1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK9-IN-19

CDK9-IN-19 

Cat. No.: HY-150562
Handling Instructions

CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML).

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

CDK9-IN-19 Chemical Structure

CDK9-IN-19 Chemical Structure

CAS No. : 2479306-60-8

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Description

CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML)[1].

IC50 & Target[1]

CDK9/cyclinT1

2 nM (IC50)

In Vitro

CDK9-IN-19 (compound 30i) has antiproliferative activity against a panel of human tumor cell lines with IC50 ranks of 0.08~0.64 μM (for example: Hep G2, HCT-116, SW620, A549, MV-4-11, et al.)[1].
CDK9-IN-19 has low hERG inhibitory activity (IC50=10080 nM) and over 5000-fold selectivity for CDK9[1].
CDK9-IN-19 (0.1-0.8 μM; 24 h) reduces the expression levels of Mcl-1 and c-Myc[1].

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

Western Blot Analysis[1]

Cell Line: MV4-11
Concentration: 0.1, 0.2, 0.4 and 0.8 μM
Incubation Time: 24 h
Result: Clearly reduced the expression levels of Mcl-1 and c-Myc at 0.1 μM, and completely reduced at 0.2-0.8 μM.
In Vivo

CDK9-IN-19 (10, 20 or 40 mg/kg; IV, for 32 days) significantly suppresses the tumour progression in MV4-11 xenograft model[1].
Pharmacokinetic Parameters of CDK9-IN-19 in ICR mice[1].

PO (30 mg/kg) IV (2 mg/kg)
T1/2 (h) NR 0.23
Tmax (h) 0.25 -
C0 (ng/mL) - 3060
Cmax (ng/mL) 665 -
AUC0-t (ng/mL·h) 1200 560
AUC0-∞ (ng/mL·h) NR 561
CL (L/h/kg) - 3.56
VdSS (L/kg) - 0.67
F (%) 14.3 -

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

Animal Model: Female BALB/c nude mice (injected with MV4-11)[1]
Dosage: 10, 20 or 40 mg/kg
Administration: IV, for 32 days
Result: Significantly suppressed the tumour progression and tumour growth inhibition (TGI) values up to 100% from days 14-32 at 40 mg/kg.
Molecular Weight

508.47

Formula

C26H22F2N4O5

CAS No.
SMILES

O=C1C(C(C)=O)=C(N2CCOCC2)C3=C(O1)C=C(NC4=NC=C(F)C(C5=CC=C(F)C=C5OC)=N4)C=C3

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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.

References
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CDK9-IN-19
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HY-150562
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