2. Cell Cycle/DNA Damage
  3. CDK
  4. 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.

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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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Dalpiciclib Related Antibodies

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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.

Dalpiciclib Related Antibodies

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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Dalpiciclib Related Classifications

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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.

Keywords:

Dalpiciclib1637781-04-4SHR-6390SHR6390SHR 6390CDKCyclin dependent kinaseantitumor activityEca 109Eca 9706and KYSE-510 ESCCMCF7MCF7/TRBT-474/TInhibitorinhibitorinhibit

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