1. Cell Cycle/DNA Damage
    Apoptosis
  2. CDK
    Apoptosis
  3. CDK4/6-IN-10

CDK4/6-IN-10 

Cat. No.: HY-115993
Handling Instructions

CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC50s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM).

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

CDK4/6-IN-10 Chemical Structure

CDK4/6-IN-10 Chemical Structure

CAS No. : 2688098-11-3

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC50s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM)[1].

IC50 & Target[1]

CDK4

22 nM (IC50)

CDK6/cyclinD1

10 nM (IC50)

In Vitro

CDK4/6-IN-10 (compouns 32) (1 µM) shows kinase selectivity with IC50s of 22 nM and 10 nM for CDK4 and CDK6, respectively[1].
CDK4/6-IN-10 (72 h) shows antiproliferative activity (GI50s of 2.028, 5.802, 2.286, 2.238, 1.526, 11.381 µM for RPMI-8226, U266, K562, HL-60, 22RV1, HEK-293 cells, respectively)[1].
CDK4/6-IN-10 (0, 1.5, 3, 6 µM, 24 h) induces cell cycle arrest at the G1 phase in a concentration-dependent manner[1].
CDK4/6-IN-10 ( 0, 1, 2, 3 µM, 24 h) induces apoptosis of RPMI-8226 cells in a concentration-dependent manner[1].
CDK4/6-IN-10 (0, 1.5, 3, 6 µM, 24 h) reduces the CDK4/6 activity by decreases the expression level of p-RB, c-MYC and BCL-2[1].

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

Cell Proliferation Assay[1]

Cell Line: RPMI-8226, U266, K562, HL-60, 22RV1, HEK-293 cells
Concentration:
Incubation Time: 72 h
Result: Shows antiproliferative activity (GI50s of 2.028, 5.802, 2.286, 2.238, 1.526, 11.381 µM for RPMI-8226, U266, K562, HL-60, 22RV1, HEK-293 cells, respectively).

Cell Cycle Analysis[1]

Cell Line: RPMI-8226 cells
Concentration: 0, 1.5, 3, 6 µM
Incubation Time: 24 h
Result: Cells were arrested at the G1 phase in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: RPMI-8226 cells
Concentration: 0, 1.5, 3, 6 µM
Incubation Time: 24 h
Result: Reduced the CD4/K activity by decreased the expression level of p-RB, c-MYC and BCL-2.
In Vivo

CDK4/6-IN-10 (1000, 5000, 10000 mg/kg; p.o.) shows safety profile with LD50 much higher than 10,000 mg/kg[1].
CDK4/6-IN-10 (10 mg/kg; p.o.) shows oral bioavailability (F=51%) in SD rats[1].
CDK4/6-IN-10 (100, 200 mg/kg; p.o., once a day for 19 days) shows antitumor potency and favorable safety profile[1].
Pharmacokinetic Parameters of CDK4/6-IN-10 in SpragueeDawley rats[1].

Compd Admin. Cmax (ng/mL) AUC0-t (h·ng/mL) MRT0-t (h) Tmax (h) t1/2 (h) CL (mL/h/kg) F (%)
32 i.v. 355 960 5.9 0.033 8.9 641 -
p.o. 257 4,878 12.8 10.7 >24 524 51
SpragueeDawley rats, 10 mg/kg, p.o.

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

Animal Model: ICR mice[1]
Dosage: 1000, 5000, 10000 mg/kg
Administration: p.o.
Result: Showed safety profile with LD50 much higher than 10,000 mg/kg.
Animal Model: SpragueeDawley rats[1]
Dosage: 10 mg/kg
Administration: p.o.
Result: Showed oral bioavailability (F=51%).
Animal Model: BALB/c nude mice (6-8 weeks) (MM xenograft model)[1]
Dosage: 100, 200 mg/kg
Administration: p.o., once a day, 19 days
Result: Showed antitumor potency and favorable safety profile.
Molecular Weight

418.47

Formula

C22H23FN8

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CDK4/6-IN-10
Cat. No.:
HY-115993
Quantity:
MCE Japan Authorized Agent: