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).
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- CAS No.: 2688098-11-3
- Formule: C22H23FN8
- Masse moléculaire:418.47
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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CDK4 22 nM (IC50) |
CDK6/cyclinD1 10 nM (IC50) |
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.
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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.
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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Masse moléculaire 418.47
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK4/6-IN-10 Related Classifications
HY-115993 Related Classifications
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