Dalpiciclib|CAS 1637781-04-4|DC Chemicals

Cas No.:	1637781-04-4
Chemical Name:	Dalpiciclib free base
Synonyms:	SHR-6390; SHR6390; SHR 6390; Dalpiciclib;
SMILES:	O=C1C(C(C)=O)=C(C)C2=CN=C(NC3=NC=C(C4CCNCC4)C=C3)N=C2N1C5CCCC5
Formula:	C₂₅H₃₀N₆O₂
M.Wt:	446.555
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. Zhang P, et al. A phase 1 study of dalpiciclib, a cyclin-dependent kinase 4/6 inhibitor in Chinese patients with advanced breast cancer. Biomark Res. 2021;9(1):24. Published 2021 Apr 12. [2]. Wang J, et al. CDK4/6 inhibitor-SHR6390 exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated Rb and inducing G1 cell cycle arrest. J Transl Med. 2017;15(1):127. Published 2017 Jun 2.

Target:	CDK4:12.4 nM (IC50) CDK6:9.9 nM (IC50)
In Vivo:	Dalpiciclib (SHR-6390) (150 mg/kg; oral gavage; weekly for 3 weeks) shows antitumor activity against ESCC xenografts[2]. Dalpiciclib combines with Paclitaxel (PTX) or Cisplatin (CDDP) offered synergistic inhibitory effects in ESCC xenografts[2]. Animal Model: NOD/SCID mice (ESCC PDXs models) [2] Dosage: 150 mg/kg Administration: Oral gavage; weekly for 3 weeks Result: The growth of tumor was significantly suppressed in SHR6390 treatment group with various suppressions.
In Vitro:	Dalpiciclib (SHR-6390) (0-4 μM) inhibits cell proliferation in a dose-dependent manner[2]. Dalpiciclib (24 hours) significantly blocks phosphorylation of Rb at serine 780 in relative sensitive Eca 109 and KYSE-510 cell lines, but not in relative resistant Eca 9706 cell line.Dalpiciclib induces cell cycle arrest at G1 phase in Eca 109 and KYSE-510 cell lines[2]. Cell Proliferation Assay[2] Cell Line: Eca 109, Eca 9706, and KYSE-510 ESCC cell lines Concentration: 0-4 μM Incubation Time: 72 hours Result: Inhibited cell proliferation in a dose-dependent manner, with Eca 109 being the relative sensitive one and Eca 9706 being the relative resistant one.
References:	[1]. Zhang P, et al. A phase 1 study of dalpiciclib, a cyclin-dependent kinase 4/6 inhibitor in Chinese patients with advanced breast cancer. Biomark Res. 2021;9(1):24. Published 2021 Apr 12. [2]. Wang J, et al. CDK4/6 inhibitor-SHR6390 exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated Rb and inducing G1 cell cycle arrest. J Transl Med. 2017;15(1):127. Published 2017 Jun 2.

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