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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
Molecular Weight:
433.42
MDL Number:
MFCD22417098
MOL File:
1372540-25-4.mol
MSDS File:
SDS
Last updated:2025-09-29 22:33:22

GSK2636771 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
FDA UNII DW94IAT0LS

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338

GSK2636771 price More Price(36)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 17380 GSK2636771 ≥98% 1372540-25-4 500μg $44 2024-03-01 Buy
Cayman Chemical 17380 GSK2636771 ≥98% 1372540-25-4 1mg $74 2024-03-01 Buy
Cayman Chemical 17380 GSK2636771 ≥98% 1372540-25-4 5mg $278 2024-03-01 Buy
Cayman Chemical 17380 GSK2636771 ≥98% 1372540-25-4 10mg $384 2024-03-01 Buy
Usbiological 451491 GSK2636771 1372540-25-4 2.5mg $403 2021-12-16 Buy
Product number Packaging Price Buy
17380 500μg $44 Buy
17380 1mg $74 Buy
17380 5mg $278 Buy
17380 10mg $384 Buy
451491 2.5mg $403 Buy

GSK2636771 Chemical Properties,Uses,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

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

1372540-24-3

GSK2636771

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

Global( 163)Suppliers
Supplier Tel Email Country ProdList Advantage
Hubei Chuchang Biotech Co., Ltd.
+undefined15623860702 info@chuchangbiotech.com China 202 58
Capot Chemical Co.,Ltd.
+8613336195806 sales@capot.com China 29734 60
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 33024 60
career henan chemical co
+86-0371-86658258 +8613203830695 sales@coreychem.com China 29852 58
Changzhou PBpharmaceutical R&D Co.,Ltd
0519-83990708 info@pbpharm.com CHINA 498 58
Hubei xin bonus chemical co. LTD
86-13657291602 linda@hubeijusheng.com CHINA 22963 58
TargetMol Chemicals Inc.
+1-781-999-5354; +17819995354 marketing@targetmol.com United States 32432 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
86-571-88216897,88216896 13588875226 sales@hzclap.com CHINA 6312 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250 1026@dideu.com China 20424 58
Chemia Biotechnology(Shanghai) Co., Ltd
+8613816753574 info@chemia-pharm.com CHINA 311 58

View Lastest Price from GSK2636771 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
GSK2636771 pictures 2025-09-29 GSK2636771
1372540-25-4
US $36.00-153.00 / mg 99.74% 10g TargetMol Chemicals Inc.
GSK2636771 pictures 2025-04-04 GSK2636771
1372540-25-4
US $0.00-0.00 / KG 1KG 98% 1Ton Henan Aochuang Chemical Co.,Ltd.
GSK-2636771 pictures 2025-03-16 GSK-2636771
1372540-25-4
US $0.00-0.00 / mg 1mg 98% 20G Hubei Chuchang Biotech Co., Ltd.
  • GSK2636771 pictures
  • GSK2636771
    1372540-25-4
  • US $36.00-153.00 / mg
  • 99.74%
  • TargetMol Chemicals Inc.
  • GSK2636771 pictures
  • GSK2636771
    1372540-25-4
  • US $0.00-0.00 / KG
  • 98%
  • Henan Aochuang Chemical Co.,Ltd.
  • GSK-2636771 pictures
  • GSK-2636771
    1372540-25-4
  • US $0.00-0.00 / mg
  • 98%
  • Hubei Chuchang Biotech Co., Ltd.

GSK2636771 Spectrum

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