1. Cell Cycle/DNA Damage
  2. CDK
  3. 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.

CDK9-IN-28 Chemical Structure

CDK9-IN-28 Chemical Structure

CAS No. : 3020773-81-0

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Description

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[1].

IC50 & Target

CDK9/cyclinT1

 

In Vitro

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.

Western Blot Analysis[1]

Cell Line: U-2932 cells
Concentration: 100nM
Incubation Time: 6h
Result: CDK9 degradation induced apoptosis, and degradation through autophagy.
In Vivo

CDK9-IN-28 (5 mg/kg, i.p., once a day for 15 days) inhibits the growth of tumors in MV4-11 Tumor Nude mice model[1].
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]
药代动力学分析[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.

Animal Model: MV4-11 tumor nude mice
Dosage: 5 mg/kg
Administration: Intraperitoneal injection, once a day for 15 days.
Result: Effective delayed of tumor growth but weight did not lose.
Molecular Weight

640.81

Formula

C32H40N4O6S2

CAS No.
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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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CDK9-IN-28
Cat. No.:
HY-156083
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