CDK9-IN-28
PROTAC CDK9/CycT1 Degrader-1 (compounds 10) is a potent inhibitor of CDK9. PROTAC CDK9/CycT1 Degrader-1 can be used as a PROTAC target protein ligand for PROTAC synthesis. PROTAC CDK9/CycT1 Degrader-1 shows strong anti-proliferative activity in solid tumors.
For research use only. We do not sell to patients.
- CAS No.: 3020773-81-0
- Formula: C32H40N4O6S2
- Molecular Weight:640.81
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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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CDK9/cyclinT1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U2932 | IC50 |
45 nM
Compound: 10
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Cytotoxicity against human U2932 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
Cytotoxicity against human U2932 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay
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[PMID: 37671907] |
CDK9-IN-28 shows obvious CDK9 degradation in U-2932 cells and has obvious anti-proliferation activity in tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U-2932 cells
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Concentration:100nM
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Incubation Time:6h
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Result:CDK9 degradation induced apoptosis, and degradation through autophagy.
CDK9-IN-28 (1mg/kg, i.v.,5 mg/kg, i.p., 15 days) exhibits an acceptable half-life (T1/2:4.66h) and moderate bioavailability (F = 43.1%) in ICR (CD-1) mice model[1].
Pharmacokinetic Analysis[1]
| T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0-t (h*ng/mL) | CL_obs(mL/min/kg) | MRTINF_obs (h) | Vss_obs (mL/kg) | F (%) | |
| i.p. 5 mg/kg | 4.66 | 0.25 | 88.4 | 156 | / | 4.17 | / | 43.1 |
| i.v. 1 mg/kg | 1.97 | / | / | 72.3 | 229 | 0.79 | 10480 | / |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV4-11 tumor nude mice
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection, once a day for 15 days.
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Result:Effective delayed of tumor growth but weight did not lose.
Chemical Information
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CAS No. 3020773-81-0
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Molecular Weight 640.81
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Formula C32H40N4O6S2
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SMILES
CC(C)(C1=CN=C(O1)CSC2=CN=C(S2)NC(C3CCN(CC3)CCCCCOC4=C5C(OC(C=C5C)=O)=CC(O)=C4)=O)C
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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)
CDK9-IN-28 Related Classifications
HY-156083 Related Classifications
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