2. Cell Cycle/DNA Damage Apoptosis Epigenetics
  3. CDK Apoptosis PARP Caspase Bcl-2 Family
  4. 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.

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

CDK9-IN-47

CDK9-IN-47 Chemical Structure

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CDK9-IN-47 Related Antibodies

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Description

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[1].

In Vitro

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.

CDK9-IN-47 Related Antibodies

Cell Proliferation Assay[1]

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)
Concentration: /
Incubation Time: 72 h
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.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 and 4T1 TNBC cells
Concentration: 0.3 μM, 1.0 μM, 3.0 μM
Incubation Time: 8 h
Result: Increased cleaved PARP and Caspase 3 levels.
Reduced levels of the antiapoptotic proteins XIAP and Bcl2.
Parmacokinetics
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 % / / /
In Vivo

CDK9-IN-47 (10-20 mg/kg; intravenous injection; once daily; for 7 consecutive days) exerts potent tumor growth inhibitory effects in the BALB/c mouse 4T1 syngeneic triple-negative breast cancer model[1].
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.

Animal Model: BALB/c (syngeneic triple-negative breast cancer model via 4T1 cell implantation)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.v.; daily; 7 days
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.
Animal Model: Immunocompromised (xenograft triple-negative breast cancer model via MDA-MB-231 human cell implantation)[1]
Dosage: 30 mg/kg; 60 mg/kg
Administration: i.g.; intermittent schedule; 15 days
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.
Molecular Weight

450.51

Formula

C25H27FN4O3
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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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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CDK9-IN-47 Related Classifications

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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.

Keywords:

CDK9-IN-47CDKApoptosisPARPCaspaseBcl-2 FamilyCyclin dependent kinasepoly ADP ribose polymeraseBcl2CDK9XIAPTwist1Snail1caspase 3MMP9triple-negative breast cancerInhibitorinhibitorinhibit

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