GSK2636771

Product Name: GSK2636771
CAS No.: 1372540-25-4
Chemical Name: GSK2636771
Synonyms: CS-357;GSK2636771;GSK 2636771B;GSK2636771cas;GSK2636771 ，S8002;GSK2636771 USP/EP/BP;GSK2636771/GSK-2636771;GSK2636771, 10 mM in DMSO;GSK 2636771 dihydrochloride;PI3Kβ-selective inhibitor GS2636771
CBNumber: CB52624179
Molecular Formula: C22H22F3N3O3
Formula Weight: 433.42
MOL File: 1372540-25-4.mol

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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

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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.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 17380
Product name: GSK2636771
Purity: ≥98%
Packaging: 500μg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 17380
Product name: GSK2636771
Purity: ≥98%
Packaging: 1mg
Price: $74
Updated: 2024/03/01

Cayman Chemical

Product number: 17380
Product name: GSK2636771
Purity: ≥98%
Packaging: 5mg
Price: $278
Updated: 2024/03/01

Cayman Chemical

Product number: 17380
Product name: GSK2636771
Purity: ≥98%
Packaging: 10mg
Price: $384
Updated: 2024/03/01

TRC

Product number: G797495
Product name: GSK2636771
Packaging: 5mg
Price: $185
Updated: 2021/12/16

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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.

Synthesis

1372540-24-3

1372540-25-4

2-Methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylate (180 mg, 0.4 mmol) was used as a starting material and dissolved in THF (10 mL). To this solution, 2N LiOH aqueous solution (1.2 mL) was added, followed by stirring the reaction at 50 °C for 1 hour. The progress of the reaction was monitored by TLC and after confirming complete consumption of the feedstock, the reaction mixture was cooled to room temperature. THF was removed under reduced pressure and the mixture was subsequently acidified by adjusting the pH to 3. The resulting suspension was filtered and the filter cake was washed with water (10 mL) to give the final white solid product 2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylic acid (152 mg, yield). The product was characterized by 1H NMR (300 MHz, DMSO-d6): δ 2.46 (s, 3H), 2.54 (s, 3H), 3.10 (t, 4H, J = 4.8 Hz), 3.73 (t, 4H, J = 4.8 Hz), 5.63 (s, 2H), 6.37 (d, 1H, J = 7.8 Hz), 7.26 (t, 1H, J = 7.8 Hz), 7.35 (d, 1H, J = 2.4 Hz), 7.44 (d, 1H, J = 2.4 Hz), 7.62 (d, 1H, J = 7.8 Hz); LC-MS: m/e = 434 [M + 1]+.

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.

in vivo

GSK2636771 is a p110β inhibitor, and the p110β primes cells for response to growth factor stimulation. While p110β inhibition suppresses cell and tumor growth, dual targeting of p110α/β enhances apoptosis and provides sustained tumor response in mice model^[2].

IC 50

PI3Kβ: 0.89 nM (Ki); PI3Kβ: 5.2 nM (IC₅₀)

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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GSK2636771 Suppliers

China 145 United States 18 Global 163

Shanghai Boyle Chemical Co., Ltd.

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View Lastest Price from GSK2636771 manufacturers

Henan Aochuang Chemical Co.,Ltd.

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

Hubei Chuchang Biotech Co., Ltd.

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

Career Henan Chemical Co

Product: GSK2636771 1372540-25-4
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-23

1372540-25-4, GSK2636771Related Search:

GSK-3326595 Bortezomib AZD6482 Alpelisib (BYL719) Pictilisib IPI 145 GSK-2256098 GSK369796 GSK2982772 MethanesulfonaMide, N-[5-[4-[5-[[(2R,6S)-2,6-diMethyl-4-Morpholinyl]Methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-Methoxy-3-pyridinyl]-, rel- GSK-2881078 GSK-2018682 GSK 2239633A GSK2838232 GSK2126458 GSK 2330672 GSK2795039 GSK2879552

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

2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(morpholin-4-yl)-1H-1,3-benzodiazole-4-carboxylic acid

CS-357

PI3Kβ-selective inhibitor GS2636771

GSK 2636771B

GSK2636771 USP/EP/BP

GSK2636771cas

2-methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic acid

GSK2636771, 10 mM in DMSO

GSK2636771 ，S8002

1372540-25-4

Inhibitors

PI3K/Akt/mTOR

Akt

mTOR

PI3K

api

1372540-25-4