GSK2636771
GSK2636771 Basic information
- Product Name:
- GSK2636771
- Synonyms:
-
- GSK2636771
- 2-Methyl-1-[[2-Methyl-3-(trifluoroMethyl)phenyl]Methyl]-6-(4-Morpholinyl)-1H-benziMidazole-4-carboxylic acid
- GSK2636771/GSK-2636771
- GSK 2636771 dihydrochloride
- 2-Methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic
- 1H-Benzimidazole-4-carboxylic acid, 2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(4-morpholinyl)-
- 2-Methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylic acid GSK2636771
- 2-METHYL-1-[[2-METHYL-3-(TRIFLUOROMETHYL)PHENYL]METHYL]-6-MORPHOLIN-4-YLBENZIMIDAZOLE-4-CARBOXYLIC ACID
- CAS:
- 1372540-25-4
- MF:
- C22H22F3N3O3
- MW:
- 433.42
- Product Categories:
-
- Inhibitors
- PI3K/Akt/mTOR
- Akt
- mTOR
- PI3K
- api
- 1372540-25-4
- Mol File:
- 1372540-25-4.mol
GSK2636771 Chemical Properties
- Melting point:
- >225°C (dec.)
- Boiling point:
- 641.3±55.0 °C(Predicted)
- Density
- 1.38
- storage temp.
- -20°C Freezer
- solubility
- DMSO (Slightly), Methanol (Slightly)
- pka
- -2.70±0.30(Predicted)
- form
- Solid
- color
- Pale Yellow
- InChI
- InChI=1S/C22H22F3N3O3/c1-13-15(4-3-5-18(13)22(23,24)25)12-28-14(2)26-20-17(21(29)30)10-16(11-19(20)28)27-6-8-31-9-7-27/h3-5,10-11H,6-9,12H2,1-2H3,(H,29,30)
- InChIKey
- XTKLTGBKIDQGQL-UHFFFAOYSA-N
- SMILES
- C1(C)N(CC2=CC=CC(C(F)(F)F)=C2C)C2=CC(N3CCOCC3)=CC(C(O)=O)=C2N=1
GSK2636771 Usage And Synthesis
Description
GSK2636771 is a potent, orally bioavailable, adenosine triphosphate-competitive, selective inhibitor of PI3Kβ with an apparent Ki value of 0.89 nmol/L (IC50 = 5.2 nmol/L), >900-fold selectivity over p110α and p110γ, and >10-fold selectivity over p110δ isoforms, while sparing other PI3K superfamily kinases[1-2].
Uses
GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines.
in vitro
GSK-2636771 shows selectively inhibitory activity in PTEN null cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 nM and 72 nM, respectively. GSK2636771 significantly decreases cell viability in p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines. It leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines.
References
[1] Mateo, Joaquin , et al. "A first-time-in-human study of GSK2636771, a phosphoinositide 3 kinase beta-selective inhibitor, in patients with advanced solid tumors." Clinical Cancer Research (2017):clincanres.0725.2017.
[2] Sarker, Debashis , et al. "A Phase I, Open-Label, Dose-Finding Study of GSK2636771, a PI3Kβ Inhibitor, Administered with Enzalutamide in Patients with Metastatic Castration-Resistant Prostate Cancer." Clinical Cancer Research 27.19(2021):5248-5257.
GSK2636771Supplier
- Tel
- sales@boylechem.com
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- +86-21-20908456
- sales@BioChemBest.com
- Tel
- +86 (531) 88811783
- sales@trio-pharmatech.com (International market)
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Tel
- 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
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