2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Apoptosis
  3. CDK Androgen Receptor c-Myc Apoptosis DNA/RNA Synthesis
  4. CDK9-IN-50

CDK9-IN-50 is a selective and orally active CDK9 inhibitor with an IC50 of 2.2 nM. CDK9-IN-50 targets a distinct CDK9-specific subpocket to disrupt RNA polymerase II Ser2 phosphorylation and downregulate short-lived oncoproteins, including AR-V7 and Myc. CDK9-IN-50 exhibits antiproliferative activity against cancer cells, induces apoptosis and induces tumor growth inhibition in CRPC orthotopic mice models. CDK9-IN-50 can be used for the research of cancer, such as prostate cancer.

For research use only. We do not sell to patients.

CDK9-IN-50

CDK9-IN-50 Chemical Structure

CAS No. : 3114520-65-6

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CDK9-IN-50 Related Antibodies

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Description

CDK9-IN-50 is a selective and orally active CDK9 inhibitor with an IC50 of 2.2 nM. CDK9-IN-50 targets a distinct CDK9-specific subpocket to disrupt RNA polymerase II Ser2 phosphorylation and downregulate short-lived oncoproteins, including AR-V7 and Myc. CDK9-IN-50 exhibits antiproliferative activity against cancer cells, induces apoptosis and induces tumor growth inhibition in CRPC orthotopic mice models. CDK9-IN-50 can be used for the research of cancer, such as prostate cancer[1].

IC50 & Target[1]

CDK9

2.2 nM (IC50)

CDK2

268.3 nM (IC50)

In Vitro

CDK9-IN-50 (Compound 91) potently inhibits CDK9/ with an IC50 of 2.2 nM, shows weak inhibition of CDK7 and CDK2, and is inactive against all other tested CDK family kinases[1].
CDK9-IN-50 (0.11-1 μM) potently inhibits the proliferation of 22Rv1 and C4-2 castration-resistant prostate cancer cells with a GI50 of 138 and 0.160 nM, and suppresses the migratory capacity[1].
CDK9-IN-50 (1 μM; 48 h) induces apoptosis in 41.4% of 22Rv1 castration-resistant prostate cancer cells[1].
CDK9-IN-50 (100-800 nM; 48 h) triggers pro-apoptotic signaling, downregulates key oncogenic and anti-apoptotic proteins[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CDK9-IN-50 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: 22Rv1 castration-resistant prostate cancer cells
Concentration: 0.33-1 μM
Incubation Time: long-term incubation for colony formation
Result: Markedly reduced 22Rv1 colony formation at both tested concentrations, showing superior potency compared to clinical CDK9 inhibitor KB-0742.

Apoptosis Analysis[1]

Cell Line: 22Rv1 castration-resistant prostate cancer cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Triggered total apoptosis in 41.4% of 22Rv1 cells, including 17.7% early apoptosis and 23.7% late apoptosis, showing more pronounced pro-apoptotic effects than KB-0742 (HY-137478).

Western Blot Analysis[1]

Cell Line: 22Rv1 castration-resistant prostate cancer cells
Concentration: 100, 111, 200, 333, 400, 800, 1000 nM
Incubation Time: 48 h
Result: Induced concentration-dependent upregulation of cleaved PARP and cleaved caspase-3, downregulation of survivin, AR, AR-V7, c-Myc, MCL-1, and XIAP, and suppression of RNA polymerase II Ser2 phosphorylation (p-PoLR2A) without altering total PoLR2A levels.
Did not alter phosphorylated Rb (p-Rb) or total Rb levels.
Suppressed RNA polymerase II Ser5 phosphorylation (p-Ser5) only at 800 nM.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ CL Vd F
Mice[1] 2 mg/kg i.v. 1.6 h 0.08 h 474.6 ng/mL 554.8 ng·h/mL 591.7 ng·h/mL 3.4 L/h/kg 8.1 L/kg /
Mice[1] 20 mg/kg p.o. 3.5 h 0.42 h 814.7 ng/mL 2279.1 ng·h/mL 2832.5 ng·h/mL / / 41 %
In Vivo

CDK9-IN-50 (Compound 91) (25-50 mg/kg; p.o.; daily for 14 days) achieves 66% tumor growth inhibition in an orthotopic CRPC xenograft mice model with a favorable safety profile[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Prostate cancer BALB/c-nu mice (2 months old)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: p.o.; daily for 14 days
Result: Achieved a 66% tumor growth inhibition (TGI) at 50 mg/kg.
Reduced proliferation marker Ki-67, antiapoptotic protein MCL-1, and androgen receptor (AR) expression in treated tumors with statistical significance.
Caused no significant body weight reduction.
Detected no statistically significant alterations in organ indices or liver/renal function parameters (ALT, AST, CRE, BUN).
Showed no structural or morphological abnormalities in major organs (heart, liver, spleen, lung, kidney) compared to controls.
Molecular Weight

555.62

Formula

C32H31F2N5O2
CAS No.
SMILES

N[C@@H]1CN(CC12CC2)C3=C(C=NC4=C3C=C(C=C4)C5=C(C=NC(NC(C6CC6)=O)=C5)F)C7=CC(OCC)=CC=C7F
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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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CDK9-IN-50 Related Classifications

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Help & FAQs
  • 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.

Keywords:

CDK9-IN-503114520-65-6CDKAndrogen Receptorc-MycApoptosisDNA/RNA SynthesisCyclin dependent kinaseMycPol IICDK9castration-resistant prostate cancer22Rv1AR-V7C4-2CDK2/CycA2CDK7Inhibitorinhibitorinhibit

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