2479306-60-8
2479306-60-8 structure
- Name: CDK9-IN-19
- Chemical Name: CDK9-IN-19
- CAS Number: 2479306-60-8
- Molecular Formula: C26H22F2N4O5
- Molecular Weight: 508.47
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2022-08-17 19:30:56
- Modify Date: 2024-01-19 22:38:55
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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].
| Name | CDK9-IN-19 |
|---|
| 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]. |
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| Related Catalog | |
| Target |
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]. 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 - 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. |
| References |
| Molecular Formula | C26H22F2N4O5 |
|---|---|
| Molecular Weight | 508.47 |