |
Smiles | CS(O)(=O)=O.CS(O)(=O)=O.CS(=O)(=O)N1CCN(Cc2cc3nc(nc(N4CCOCC4)c3s2)-c2cccc3[nH]ncc23)CC1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (70.84 mM), Sonication is recommended. H2O: < 0.1 mg/mL (insoluble) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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