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

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CDK11-IN-1 hydrochloride

CDK11-IN-1 hydrochloride Chemical Structure

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Description

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[1].

IC50 & Target

CDK11

4 nM (IC50)

In Vitro

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 Viability Assay[1]

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.
In Vivo

CDK11-IN-1 (compound 37) (50-200 mg/kg; p.o.; once daily; 14 days) hydrochloride is well tolerated in female BALB/c nude mouse models, with no obvious toxicity or significant body weight loss[1].
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.
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
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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.

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Product Name:
CDK11-IN-1 hydrochloride
Cat. No.:
HY-182764A
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