NSC781406

Cas No.:	1676893-24-5
Chemical Name:	NSC781406,NSC-781406,NSC 781406
Synonyms:	NSC781406,NSC-781406,NSC 781406
SMILES:	COC1=C(C=C(C=N1)C2=CC3=C(C=CN=C3C=C2)C#CCN4CCN(CC4)S(=O)(=O)C)NS(=O)(=O)C5=C(C=C(C=C5)F)F
Formula:	C29H27F2N6O6S2
M.Wt:	627.68
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.
In Vivo:	In the xenograft models, treatment with 30 mg/kg of NSC781406 results in statistically significant antitumor activity, with a mean reduction in relative tumor volume ratio of 52%. Sorafenib displays an inhibition ratio of 44% at 50 mg/kg. NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight[1].
In Vitro:	NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC50=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20 nM). NSC781406 displays reasonable liver microsome stability. NSC781406 demonstrates cytotoxic activities against leukemia, non-small cell, lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. It is potent against 60 cancer cell lines with a mean GI50 value of 65 nM, and with a GI50 value less than 10 nM against four cancer cell lines[1].