GSK2636771
- Product Name
- GSK2636771
- CAS No.
- 1372540-25-4
- Chemical Name
- GSK2636771
- Synonyms
- CS-357;GSK2636771;GSK 2636771B;GSK2636771cas;GSK2636771 USP/EP/BP;GSK2636771/GSK-2636771;GSK 2636771 dihydrochloride;PI3Kβ-selective inhibitor GS2636771;2-Methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic;2-methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic acid
- CBNumber
- CB52624179
- Molecular Formula
- C22H22F3N3O3
- Formula Weight
- 433.42
- MOL File
- 1372540-25-4.mol
GSK2636771 Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 17380
- Product name
- GSK2636771
- Purity
- ≥98%
- Packaging
- 500μg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 17380
- Product name
- GSK2636771
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $74
- Updated
- 2024/03/01
- Product number
- 17380
- Product name
- GSK2636771
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $278
- Updated
- 2024/03/01
- Product number
- 17380
- Product name
- GSK2636771
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $384
- Updated
- 2024/03/01
- Product number
- 451491
- Product name
- GSK2636771
- Packaging
- 2.5mg
- Price
- $403
- Updated
- 2021/12/16
GSK2636771 Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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View Lastest Price from GSK2636771 manufacturers
- Product
- GSK-2636771 1372540-25-4
- Price
- US $0.00-0.00/mg
- Min. Order
- 1mg
- Purity
- 98%
- Supply Ability
- 20G
- Release date
- 2024-04-17
- Product
- GSK2636771 1372540-25-4
- Price
- US $0.00-0.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 1Ton
- Release date
- 2022-10-13
- Product
- GSK2636771 1372540-25-4
- Price
- US $2.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2018-12-23