CDK2/4/6-IN-1
CDK2/4/6-IN-1(example 29) is a CDK2/4/6 inhibitor with IC50 values of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6, respectively. CDK2/4/6-IN-1 can be used in cancer research. CDK2/4/6-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
For research use only. We do not sell to patients.
- CAS No.: 2803837-13-8
- Formula: C22H22N4O4S
- Molecular Weight:438.50
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CDK2 2.5 nM (IC50) |
CDK4 23.7 nM (IC50) |
CDK6 44.3 nM (IC50) |
CDK2/4/6-IN-1(example 29) (0-600 nM, 24 h) inhibits the proliferation of OVCAR3 and MCF7 cells with the IC50 values of 14.6 and 117.8 nM, respectively[1].
CDK2/4/6-IN-1(example 29) (0-600 nM, 24 h) inhibits phosphorylation of Rb protein in OVCAR3 and MCF7 cells with the IC50 values of 18 and 581 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
The pharmacokinetic parameters of example 29 in BALB/c mice (10 mg/kg, p.o.)
| Parameters | Cmax(ng/mL) | Tmax(hr) | AUClast(hr*ng/mL) | T1/2(hr) |
| PO | 4050 | 0.5 | 10050 | 4.8 |
| Parameters | C0(ng/mL) | T1/2(hr) | AUClast(hr*ng/mL) | Vss(L/Kg) |
| IV | 4407 | 0.7 | 3245 | 0.9 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2803837-13-8
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Molecular Weight 438.50
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Formula C22H22N4O4S
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SMILES
O=S(C1=CC=C(NC2=NC=C3C(N([C@@H]4CCC[C@]4(O)C)C(C(C#C)=C3)=O)=N2)C=C1)(C)=O
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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