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Chemical Structure| 1372540-25-4 Chemical Structure| 1372540-25-4

Structure of GSK2636771
CAS No.: 1372540-25-4

Chemical Structure| 1372540-25-4

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GSK2636771 is a potent, selective and orally bioavailable PI3Kβ inhibitor. It has been used in trials studying the treatment of CANCER, LYMPHOMA, Solid Neoplasm, Recurrent Solid Neoplasm, and Advanced Malignant Neoplasm, among others.

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Product Details of GSK2636771

CAS No. :1372540-25-4
Formula : C22H22F3N3O3
M.W : 433.42
SMILES Code : O=C(C1=C2C(N(CC3=CC=CC(C(F)(F)F)=C3C)C(C)=N2)=CC(N4CCOCC4)=C1)O
MDL No. :MFCD22417098
InChI Key :XTKLTGBKIDQGQL-UHFFFAOYSA-N
Pubchem ID :56949517

Safety of GSK2636771

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of GSK2636771

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110β

In Vitro:

Cell Line
Concentration Treated Time Description References
ZR75-1 1 µM 1 hour P110β inhibition delayed AKT phosphorylation Clin Cancer Res. 2017 Jun 1;23(11):2795-2805.
MDA-MB-415 1 µM 1 hour P110β inhibition delayed AKT phosphorylation Clin Cancer Res. 2017 Jun 1;23(11):2795-2805.
CAMA-1 1 µM 1 hour P110β inhibition delayed AKT phosphorylation Clin Cancer Res. 2017 Jun 1;23(11):2795-2805.
HTLA cells 10 µM Overnight To detect the agonist activity of GSK2636771 on GPR39 Mol Pharmacol. 2016 Dec;90(6):726-737.
VTC-103 cells 25 µM 6 days Evaluate the synergistic inhibitory effect of GSK2636771 combined with αCT1 and TMZ on VTC-103 cells Oncogenesis. 2022 Jan 12;11(1):2.
U87MG cells 25 µM 6 days Evaluate the synergistic inhibitory effect of GSK2636771 combined with αCT1 and TMZ on U87MG cells Oncogenesis. 2022 Jan 12;11(1):2.
LN229 cells 25 µM 6 days Evaluate the synergistic inhibitory effect of GSK2636771 combined with αCT1 and TMZ on LN229 cells Oncogenesis. 2022 Jan 12;11(1):2.
EEC cell lines 1 µM/10 µM 72 hours No significant difference in cell viability following p110 β inhibition between PTEN -mutant and PTEN wild-type EEC cell lines was found, and a marked decrease in cell viability was only observed in the p110 β-reliant prostate and breast cancer cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3533-44.
N-TERT cells 1 µM 72 hours GSK2636771 slightly reduced the number of N-TERT cells but did not significantly affect cell viability. Int J Mol Sci. 2021 Mar 30;22(7):3567.
IC8 cells 1 µM 72 hours GSK2636771 had a minor effect on the number and viability of IC8 cells. Int J Mol Sci. 2021 Mar 30;22(7):3567.
Met1 cells 1 µM 72 hours GSK2636771 slightly reduced the number of Met1 cells but did not significantly affect cell viability. Int J Mol Sci. 2021 Mar 30;22(7):3567.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
SCID/beige mice SF295 xenograft tumor model Intraperitoneal injection 20 mg/kg Every other day for 18 days Evaluate the synergistic inhibitory effect of GSK2636771 combined with αCT1 and TMZ on SF295 xenograft tumors Oncogenesis. 2022 Jan 12;11(1):2.
Mice Braf-mutant, PTEN-null melanoma model Oral gavage 30 mg/kg Daily until the end of the experiment To evaluate the efficacy of GSK2636771 in combination with anti-OX40 antibody in treating PTEN-null melanoma. The results showed that the combination treatment significantly delayed tumor growth and extended the survival of mice. Clin Cancer Res. 2019 Nov 1;25(21):6406-6416
Nude mice ZR75-1/FR xenograft model Oral 30 mg/kg/d Daily for 4 weeks P110β inhibition induced tumor regression, but tumors resumed growth after 3 weeks, while combined p110α/β inhibition provided durable tumor regression Clin Cancer Res. 2017 Jun 1;23(11):2795-2805.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01458067 Cancer PHASE1 COMPLETED 2016-02-25 GSK Investigational Site, New ... More >>Haven, Connecticut, 06520, United States|GSK Investigational Site, Oklahoma City, Oklahoma, 73104, United States|GSK Investigational Site, Nashville, Tennessee, 37203, United States|GSK Investigational Site, Salt Lake City, Utah, 84112, United States|GSK Investigational Site, Seoul, 110-744, Korea, Republic of|GSK Investigational Site, Seoul, 120/752, Korea, Republic of|GSK Investigational Site, Sutton, Surrey, SM2 5PT, United Kingdom|GSK Investigational Site, London, W1G 6AD, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.54mL

2.31mL

1.15mL

23.07mL

4.61mL

2.31mL

References

 

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