Dalpiciclib

Dalpiciclib (SHR-6390) is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4 nM and 9.9 nM, respectively[1][2]. Dalpiciclib shows antitumor activity against breast cancer and esophageal squamous cell carcinoma[1][2][3][4].

Product Specifications

CAS Number

[1637781-04-4]

Product Name Alternative

SHR-6390

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

CDK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/dalpiciclib.html

Purity

99.70

Solubility

1 M HCl : 5 mg/mL (ultrasonic; warming; heat to 60°C) |DMSO : 50 mg/mL (ultrasonic; warming; adjust pH to 7 with 1 M HCl; heat to 60°C)

Smiles

O=C1C(C(C)=O)=C(C)C2=C(N1C3CCCC3)N=C(NC4=NC=C(C5CCNCC5)C=C4)N=C2

Molecular Formula

C25H30N6O2

Molecular Weight

446.54

Precautions

H302, H315, H319

References & Citations

[1]Jose Manuel Perez-Garcia, et al. Perez-Garcia JM, Cortes J, Llombart-Cussac A. CDK4/6 inhibitors in breast cancer: spotting the difference. Nat Med. 2021 Nov;27 (11) :1868-1869.|[2]Pin Zhang, 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 Apr 12;9 (1) :24.|[3]Jiayuan Wang, 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 Jun 2;15 (1) :127.|[4]Fei Long, et al. Preclinical characterization of SHR6390, a novel CDK 4/6 inhibitor, in vitro and in human tumor xenograft models. Cancer Sci. 2019 Apr;110 (4) :1420-1430.