Dalpiciclib

SKU: orb1297963

Description

Dalpiciclib (SHR-6390) is a potent and selective oral inhibitor of CDK4/6, exhibiting antitumor activity in models such as esophageal squamous cell carcinoma. It functions by inhibiting Rb phosphorylation, inducing G1 arrest, and has demonstrated efficacy in both in vitro and in vivo studies across various cancer research fields.

Research Area

Cell Biology

Key Properties

• CAS Number: 1637781-04-4
• MW: 446.54
• Purity: 99.69% (May vary between batches)
• Formula: C₂₅H₃₀N₆O₂
• SMILES: O=C1N(C=2C(C(C)=C1C(C)=O)=CN=C(NC3=CC=C(C=N3)C4CCNCC4)N2)C5CCCC5
• Target: CDK
• Solubility: DMSO:< 1 mg/mL (insoluble)

Bioactivity

• Target IC50:
  CDK6:9.9 nM|CDK4:12.4 nM
• In Vivo:
  Dalpiciclib administered at 150 mg/kg weekly for 3 weeks by oral gavage has antitumor activity in ESCC xenografts. Dalpiciclib in combination with Paclitaxel or Cisplatin provides synergistic inhibition in ESCC xenografts.
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• In Vitro:
  Dalpiciclib inhibits cell proliferation in a dose-dependent manner following administration of 0-4 μM for 72 hours.In the relative sensitive Eca 109 and KYSE-510 cell lines, Dalpiciclib significantly blocks Rb phosphorylation at serine 780 after 24 hours of administration and induces cell cycle arrest but not in relative resistant Eca 9706 cell line.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CDK, CDK4, CDK6, Cyclin dependent kinase, Dalpiciclib, Eca 109, Eca 9706, and KYSE-510 ESCC, antitumor activity, BT-474/T, inhibit, MCF7, MCF7/TR, Inhibitor, SHR6390, SHR-6390, SHR 6390

Compound Identifiers

PubChem CID

86279927