957054-33-0 GDC-094...

957054-33-0 GDC-0941 Bimesylate

957054-33-0 GDC-0941 Bimesylate

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1 Kilogram

FOB Price: USD 1000.0000

  • Min.Order :1 Kilogram
  • Purity: 99%
  • Payment Terms : L/C,T/T

Keywords

957054-33-0 GDC-0941 Bimesylate GDC-0941 Bimesylate

Quick Details

  • Appearance:white powder
  • Application:pharma
  • PackAge:as clients needs
  • ProductionCapacity:1|Metric Ton|Day
  • Storage:RT
  • Transportation:sea

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Details:

GDC-0941 Bimesylate Chemical Properties
Melting point >280°C (dec.)
storage temp. Refrigerator
Safety Information
MSDS Information
GDC-0941 Bimesylate Usage And Synthesis
Description Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Phase 2.
In vitro GDC-0941 is equipotent against PI3Kα and PI3Kδ as well as PI3Kα mutants E545-K and H1047-R, displaying modest levels of selectivity against PI3Kβ (10-fold) and PI3Kγ (25-fold), and greater levels of selectivity against members of PI3K class II, III, and IV, including C2β, Vps34, DNA-PK, and mTOR. GDC-0941 potently inhibits the phosphorylation of Akt in U87MG, PC3, and MDA-MB-361 cells with IC50 of 46 nM, 37 nM, and 28 nM, respectively. GDC-0941 inhibits the proliferation of U87MG, A2780, PC3, and MDA-MB-361 cells with IC50 of 0.95 μM, 0.14 μM, 0.28 μM, and 0.72 μM, respectively. GDC-0941 treatment potently inhibits the proliferation of both trastuzumab-sensitive and-insensitive HER2-amplified cells with IC50 of 149-944 nM. GDC-0941 inhibits proliferation of HER2-amplified cells that harbor PIK3CA mutations with IC50 of <500 nM, and effectively inhibits both proliferation and viability of HER2-amplified breast cancer cells that are resistant to trastuzumab due to PTEN loss. GDC-0941 significantly inhibits the growth of HCT116, DLD1 and HT29 cells with GI50 of 1081 nM, 1070 nM and 157 nM, respectively. GDC-0941 inhibits tumor cell proliferation, induces apoptosis and suppresses centroblast population.
In vivo Administration of GDC-0941 at 75 mg/kg/day displays significant inhibitory effect against established human U87MG glioblastoma xenografts in female NCr athymic mice, with tumor growth inhibition of 83%. Oral administration of GDC-0941 at 150 mg/kg/day inhibits the growth of HER2-amplified, trastuzumab-resistant MDA-MB-361.1 xenografts in mice, and significantly delays the tumor progression, in association with potent induced apoptosis in tumors. GDC-0941 (75 mg/kg/day) treatment for 2 weeks induces ~40% reduction in tumor volume of spontaneous B-cell follicular lymphomas developed in PTEN+/-LKB1+/hypo mice, accompanied by ablation of phosphorylation of Akt, S6K and SGK (serum and glucocorticoid protein kinase) protein kinases.
Chemical Properties Off-White Solid
Uses Potent inhibitor of Phosphatidylinositol 3-kinase (PI3K)

 

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