Briciclib

• CAT Number: I005206
• CAS Number: 865783-99-9
• Molecular Formula: C19H23O10PS
• Molecular Weight: 474.42
• Purity: ≥95%
• Target: Cyclin D1
• Solubility: DMSO: ≥ 31 mg/mL
• Storage: Store at -20°C
• IUPAC Name: [2-methoxy-5-[[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonylmethyl]phenyl] dihydrogen phosphate
• InChI: InChI=1S/C19H23O10PS/c1-25-14-10-17(27-3)15(18(11-14)28-4)7-8-31(23,24)12-13-5-6-16(26-2)19(9-13)29-30(20,21)22/h5-11H,12H2,1-4H3,(H2,20,21,22)/b8-7+
• InChIKey: LXENKEWVEVKKGV-BQYQJAHWSA-N
• SMILES: COC1=C(C=C(C=C1)CS(=O)(=O)/C=C/C2=C(C=C(C=C2OC)OC)OC)OP(=O)(O)O

Briciclib（Cat No.:I005206）is a small molecule inhibitor targeting the cyclin-dependent kinase (CDK) family, specifically CDK9. By inhibiting CDK9, briciclib disrupts the phosphorylation of RNA polymerase II, thereby interfering with transcriptional regulation and promoting apoptosis in cancer cells. This mechanism highlights its potential as an anticancer agent, particularly for hematological malignancies and solid tumors characterized by dysregulated CDK activity. Briciclib has shown promise in preclinical studies and early-phase clinical trials, with ongoing research focusing on its safety, efficacy, and potential combinations with other therapies to enhance cancer treatment outcomes.

Reference

[1]. Neel Jasani, et al. Abstract 1649: Potent anticancer activity of an orally bioavailable small molecule, ON 013100, and its water soluble derivative, briciclib, a clinical-stage eIF4E-targeted agent. Cancer Res August 1, 201575; 1649