产品
编 号：F753126
分子式：C26H22F2N4O5
分子量：508.47
分子式：C26H22F2N4O5
分子量：508.47
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CAS No: 2479306-60-8
产品详情
生物活性：
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).
体内研究：
CDK9-IN-19 (10, 20 or 40 mg/kg; IV, for 32 days) significantly suppresses the tumour progression in MV4-11 xenograft model.Pharmacokinetic Parameters of CDK9-IN-19 in ICR mice.PO (30 mg/kg) IV (2 mg/kg)
T1/2 (h)NR0.23
Tmax (h)0.25-
C0 (ng/mL)-3060
Cmax (ng/mL)665-
AUC0-t (ng/mL·h)1200560
AUC0-∞ (ng/mL·h)NR561
CL (L/h/kg)-3.56
VdSS (L/kg)-0.67
F (%)14.3-
Animal Model:Female BALB/c nude mice (injected with MV4-11)
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.
体外研究：
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.).CDK9-IN-19 has low hERG inhibitory activity (IC50=10080 nM) and over 5000-fold selectivity for CDK9.CDK9-IN-19 (0.1-0.8 μM; 24 h) reduces the expression levels of Mcl-1 and c-Myc.
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).
体内研究：
CDK9-IN-19 (10, 20 or 40 mg/kg; IV, for 32 days) significantly suppresses the tumour progression in MV4-11 xenograft model.Pharmacokinetic Parameters of CDK9-IN-19 in ICR mice.PO (30 mg/kg) IV (2 mg/kg)
T1/2 (h)NR0.23
Tmax (h)0.25-
C0 (ng/mL)-3060
Cmax (ng/mL)665-
AUC0-t (ng/mL·h)1200560
AUC0-∞ (ng/mL·h)NR561
CL (L/h/kg)-3.56
VdSS (L/kg)-0.67
F (%)14.3-
Animal Model:Female BALB/c nude mice (injected with MV4-11)
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.
体外研究：
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.).CDK9-IN-19 has low hERG inhibitory activity (IC50=10080 nM) and over 5000-fold selectivity for CDK9.CDK9-IN-19 (0.1-0.8 μM; 24 h) reduces the expression levels of Mcl-1 and c-Myc.
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