- GSK-2636771
-
- $0.00 / 500mg
-
2024-04-19
- CAS:1372540-25-4
- Min. Order: 1mg
- Purity: 98%
- Supply Ability: 20G
- GSK2636771
-
- $0.00 / 1KG
-
2022-10-14
- CAS:1372540-25-4
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 1Ton
- GSK2636771
-
- $2.00 / 1kg
-
2019-07-06
- CAS:1372540-25-4
- Min. Order: 1kg
- Purity: 99%
- Supply Ability: 100kg
|
| | 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 | | EINECS: | | | 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.
|
| | GSK2636771 Preparation Products And Raw materials |
|