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GDC-0941 dimethanesulfonate (Synonyms: Pictilisib dimethanesulfonate; GDC-0941 (2 MeSO3H salt); GDC-0941)

Cat. No.: HY-20180 Purity: 99.12%
Data Sheet SDS Handling Instructions

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).

For research use only. We do not sell to patients.
GDC-0941 dimethanesulfonate Chemical Structure

GDC-0941 dimethanesulfonate Chemical Structure

CAS No. : 957054-33-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
10 mg $50 In-stock
50 mg $75 In-stock
100 mg $120 In-stock
200 mg $210 In-stock
500 mg   Get quote  
1 g   Get quote  

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Other Forms of GDC-0941 dimethanesulfonate:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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). IC50 value: 3 nM Target: PI3Kα/δ GDC-0941 is a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer. GDC-0941 against p110a IC50=0.003μM,U87MG IC50=0.95μM, A2780 IC50=0.14 μM, and in vitro metabolic stability in mouse and human is 91.96%. The inhibitions of U87MG , PC3, MDA-MB-361 cancer cell proliferation are (IC50) 0.95, 0.28, 0.72 μM, respectively.

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00876109 Genentech, Inc. Solid Cancers October 2007 Phase 1
NCT01740336 Genentech, Inc. Breast Cancer February 6, 2013 Phase 2
NCT00876122 Genentech, Inc. Non-Hodgkin's Lymphoma, Solid Cancers March 2008 Phase 1
NCT00975182 Genentech, Inc. Non-Squamous Non-Small Cell Lung Cancer, Solid Cancers September 2009 Phase 1
NCT00999128 Genentech, Inc. Healthy Volunteers October 26, 2009 Phase 1
NCT01240226 Genentech, Inc. Healthy Volunteer November 2010 Phase 1
NCT01437566 Genentech, Inc. Breast Cancer October 2011 Phase 2
NCT00974584 Genentech, Inc. Non-Squamous Non-Small Cell Lung Cancer October 2009 Phase 1
NCT00928330 Genentech, Inc. Metastatic Breast Cancer July 2009 Phase 1
NCT01474668 Genentech, Inc. Healthy Volunteer October 2011 Phase 1
NCT02092831 Genentech, Inc. Healthy Volunteer April 2014 Phase 1
NCT00996892 Genentech, Inc. Solid Tumors November 2009 Phase 1
NCT00960960 Genentech, Inc. Breast Cancer August 2009 Phase 1
NCT01493843 Genentech, Inc. Non-Small Cell Lung Cancer January 20, 2012 Phase 2
NCT02389842 Royal Marsden NHS Foundation Trust|Institute of Cancer Research, United Kingdom|Roche Pharma AG|Pfizer Advanced Solid Tumours|Breast Cancer February 2015 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.4167 mL 7.0837 mL 14.1673 mL
5 mM 0.2833 mL 1.4167 mL 2.8335 mL
10 mM 0.1417 mL 0.7084 mL 1.4167 mL
References
Molecular Weight

705.85

Formula

C₂₅H₃₅N₇O₉S₄

CAS No.

957054-33-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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GDC-0941 dimethanesulfonate
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HY-20180
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