GSK2636771 free base · Synonyms: GSK-2636771 · GSK 2636771

GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ.

For research use only. Not for human or veterinary use.

Target PI3K

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

GSK2636771 structure

CAS No.: 1372540-25-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 480.00	BP-02304-500mg	Inquire	Get quote
1 g	USD 760.00	BP-02304-1g	In stock	Get quote
2 g	USD 1,220.00	BP-02304-2g	In stock	Get quote
3 g	USD 1,470.00	BP-02304-3g	In stock	Get quote
5 g	USD 1,960.00	BP-02304-5g	In stock	Get quote
10 g	USD 3,130.00	BP-02304-10g	In stock	Get quote

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Description

GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.

Biological activity

In Vitro GSK2636771 treatment causes cell viability significantly more decreased in the control cells (p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines) than in PTEN-mutant and PTEN wild-type EEC cells. Inhibition of p110β by GSK2636771 or AZD6482 leads to a marked decrease of AKT phosphorylation only in the control prostate and breast cancer cell lines, whereas only marginal effects on AKT activation are observed in EEC cells. 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.

Identifiers

SMILES: CC1=NC2=C(C=C(C=C2N1CC1=CC=CC(=C1C)C(F)(F)F)N1CCOCC1)C(O)=O
InChIKey: XTKLTGBKIDQGQL-UHFFFAOYSA-N

Specifications

MW (average): 433.4236
Formula: C₂₂H₂₂F₃N₃O₃
CAS No.: 1372540-25-4
Physical state: Solid
Color: White to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Weigelt B, et al. PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clin Cancer Res. 2013, 19(13), 3533-3544.

[2]. Hosford SR, et al. Combined inhibition of both p110α and p110β isoforms of phosphatidylinositol 3-kinase is required for sustained therapeutic effect in PTEN-deficient, ER+ breast cancer. Clin Cancer Res. 2016 Nov 30

Same target

Search PI3K

Same research area

Search Cancer