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

Dalpiciclib hydrochloride  (Synonyms: SHR-6390 hydrochloride)

Cat. No.: HY-114338A Purity: 98.22%
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Dalpiciclib (SHR-6390) hydrochloride 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 hydrochloride shows antitumor activity against breast cancer and esophageal squamous cell carcinoma.

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

Dalpiciclib hydrochloride Chemical Structure

Dalpiciclib hydrochloride Chemical Structure

CAS No. : 2891598-76-6

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Based on 1 publication(s) in Google Scholar

Other Forms of Dalpiciclib hydrochloride:

Dalpiciclib hydrochloride Related Antibodies

Top Publications Citing Use of Products

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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Description

Dalpiciclib (SHR-6390) hydrochloride 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 hydrochloride shows antitumor activity against breast cancer and esophageal squamous cell carcinoma[1][2][3][4].

IC50 & Target

CDK6

9.9 nM (IC50)

CDK4

12.4 nM (IC50)

In Vitro

Dalpiciclib hydrochloride (0-4 μM, 72 h) inhibits cell proliferation in a dose-dependent manner[3].
Dalpiciclib hydrochloride (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 hydrochloride 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 hydrochloride (oral gavage; 150 mg/kg; once weekly; 3 weeks) shows antitumor activity against ESCC xenografts[3].
Dalpiciclib hydrochloride combined with Paclitaxel (PTX) or Cisplatin (CDDP) offer synergistic inhibitory effects in ESCC xenografts[3].
Dalpiciclib hydrochloride (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

483.01

Formula

C25H31ClN6O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C(C(C)=O)=C(C)C2=C(N1C3CCCC3)N=C(NC4=NC=C(C5CCNCC5)C=C4)N=C2.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (10.35 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0704 mL 10.3518 mL 20.7035 mL
5 mM 0.4141 mL 2.0704 mL 4.1407 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0704 mL 10.3518 mL 20.7035 mL 51.7588 mL
5 mM 0.4141 mL 2.0704 mL 4.1407 mL 10.3518 mL
10 mM 0.2070 mL 1.0352 mL 2.0704 mL 5.1759 mL
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Dalpiciclib hydrochloride Related Classifications

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:

Dalpiciclib2891598-76-6SHR-6390SHR6390SHR 6390CDKCyclin dependent kinaseantitumor activityEca 109Eca 9706and KYSE-510 ESCCMCF7MCF7/TRBT-474/TInhibitorinhibitorinhibit

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