Newblue-CHEM - GDC-0941 Bimesylate CAS NO.957054-33-0

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Product Details

Keywords

GDC-0941 Bimesylate
957054-33-0
C24H30N7O6S3

Quick Details

ProName: Newblue-CHEM - GDC-0941 Bimesylate
CasNo: 957054-33-0
Molecular Formula: C24H30N7O6S3
Appearance: Solid
Application: Organic synthesis
DeliveryTime: PROMPT
PackAge: IN 25kg drums
Port: SHANGHAI
ProductionCapacity: 10 Metric Ton/Month
Purity: 99.0%
Storage: In Room Temperature
Transportation: As per MSDS
LimitNum: 1 Gram
Heavy metal: N/A
Grade: Industrial Grade,Food Grade,Pharma Gra...

Superiority

Henan Newblue Chemical Co., Ltd. is located in Zhengzhou High-tech Development Zone with import and export license.

We passed ISO 9001:2008 in 2009, and won "High-tech Enterprise" by provincial government in 2013.The objective of the company is to put quality first and put our customer’s needs first - the satisfaction of our customers is the company's ultimate goal.

Improving product quality and service level is our responsibility, and creating more value for our customer’s is our purpose. We are constantly striving to make Henan Newblue a leading chemical supplier, and hope to create a better future with you.

Details

GDC-0941 Bimesylate Basic information

Description In vitro In vivo

Product Name: GDC-0941 Bimesylate

Synonyms: GDC-0941 Bimesylate;GDC-0941 (diMethanesulfonate);GDC 0941 (2 MeSO3H salt);GDC-0941 (2 MeSO3H salt);Pictilisib;GDC-0941 BiMesylate/pictilisib;2-(1H-Indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)thieno[3,2-d]pyrimidine methanesulfonate (1:2);Pictilisib (GDC-0941)

CAS: 957054-33-0

MF: C24H30N7O6S3

MW: 608.7333

EINECS:

Product Categories: Intermediates & Fine Chemicals;Pharmaceuticals;Protein Kinase Inhibitors and Activators

Mol File: 957054-33-0.mol

GDC-0941 Bimesylate Structure

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)

GDC-0941 Bimesylate Preparation Products And Raw materials