GDC-mTOR inhibitor

Short Summary : MTOR inhibitor

Category : PI3K/Akt/mTOR Signaling|mTOR

Purity : 0.98

CAS Number : 1207358-59-5

Formula : C25H30N8O2

Molecular Weight : 474.56

SMILE : CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CCN(C3)C4=NC=CC=N4)C(=N2)N5CCOCC5C

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : Description:
IC50 Value: 1.5nM (Ki)
GDC-mTOR inhibitor is a potent and selective ATP-competitive inhibitor of mTOR. It’s derivative drug, GDC-0349, demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models.
Abstract: Selective inhibitors of mammalian target of rapamycin (mTOR) kinase based upon saturated heterocycles fused to a pyrimidine core were designed and synthesized. Each series produced compounds with Ki 500-fold selectivity over closely related PI3 kinases. This potency translated into strong pathway inhibition, as measured by phosphorylation of mTOR substrate proteins and antiproliferative activity in cell lines with a constitutively active PI3K pathway. Two compounds exhibiting suitable mouse PK were profiled in in vivo tumor models and were shown to suppress mTORC1 and mTORC2 signaling for over 12 h when dosed orally. Both compounds were additionally shown to suppress tumor growth in vivo in a PC3 prostate cancer model over a 14 day study.

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