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Pictilisib dimethanesulfonate

Catalog No. T11381 CAS 957054-33-0

Synonyms: 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).

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Pictilisib dimethanesulfonate Chemical Structure

Pictilisib dimethanesulfonate, CAS 957054-33-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 32.00
10 mg	In stock	$ 50.00
25 mg	In stock	$ 67.00
50 mg	In stock	$ 74.00
1 mL * 10 mM (in DMSO)	In stock	$ 55.00

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Purity: 99.69%

Biological Description

Chemical Properties

Storage & Solubility Information

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	mTOR:0.58 μM (Ki), p110α-E545K:3 nM, p110α:3 nM, p110γ:75 nM, DNA-PK:1.23 μM, p110δ:3 nM, 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.

Synonyms	GDC-0941 dimethanesulfonate, GDC-0941 2 MeSO3H salt
Molecular Weight	705.85
Formula	C25H35N7O9S4
CAS No.	957054-33-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (70.84 mM), Sonification is recommended.

H2O: < 0.1 mg/mL (insoluble)

References and Literature

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. 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. 3. 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. 4. 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. 5. 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

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Glutamine Metabolism Compound Library Anti-Cancer Metabolism Compound Library Anti-Aging Compound Library Anti-Lung Cancer Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Pictilisib dimethanesulfonate 957054-33-0 Apoptosis Autophagy DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK PI3K mTOR GDC 0941 inhibit Inhibitor GDC-0941 dimethanesulfonate Pictilisib GDC0941 GDC-0941 2 MeSO3H Phosphoinositide 3-kinase GDC-0941 2 MeSO3H salt GDC-0941 inhibitor

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