CDK4/6-IN-10
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.
- CAS No.: 2688098-11-3
- Formula: C22H23FN8
- Molecular Weight:418.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:RPMI-8226, U266, K562, HL-60, 22RV1, HEK-293 cells
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Concentration:
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Incubation Time:72 h
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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).
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Cell Line:RPMI-8226 cells
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Concentration:0, 1.5, 3, 6 µM
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Incubation Time:24 h
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Result:Cells were arrested at the G1 phase in a concentration-dependent manner.
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Cell Line:RPMI-8226 cells
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Concentration:0, 1.5, 3, 6 µM
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Incubation Time:24 h
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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 (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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice[1]
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Dosage:1000, 5000, 10000 mg/kg
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Administration:p.o.
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Result:Showed safety profile with LD50 much higher than 10,000 mg/kg.
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Animal Model:SpragueeDawley rats[1]
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Dosage:10 mg/kg
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Administration:p.o.
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Result:Showed oral bioavailability (F=51%).
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Animal Model:BALB/c nude mice (6-8 weeks) (MM xenograft model)[1]
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Dosage:100, 200 mg/kg
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Administration:p.o., once a day, 19 days
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Result:Showed antitumor potency and favorable safety profile.
Chemical Information
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CAS No. 2688098-11-3
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Molecular Weight 418.47
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Formula C22H23FN8
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SMILES
CN1C=C(C2=NC(NC3=NC=C(CN4CCNCC4)C=C3)=NC=C2F)C5=CC=CN=C51
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK4/6-IN-10 Related Classifications
HY-115993 Related Classifications
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