[CAS NO. 1372540-25-4] GSK2636771
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PRODUCTS SPECIFICATIONS [1372540-25-4]
Store
Catalog
SLK-S8002
Brand
Selleck
CAS
1372540-25-4
DESCRIPTION [1372540-25-4]
Overview
| MDL | MFCD22417098 |
|---|---|
| Molecular Weight | 433.42 |
| Molecular Formula | C22H22F3N3O3 |
| SMILES | O=C(C1=C2C(N(CC3=CC=CC(C(F)(F)F)=C3C)C(C)=N2)=CC(N4CCOCC4)=C1)O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3072 mL | 11.5362 mL | 23.0723 mL |
| 5 mM | 0.4614 mL | 2.3072 mL | 4.6145 mL |
| 10 mM | 0.2307 mL | 1.1536 mL | 2.3072 mL |
| 50 mM | 0.0461 mL | 0.2307 mL | 0.4614 mL |
Description
GSK2636771 is a potent, orally bioavailable and selective inhibitor of with >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ. Sensitive to PTEN null cell lines.
Targets
| PI3Kβ [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, and leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines.
In vivo
GSK-2636771 decreases phosphorylated protein kinase Akt (Ser473) levels in these xenograft models. GSK-2636771 (100 mg/kg) do not increase glucose/insulin levels in mice.
References
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