Dalpiciclib free base

Dalpiciclib, also known as SHR-6390, is a cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. SHR6390 exhibited potent antiproliferative activity against a wide range of human RB‐positive tumor cells in vitro, and exclusively induced G1 arrest as well as cellular senescence, with a concomitant reduction in the levels of Ser780‐phosphorylated RB protein. Compared with the well‐known CDK4/6 inhibitor palbociclib, orally administered SHR6390 led to equivalent or improved tumor efficacy against a panel of carcinoma xenografts, and produced marked tumor regression in some models, in association with sustained target inhibition in tumor tissues. Furthermore, SHR6390 overcame resistance to endocrine therapy and HER2‐targeting antibody in ER‐positive and HER2‐positive breast cancer, respectively. Moreover, SHR6390 combined with endocrine therapy exerted remarkable synergistic antitumor activity in ER‐positive breast cancer.

Product information

CAS Number: 1637781-04-4

Molecular Weight: 446.54

Formula: C25H30N6O2

Chemical Name: 6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperidin-4-yl)pyridin-2-yl]amino}pyrido[2, 3-d]pyrimidin-7(8H)-one

Smiles: CC(=O)C1C(=O)N(C2CCCC2)C2=NC(NC3=CC=C(C=N3)C3CCNCC3)=NC=C2C=1C

InChiKey: SGJLSPUSUBJWHO-UHFFFAOYSA-N

InChi: InChI=1S/C25H30N6O2/c1-15-20-14-28-25(29-21-8-7-18(13-27-21)17-9-11-26-12-10-17)30-23(20)31(19-5-3-4-6-19)24(33)22(15)16(2)32/h7-8,13-14,17,19,26H,3-6,9-12H2,1-2H3,(H,27,28,29,30)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Mezni E, Sabatier R, Goncalves A, Vicier C. Actualités 2021 sur le cancer du sein localement avancé ou métastatique RH+/HER2− [Updates in hormone-receptor- positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer in 2021]. Bull Cancer. 2022 Feb;109(2):216-225. French. doi: 10.1016/j.bulcan.2021.12.009. Epub 2022 Feb 1. PMID: 35115114.
2. Wang Y, Yuan X, Li J, Liu Z, Li X, Wang Z, Wei L, Li Y, Wang X. The Synergistic Effects of SHR6390 Combined With Pyrotinib on HER2+/HR+ Breast Cancer. Front Cell Dev Biol. 2021 Dec 16;9:785796. doi: 10.3389/fcell.2021.785796. PMID: 34977029; PMCID: PMC8716872.
3. Zhang P, Xu B, Gui L, Wang W, Xiu M, Zhang X, Sun G, Zhu X, Zou J. A phase 1 study of dalpiciclib, a cyclin-dependent kinase 4/6 inhibitor in Chinese patients with advanced breast cancer. Biomark Res. 2021 Apr 12;9(1):24. doi: 10.1186/s40364-021-00271-2. PMID: 33845905; PMCID: PMC8042970.

Products are for research use only. Not for human use.