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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- CAS No.: 3114520-65-6
- Formule: C32H31F2N5O2
- Masse moléculaire:555.62
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Voir tous les produits spécifiques à Isoform DNA/RNA Synthesis
More
Activité biologique
|
CDK9 2.2 nM (IC50) |
CDK2 268.3 nM (IC50) |
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 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.
-
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).
-
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.
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 No. 3114520-65-6
-
Masse moléculaire 555.62
-
Formule 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
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK9-IN-50 Related Classifications
HY-183710 Related Classifications
Powered by Bioz