Basic information Safety Supplier Related
ChemicalBook >  Product Catalog >  Biochemical Engineering >  Inhibitors >  PI3K / Akt / mTOR >  PI3K inhibitor >  GSK-2126458

GSK-2126458

Basic information Safety Supplier Related

GSK-2126458 Basic information

Product Name:
GSK-2126458
Synonyms:
  • GSK2126458
  • GSK-2126458
  • GSK2126458; GSK-2126458
  • 2,4-Difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]benzenesulfonamide
  • GSK2126458 (HYR-582)
  • CS-55
  • Omipalisib GSK2126458
  • HYR-582
CAS:
1086062-66-9
MF:
C25H17F2N5O3S
MW:
505.5
EINECS:
629-873-1
Product Categories:
  • Akt
  • mTOR
  • Aromatics
  • PI3K/Akt/mTOR
  • Inhibitors
  • PI3K
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Sulfur & Selenium Compounds
Mol File:
1086062-66-9.mol
More
Less

GSK-2126458 Chemical Properties

Melting point:
187-189℃
Boiling point:
715.6±70.0 °C(Predicted)
Density 
1.45
storage temp. 
Refrigerator
solubility 
Chloroform (Slightly), DMSO (Slightly), Methanol (Very Slightly, Heated)
form 
Solid
pka
6.23±0.40(Predicted)
color 
White to Pale Yellow
More
Less

Safety Information

HS Code 
29350090
More
Less

GSK-2126458 Usage And Synthesis

Description

GSK2126458 is a potent inhibitor of phosphoinositide 3-kinase isoforms (Kis = 19, 130, 24, and 60 pM for p110α, β, δ, and γ, respectively). It also inhibits mTOR in both mTORC1 and mTORC2 (Kis = 180 and 300 nM, respectively), as well as several common mutant forms of p110α. GSK2126458 is orally bioavailable, displays favorable pharmacokinetics, and shows efficacy in tumor growth models. GSK2126458 positively combines with inhibitors of discoidin domain receptor 1 (DDR1) inhibitor DDR1-IN-1 to suppress the growth of SNU-1040 colorectal cancer cells.

Uses

A highly potent inhibitor of PI3K and the mammalian target of Rapamycin.

Definition

ChEBI: Omipalisib is a member of the class of quinolines that is quinoline which is substituted by pyridazin-4-yl and 5-[(2,4-difluorobenzene-1-sulfonyl)amino]-6-methoxypyridin-3-yl groups at positions 4 and 6, respectively. It is a highly potent inhibitor of PI3K and mTOR developed by GlaxoSmithKline and was previously in human phase 1 clinical trials for the treatment of idiopathic pulmonary fibrosis and solid tumors. It has a role as an autophagy inducer, an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor, a mTOR inhibitor, an antineoplastic agent, a radiosensitizing agent and an anticoronaviral agent. It is a member of quinolines, a difluorobenzene, a sulfonamide, an aromatic ether, a member of pyridines and a member of pyridazines.

target

p110α

storage

Store at -20°C

GSK-2126458Supplier

ShangHai Biochempartner Co.,Ltd Gold
Tel
177-54423994 17754423994
Email
2853530910@QQ.com
Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Email
jkinfo@jkchemical.com
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Email
sales@BioChemBest.com
JinYan Chemicals(ShangHai) Co.,Ltd.
Tel
13817811078
Email
sales@jingyan-chemical.com