2. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. CDK Epigenetic Reader Domain Reactive Oxygen Species (ROS)
  4. KWZL-7f15

KWZL-7f15 is a dual CDK6/BRD4 inhibitor with an IC50 of 31.81 nM against human CDK6. KWZL-7f15 inhibits the CDK6-RB axis and BRD4-Myc axis, and also acts as a pan-BET inhibitor. KWZL-7f15 exhibits antiproliferative activity against triple-negative breast cancer cells. KWZL-7f15 shows antitumor activity in xenograft mouse models. KWZL-7f15 can be used in studies related to triple-negative breast cancer.

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

KWZL-7f15

KWZL-7f15 Chemical Structure

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KWZL-7f15 Related Antibodies

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Description

KWZL-7f15 is a dual CDK6/BRD4 inhibitor with an IC50 of 31.81 nM against human CDK6. KWZL-7f15 inhibits the CDK6-RB axis and BRD4-Myc axis, and also acts as a pan-BET inhibitor. KWZL-7f15 exhibits antiproliferative activity against triple-negative breast cancer cells. KWZL-7f15 shows antitumor activity in xenograft mouse models. KWZL-7f15 can be used in studies related to triple-negative breast cancer[1].

IC50 & Target[1]

CDK6

31.81 nM (IC50)

BRD4

56.41 nM (IC50)

BET

 

In Vitro

KWZL-7f15 (compound 7f15) exhibited potent cytotoxicity against triple-negative breast cancer (TNBC) cell lines MDA-MB-231 (IC50 = 0.35 μM), BT-549 (IC50 = 2.77 μM), and showed high selectivity with IC50 > 30 μM against normal mammary epithelial MCF-10A cells[1].
KWZL-7f15 (500 nM for CDK4/CycD1 and CDK6/CycD3) acted as a pan-BET and preferential CDK4/CDK6 inhibitor, with IC50 values of 31.81 nM (CDK6), 56.41 nM (BRD4), 37.30 nM (BRD2 BD1+BD2), 34.02 nM (BRD3 BD1+BD2), 31.79 nM (BRD4 BD2), and showed 57.73% inhibition of CDK4/CycD1 and 80.53% inhibition of CDK6/CycD3 at 500 nM[1].
KWZL-7f15 (0.25-1 μM; 12-48 h) modulated protein expression in MDA-MB-231 cells, causing dose- and time-dependent downregulation of BRD4, c-Myc, p-Rb, and Bcl2, and upregulation of Bax and cleaved-caspase 3[1].
KWZL-7f15 (0.25-1 μM; 48 h) induced G0/G1 phase arrest in MDA-MB-231 cells in a dose-dependent manner[1].
KWZL-7f15 induced oxidative stress and DNA damage in MDA-MB-231 cells, increasing intracellular ROS levels, elevating γ-H2AX, suppressing RAD51, and inducing DNA strand breaks[1].
KWZL-7f15 (0.25 μM, 48 h) inhibited cell migration of MDA-MB-231 cells in a wound-healing assay[1].
KWZL-7f15 (0.25 μM, 48 h) inhibited colony formation of MDA-MB-231 cells[1].

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

KWZL-7f15 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231
Concentration: 0.25, 0.5, 1 μM
Incubation Time: 48 h
Result: Induced G0/G1 phase arrest in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231
Concentration: 1 μM
Incubation Time: 48 h
Result: Promoted caspase-dependent apoptosis.
Reversed cytotoxicity when co-treated with pan-caspase inhibitor Z-VAD-FMK.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231
Concentration: 0.25 μM
Incubation Time: 48 h
Result: Inhibited colony formation of MDA-MB-231 cells.

Cell Migration Assay [1]

Cell Line: MDA-MB-231
Concentration: 0.25 μM
Incubation Time: 48 h
Result: Inhibited cell migration of MDA-MB-231 cells in a wound-healing assay.

Western Blot Analysis[1]

Cell Line: MDA-MB-231
Concentration: 0.25, 0.5, 1 μM
0.5 μM
Incubation Time: 48 h
12, 24, 48 h
Result: Reduced the protein expression of CDK6, BRD4, p-Rb and c-Myc in MDA-MB-231 cells in a time-dependent manner, and has no significant effect on CDK4 protein level.
Downregulated CDK6, BRD4, p-Rb and c-Myc protein expression in MDA-MB-231 cells with concentration dependence, and does not alter CDK4 expression obviously.
Parmacokinetics
Species Dose Route Cmax Tmax AUC0-t T1/2 Vd CL MRT0-∞
Rat[1] 5 mg/kg i.p. 160.60 ng/mL 6.00 h 2114.18 ng·h/mL 13.06 h 420.19 L/kg 22.84 L/h/kg 20.73 h
In Vivo

KWZL-7f15 (compound 7f15) (20-40 mg/kg; i.p.; daily; 14 days) exhibits dose-dependent in vivo antitumor activity in a BALB/c nude mouse MDA-MB-231 xenograft model[1].

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

Animal Model: BALB/c nude (female, 4-5 weeks old, 18-20 g, subcutaneous xenograft model via MDA-MB-231 tumor cell implantation)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: i.p.; daily; 14 days
Result: Produced a tumor growth inhibition (TGI) rate of 61.64% at 20 mg/kg.
Produced a TGI rate of 84.69% at 40 mg/kg.
Caused no significant body weight loss.
Showed no treatment-related lesions in heart, liver, spleen, lung, and kidney via histopathological analysis.
Reduced positive expression of c-Myc and p-Rb significantly in tumor tissues compared to the control group via immunohistochemical analysis.
Molecular Weight

490.58

Formula

C26H31FN8O
SMILES

CN(C(C=C1)=C(N(C(C)C)[C@@H]2C)C=C1C3=C(F)C=NC(NC4=CC=C(N5CCNCC5)C=N4)=N3)C2=O
Shipping

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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KWZL-7f15 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:

KWZL-7f15CDKEpigenetic Reader DomainReactive Oxygen Species (ROS)Cyclin dependent kinaseBRD4triple-negative breast cancerRB axisBT-549CDK6Myc axisCDK4MDA-MB-231BETMCF-10AInhibitorinhibitorinhibit

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