A selective PI3Kβ/δ inhibitor (IC50 = 3

AZD 8186 – 25 mg

Brand:
Cayman
CAS:
1627494-13-6
Storage:
-20
UN-No:
De Minimis - 3077 / 9

AZD 8186 is a selective PI3Kβ/δ inhibitor that exhibits IC50 values of 3, 17, and 752 nM for PI3Kβ, δ, and α, respectively, in cells sensitive to isoform-specific PI3K inhibition.{33193,33194} It shows no significant binding against a panel of 442 other kinases when tested at a concentration of 10 µM and exhibits high oral efficacy in mouse cancer models.{33193} AZD 8186 inhibits growth of a range of cell lines, with preferential activity in cells with PTEN mutation or deficiency, and inhibits growth of prostate and triple negative breast cancer tumors in vivo, both as a single agent and in combination with docetaxel (Item No. 11637).{33194}  

 

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Description

A selective PI3Kβ/δ inhibitor (IC50 = 3, 17, and 752 nM for PI3Kβ, δ, and α, respectively); shows no significant binding against a panel of 442 other kinases; inhibits growth of a range of cell lines, with preferential activity in cells with PTEN mutation or deficiency; orally bioavailable

Formal name: 8-[(1R)-1-[(3,5-difluorophenyl)amino]ethyl]-N,N-dimethyl-2-(4-morpholinyl)-4-oxo-4H-1-benzopyran-6-carboxamide

Synonyms: 

Molecular weight: 457.5

CAS: 1627494-13-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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