CDK11-IN-1 hydrochloride
CDK11-IN-1 hydrochloride is a potent, highly selective, and orally active CDK11 inhibitor with an IC50 of 4 nM, showing 32.5-fold and 2700-fold selectivity over CDK7 and CDK9, respectively. CDK11-IN-1 hydrochloride binds competitively to the ATP-binding pocket of CDK11 and forms a hydrogen bond with the hinge region residue Val163. It inhibits tumor cell proliferation and exhibits antitumor activity in lung cancer xenograft models. CDK11-IN-1 hydrochloride can be used for studies on the pathophysiology of CDK11-mediated tumors, as well as research on malignant tumors such as lung cancer.
For research use only. We do not sell to patients.
- Formula: C19H21ClFN5
- Molecular Weight:373.85
-
Storage:
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]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
CDK11 4 nM (IC50) |
CDK11-IN-1 (compound 37) (5 nM-100 μM；72 h) hydrochloride , inhibits KHOS and LU99 cells in CellTiter-Glo viability assays, with the GI50 values are 3.7 μM for KHOS cells and 0.40 μM for LU99 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:KHOS, LU99
-
Concentration:5 nM, 15 nM, 45 nM, 135 nM, 405 nM, 1.215 μM, 3.645 μM, 10.935 μM, 32.805 μM, 100 μM (3-fold serial dilution)
-
Incubation Time:72 h
-
Result:Inhibited cell proliferation, with GI50 values of 3.7 μM in KHOS cells and 0.40 μM in LU99 cells.
CDK11-IN-1 (200 mg/kg; p.o.; single administration; 8 h post-administration) hydrochloride exhibits an intratumoral AUC0-last of 47074 ng・h/g and a Cmax of 7311 ng/g, with significantly higher tumor exposure levels than those in plasma in the LU99 lung cancer xenograft BALB/c nude mouse model[1].
CDK11-IN-1 (10, 30, 100 mg/kg; p.o.; twice daily; 14 days) hydrochloride achieves 30% tumor growth inhibition in the LU99 lung cancer xenograft BALB/c nude mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female BALB/c nude mice (7-8 weeks old, unspecified weight) bearing LU99 lung cancer xenografts, anti-tumor efficacy model[1]
-
Dosage:10 mg/kg, 30 mg/kg, 100 mg/kg (once daily for 14 days); 100 mg/kg
-
Administration:1) once daily for 14 days
2) twice daily for 14 days -
Result:Once-daily dosing at 10, 30 or 100 mg/kg did not significantly inhibit tumor growth, while twice-daily dosing at 100 mg/kg produced 30% tumor growth inhibition (TGI); all treatments were well tolerated with no significant body weight loss.
Chemical Information
-
Molecular Weight 373.85
-
Formula C19H21ClFN5
-
SMILES
F[C@H](CNC1)C[C@@H]1NC2=NC(C(C=C3)=CN3C4=CC=CC=C4)=CC=N2.Cl
-
Shipping
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK11-IN-1 hydrochloride Related Classifications
HY-182764A Related Classifications
Powered by Bioz