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

Dalpiciclib  (Synonyms: SHR-6390)

Cat. No.: HY-114338 Purity: 99.40%
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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. Dalpiciclib shows antitumor activity against breast cancer and esophageal squamous cell carcinoma.

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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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target[1]

CDK4

12.4 nM (IC50)

CDK6

9.9 nM (IC50)

In Vitro

Dalpiciclib (0-4 μM, 72 h) inhibits cell proliferation in a dose-dependent manner[3].
Dalpiciclib (0-10 μM, 6 d) inhibits the proliferation of retinoblastoma-positive tumor cell lines[4].

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

Cell Proliferation Assay[3]

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.

Cell Viability Assay[4]

Cell Line: MCF7, MCF7/TR, BT-474/T cell lines
Concentration: 0-10 μM
Incubation Time: 6  days
Result: Inhibited MCF7/TR cells, parental MCF7 cells and BT-474/T resistant cells with the IC50 values of 229.5, 115.4 and 210.7 nM, respectively.
In Vivo

Dalpiciclib (oral gavage; 150 mg/kg; once weekly; 3 weeks) shows antitumor activity against ESCC xenografts[3].
Dalpiciclib combined with Paclitaxel (PTX) or Cisplatin (CDDP) offer synergistic inhibitory effects in ESCC xenografts[3].
Dalpiciclib (oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days) shows antitumor activity in human xenograft models [4].

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

Animal Model: NOD/SCID mice (ESCC PDXs models) [3]
Dosage: 150 mg/kg
Administration: Oral gavage; 150 mg/kg; once weekly; 3 weeks
Result: Suppressed the growth of tumor.
Animal Model: 5-week-old female Balb/cA-nude mice subcutaneously inoculated MCF7/ARO, COLO 205 and U87MG[4]
Dosage: 37.5 mg/kg, 75 mg/kg, 150 mg/kg
Administration: Oral gavage; 37.5 mg/kg, 75 mg/kg, 150 mg/kg; once daily; 30 days
Result: Caused regression of all tumor xenografts at the highest dose tested.
Clinical Trial
Molecular Weight

446.54

Formula

C25H30N6O2

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Dalpiciclib
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HY-114338
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