NSC781406

Product NameNSC781406
CAS1676893-24-5
MFC29H27F2N5O5S2
MW627.68
EINECS
MOL File1676893-24-5.mol

Chemical Properties

Boiling point	775.1±70.0 °C(Predicted)
Density	1.52±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMF: 10mg/mL; DMSO: 20mg/mL; DMSO:PBS (pH 7.2) (1:4): 0.2mg/mL
form	A solid
pka	6.23±0.40(Predicted)
color	White to off-white

Usage And Synthesis

Description

NSC 781406 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC₅₀s = 2.0, 9.4, 2.7, 14, and 5.4 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, and mTOR, respectively). It inhibits cell growth in the NCI-60 panel of cancer cell lines (mean GI₅₀ = 65 nM). NSC 781406 (30 mg/kg) reduces tumor volume in a BEL-7404 hepatic cancer mouse xenograft model.

Uses

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].

IC 50

PI3Kα: 2 nM (IC₅₀); PI3Kγ: 2.7 nM (IC₅₀); PI3Kβ: 9.4 nM (IC₅₀); PI3Kδ: 14 nM (IC₅₀); mTOR: 5.4 nM (IC₅₀)

References

[1] Chen Y, et al. Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. Bioorg Med Chem. 2016 Mar 1;24(5):957-66. DOI:10.1016/j.bmc.2016.01.008