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

Cimpuciclib is a selective CDK4 inhibitor (IC50: 0.49 nM) that has anti-tumor activity.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Cimpuciclib tosylate) usually boasts enhanced water solubility and stability.

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

Cimpuciclib Chemical Structure

Cimpuciclib Chemical Structure

CAS No. : 2202767-78-8

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Description

Cimpuciclib is a selective CDK4 inhibitor (IC50: 0.49 nM) that has anti-tumor activity[1].

IC50 & Target[1]

CDK4

0.49 nM (IC50)

CDK6

9.56 nM (IC50)

In Vitro

Cimpuciclib (example 63, 141.2 nM, 6 days) inhibits proliferation in colo205 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: Colo205 cells
Concentration: 0-500 nM approximately
Incubation Time: 6 days
Result: Inhibited cell proliferation with an IC50 value of 141.2 nM.
In Vivo

Cimpuciclib (example 63, 50 mg/kg, oral gavage, twice a week) inhibits tumor growth in colo205 tumor-bearing mice[1].
Cimpuciclib (5 mg/kg for rats, 50 mg/kg for colo205 tumor-bearing mice, oral administration) shows slow metabolic rate and maintains high concentration in the plasma[1].

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

Animal Model: Colo205 tumor-bearing mice[1]
Dosage: 50 mg/kg, twice a week
Administration: Oral gavage
Result: Inhibited tumor growth by 93.63%.
Animal Model: Rats, colo205 tumor-bearing mice[1]
Dosage: 5 mg/kg for rats, 50 mg/kg for colo205 tumor-bearing mice.
Administration: Oral administration
Result: Pharmacokinetic profile of Cimpuciclib (example 63).
dose (mg/kg) Cmax (ng/mL) Tmax (h) AUC0-24 (ng/mL•h) t1/2 (h)
5 mg/kg (rats) 559.7 6 5414 2.4
50 mg/kg (mice) 7960 1 136782 14.8
Molecular Weight

542.65

Formula

C30H35FN8O

CAS No.
SMILES

O=C(N1CCC(CC1)NC2CC2)C3=CC=C(NC4=NC(C5=CC6=C(N=C(C)N6C(C)C)C=C5)=C(F)C=N4)N=C3C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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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Product Name:
Cimpuciclib
Cat. No.:
HY-112243
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