Lerociclib (G1T38)

Description: Lerociclib (G1T38) is a novel, potent, orally bioavailable and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively. Lerociclib has the potential for the treatment of Rb competent tumors. Biochemical profiling demonstrates G1T38 is a competitive, nanomolar inhibitor of CDK4/6 with highly selectivity for CDK4-cyclin D1 and CDK6-cyclin D3. G1T38 exhibits a low EC50 (< 100 in='' rb='' competent='' cell='' lines='' compared='' to=''> 3 uM in Rb null cells. In vivo, daily oral treatment with G1T38 causes significant, durable growth inhibition of tumors in a HER2/neu GEMM and in MCF7 xenograft breast cancer models.

References: Oncotarget. 2017 Jun 27; 8(26):42343-42358.

Related CAS: 2097938-59-3 (HCl) 1628256-23-4 (free base)

Chemical Name: 2'-((5-(4-isopropylpiperazin-1-yl)pyridin-2-yl)amino)-7', 8'-dihydro-6'H-spiro[cyclohexane-1, 9'-pyrazino[1', 2':1, 5]pyrrolo[2, 3-d]pyrimidin]-6'-one

InChi Key: YPJRHEKCFKOVRT-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H34N8O/c1-18(2)32-10-12-33(13-11-32)20-6-7-22(27-16-20)30-25-28-15-19-14-21-24(35)29-17-26(8-4-3-5-9-26)34(21)23(19)31-25/h6-7, 14-16, 18H, 3-5, 8-13, 17H2, 1-2H3, (H, 29, 35)(H, 27, 28, 30, 31)
SMILES Code: CC(C)N(CC1)CCN1C(C=N2)=CC=C2NC3=NC=C4C(N(C5(CCCCC5)CNC6=O)C6=C4)=N3