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Pictilisib dimethanesulfonate

🥰Excellent
Catalog No. T11381Cas No. 957054-33-0
Alias GDC-0941 dimethanesulfonate, GDC-0941 2 MeSO3H salt

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).

Pictilisib dimethanesulfonate

Pictilisib dimethanesulfonate

🥰Excellent
Purity: 99.63%
Catalog No. T11381Alias GDC-0941 dimethanesulfonate, GDC-0941 2 MeSO3H saltCas No. 957054-33-0
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 SizePriceAvailabilityQuantity
10 mg$30In Stock
25 mg$40In Stock
50 mg$50In Stock
1 mL x 10 mM (in DMSO)$33In Stock
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Purity:99.63%
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Product Introduction

Bioactivity
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.
AliasGDC-0941 dimethanesulfonate, GDC-0941 2 MeSO3H salt
Chemical Properties
Molecular Weight705.85
FormulaC25H35N7O9S4
Cas No.957054-33-0
SmilesCS(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 & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.4167 mL7.0837 mL14.1673 mL70.8366 mL
5 mM0.2833 mL1.4167 mL2.8335 mL14.1673 mL
10 mM0.1417 mL0.7084 mL1.4167 mL7.0837 mL
20 mM0.0708 mL0.3542 mL0.7084 mL3.5418 mL
50 mM0.0283 mL0.1417 mL0.2833 mL1.4167 mL

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