sy-1365

InvivoChem Cat #:V4641CAS #:1816989-16-8Purity >=98%

Description: SY-1365 is a novlel, potent, highly selective and covalent/irreversible inhibitor of CDK7 (Cyclin-dependent kinase 7). SY-1365 possesses therapeutic potential in both hematological and solid tumors. In vitro, SY-1365 inhibited cell growth of many different cancer types at nanomolar concentrations. SY-1365 treatment decreased MCL1 protein levels, and cancer cells with low BCL2L1 (BCL-XL) expression were found to be more sensitive to SY-1365. Transcriptional changes in acute myeloid leukemia (AML) cell lines were distinct from those following treatment with other transcriptional inhibitors. SY-1365 demonstrated substantial antitumor effects in multiple AML xenograft models as a single agent; SY-1365–induced growth inhibition was enhanced in combination with the BCL2 inhibitor venetoclax. Antitumor activity was also observed in xenograft models of ovarian cancer, suggesting the potential for exploring SY-1365 in the clinic in both hematologic and solid tumors. Our findings support targeting CDK7 as a new approach for treating transcriptionally addicted cancers.

References: Cancer Res. 2019 May 7. pii: canres.0119.2019.

-20C for 3 years in powder form

Synonym: SY-1365; SY 1365; SY1365;
IUPAC/Chemical Name: N-[(1S, 3R)-3-[[5-Chloro-4-(1H-indol-3-yl)-2-pyrimidinyl]amino]-1-methylcyclohexyl]-5-[[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]amino]-2-pyridinecarboxamide
InChi Key: SCJNYBYSTCRPAO-LXBQGUBHSA-N
InChi Code: InChI=1S/C31H35ClN8O2/c1-31(39-29(42)26-13-12-21(17-33-26)36-27(41)11-7-15-40(2)3)14-6-8-20(16-31)37-30-35-19-24(32)28(38-30)23-18-34-25-10-5-4-9-22(23)25/h4-5, 7, 9-13, 17-20, 34H, 6, 8, 14-16H2, 1-3H3, (H, 36, 41)(H, 39, 42)(H, 35, 37, 38)/b11-7+/t20-, 31+/m1/s1
SMILES Code: O=C(C1=NC=C(NC(/C=C/CN(C)C)=O)C=C1)N[C]2(C)C[CH](NC3=NC=C(Cl)C(C4=CNC5=C4C=CC=C5)=N3)CCC2