PI3K-IN-63 

PI3K-IN-63 (compound 9) is a PI3Kα inhibitor with a K_i of 0.35 nM against human targets. PI3K-IN-63 inhibits the phosphorylation of AKT at the S473 site in cellular assays. PI3K-IN-63 reduces the viability of non-small cell lung cancer cell lines carrying PIK3CA mutations. PI3K-IN-63 can be used in studies related to non-small cell lung cancer^[1].

PI3K-IN-63 (compound 9) potently inhibits purified PI3Kα enzyme with a K_i of 0.35 nM and exhibits greater than 7000-fold selectivity over purified mTOR enzyme^[1].
PI3K-IN-63 is more active in NSCLC cell lines harboring PIK3CA mutations than in other tested cancer cell lines^[1].
PI3K-IN-63 (3 μM) has favorable in vitro metabolic stability (HLM ER = 0.3) and does not significantly inhibit major CYP enzymes at 3 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

406.29

C₁₇H₁₃Cl₂N₅OS

1202041-71-1

N#CC1=C(SC(C2=NN=CN2)=C1C=3C=CC(Cl)=CC3Cl)N4CCOCC4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Liu KK, et al. Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity. ACS Med Chem Lett. 2011;2(11):809-813. Published 2011 Sep 19.  [Content Brief]