1. Cell Cycle/DNA Damage
  2. CDK
  3. Dalpiciclib

Dalpiciclib (Synonyms: SHR-6390)

Cat. No.: HY-114338
Handling Instructions

Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM). Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest.

For research use only. We do not sell to patients.

Dalpiciclib Chemical Structure

Dalpiciclib Chemical Structure

CAS No. : 1637781-04-4

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Description

Dalpiciclib (SHR-6390) is a highly selective, orally bioavailable CDK4/6 inhibitor with comparable potencies against CDK4 (IC50=12.4 nM) and CDK6 (IC50=9.9 nM). Dalpiciclib exerts potent antitumor activity in esophageal squamous cell carcinoma by inhibiting phosphorylated tumor-suppressor retinoblastoma protein (Rb) and inducing G1 cell cycle arrest[1][2].

IC50 & Target[1]

CDK4

12.4 nM (IC50)

CDK6

9.9 nM (IC50)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

446.54

Formula

C₂₅H₃₀N₆O₂

CAS No.
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Dalpiciclib
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HY-114338
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