CDK9-IN-47
CDK9-IN-47 is an orally active and selective CDK9 inhibitor with an IC50 of 1.4 nM. CDK9-IN-47 inhibits tumor cell proliferation, migration and invasion, and induces apoptosis. CDK9-IN-47 can be used for the research of triple-negative breast cancer.
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- 화학식: C25H27FN4O3
- 분자량:450.51
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보관:
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]
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Biological Activity
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Chemical Information
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Biological Activity
CDK9-IN-47 (compound HS34) (72 h) potently inhibits the proliferation of various breast cancer cell lines, and exhibits no cytotoxicity against normal cardiomyocytes and hepatocytes after 72 h of treatment (GI50 > 10 μM)[1].
CDK9-IN-47 (0.1-1.0 μM; 24 h) ablates the clonogenic potential of MDA-MB-231 and 4T1 triple-negative breast cancer (TNBC) cells in a dose-dependent manner[1].
CDK9-IN-47 (0.1-3.0 μM; 8-24 h) induces dose-dependent apoptosis and inhibits cell migration and invasion abilities in MDA-MB-231 and 4T1 triple-negative breast cancer (TNBC) cells[1].
CDK9-IN-47 (0.1-1.0 μM; 8 h) selectively inhibits CDK9-driven transcription processes in MDA-MB-231 and 4T1 triple-negative breast cancer (TNBC) cells, which is characterized by decreased levels of p-Ser2 CTD, downregulated expression of c-Myc and Mcl-1, and reduced cyclin T1 levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Multiple breast cancer and normal cell lines (MDA-MB-231, MDA-MB-435, BT-549, 4T1, MCF-7, MCF-7-Pa, H9c2, THLE-2)
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Concentration:/
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Incubation Time:72 h
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Result:Exhibited a half-maximal growth inhibition (GI50) of 0.22 ± 0.09 μM in MDA-MB-231 TNBC cells.
Exhibited a GI50 of 0.68 ± 0.14 μM in MDA-MB-435 cells.
Exhibited a GI50 of 0.64 ± 0.09 μM in BT-549 TNBC cells.
Exhibited a GI50 of 0.53 ± 0.12 μM in 4T1 TNBC cells.
Exhibited a GI50 of 0.47 ± 0.17 μM in MCF-7 ER-positive breast cancer cells.
Exhibited a GI50 of 0.60 ± 0.21 μM in palbociclib-resistant MCF-7-Pa cells.
Showed minimal cytotoxicity in normal cell lines, with a GI50 > 10 μM in H9c2 cardiomyocytes and THLE-2 hepatocytes.
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Cell Line:MDA-MB-231 and 4T1 TNBC cells
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Concentration:0.3 μM, 1.0 μM, 3.0 μM
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Incubation Time:8 h
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Result:Increased cleaved PARP and Caspase 3 levels.
Reduced levels of the antiapoptotic proteins XIAP and Bcl2.
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ | Bioavailability | C0 | CL | Vd |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 4 mg/kg | i.v. | / | 0.083 h | 2.53 h | 1702.7 ng·h/mL | 1767.3 ng·h/mL | 1.63 h | 1.88 h | / | 4723.9 ng/mL | 2.14 L/h/kg | 8.4 L/kg |
| Mice[1] | 20 mg/kg | p.o. | 2176.0 ng/mL | 1.0 h | 5.44 h | 3708.3 ng·h/mL | 3763.0 ng·h/mL | 3.36 h | 3.87 h | 43.6 % | / | / | / |
CDK9-IN-47 (30-60 mg/kg; i.g.; intermittent dosing; 15 days) exerts significant tumor growth inhibition in the MDA-MB-231 human triple-negative breast cancer xenograft model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (syngeneic triple-negative breast cancer model via 4T1 cell implantation)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.v.; daily; 7 days
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Result:Achieved significant tumor growth inhibition, with reduced final tumor weights compared to vehicle control.
Achieved a tumor growth inhibition (TGI) of 56.1%, with a greater reduction in final tumor weights compared to the 10 mg/kg dose and the reference paclitaxel group.
Reduced expression of proliferation marker Ki-67, and CDK9 downstream proteins Mcl-1 and c-Myc.
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Animal Model:Immunocompromised (xenograft triple-negative breast cancer model via MDA-MB-231 human cell implantation)[1]
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Dosage:30 mg/kg; 60 mg/kg
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Administration:i.g.; intermittent schedule; 15 days
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Result:Achieved significant tumor growth inhibition with reduced final tumor weights compared to vehicle control.
Achieved a tumor growth inhibition (TGI) of 71.3%, with a greater reduction in final tumor weights compared to the 30 mg/kg dose.
Chemical Information
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분자량 450.51
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화학식 C25H27FN4O3
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SMILES
O=C([C@H]1CNCCC1)NC2=NC=C(F)C(C3=CC(C(N4[C@@H](C)CCC4)=CC5=O)=C(O5)C=C3)=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK9-IN-47 Related Classifications
HY-182069 Related Classifications
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