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Art. -Nr.: HY-183710

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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.

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CAS. Nr.: 3114520-65-6
Formel: C₃₂H₃₁F₂N₅O₂
Molecular Weight:555.62

Speicherung:

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

CDK9-IN-50 Chemical Structure

CAS. Nr.: 3114520-65-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CDK9

2.2 nM (IC₅₀)

CDK2

268.3 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

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.

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	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	CL	V_d	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.

Chemical Information

CAS. Nr. 3114520-65-6
Molecular Weight 555.62
Formel C₃₂H₃₁F₂N₅O₂
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Liu W, et al. Structure-Based Drug Design to Identify Potent, Selective, and Orally Available Cyclin-Dependent Kinase 9 Inhibitors for the Treatment of Castration-Resistant Prostate Cancer. J Med Chem. 2026;69(9):11335-11364. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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CDK9-IN-50

Alle CDK Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

CDK9-IN-50 Related Classifications

HY-183710 Related Classifications