2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis DNA/RNA Synthesis Bcl-2 Family IAP
  4. ZLMT-72

ZLMT-72 is an orally active dual CDK2 and CDK9 inhibitor with IC50s of 0.741 nM and 1.03 nM, respectively. ZLMT-72 shows good selectivity in kinase profiling andcholinesterase inhibition activity. ZLMT-72 has strong antiproliferative effects in the colorectal cancer (CRC) cell line HCT116 (GI50 < 0.1 nM). ZLMT-72 induces apoptosis by inhibiting thephosphorylation of retinoblastoma and RNA polymerase II, resulting in downregulation of antiapoptotic proteins (Mcl-1 and XIAP). ZLMT-72 can be used for the study of colorectal cancer (CRC).

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ZLMT-72

ZLMT-72 Chemical Structure

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ZLMT-72 Related Antibodies

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cIAP cIAP-1 cIAP-2 XIAP

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Description

ZLMT-72 is an orally active dual CDK2 and CDK9 inhibitor with IC50s of 0.741 nM and 1.03 nM, respectively. ZLMT-72 shows good selectivity in kinase profiling andcholinesterase inhibition activity. ZLMT-72 has strong antiproliferative effects in the colorectal cancer (CRC) cell line HCT116 (GI50 < 0.1 nM). ZLMT-72 induces apoptosis by inhibiting thephosphorylation of retinoblastoma and RNA polymerase II, resulting in downregulation of antiapoptotic proteins (Mcl-1 and XIAP). ZLMT-72 can be used for the study of colorectal cancer (CRC)[1].

IC50 & Target[1]

RNA Polymerase

 

CDK2/CycA2

0.741 (IC50)

CDK9/CycT1

1.03 (IC50)

Mcl-1

 

XIAP

 

In Vitro

ZLMT-72 (1-10 nM; 10 days) completely suppresses colony formation in HCT116 cells[1].
ZLMT-72 (1-10 nM; 72 hours) demonstrates potent antiproliferative effects in HCT116 cells[1].
ZLMT-72 (1-10 nM; 48 hours) induces significant apoptosis in HCT116 cells[1].
ZLMT-72 (1-10 nM; 24 hours) significantly inhibits HCT116 cell migration[1].
ZLMT-72 (1-10 nM; 48 hours) inhibits CDK2/9 and reduces antiapoptotic protein expression in HCT116 cells[1].

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

ZLMT-72 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCT116 cells
Concentration: 1 nM, 3.3 nM, 10 nM
Incubation Time: 72 hours
Result: Exhibited potent antiproliferative effects, with GI50 values < 0.1 nM. The compound significantly inhibited cell proliferation.

Cell Proliferation Assay[1]

Cell Line: HCT116 cells
Concentration: 1 nM, 3.3 nM, 10 nM
Incubation Time: 10 days
Result: Completely suppressed colony formation in HCT116 cells at 10 nM, demonstrating strong antiproliferative activity. 

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 10 nM, 3.3 nM, 1 nM
Incubation Time: 48 hours
Result: Induced apoptosis in 30.19% of HCT116 cells at 10 nM, with 23.3% early-stage and 6.89% late-stage apoptosis. 

Cell Migration Assay [1]

Cell Line: HCT116 cells
Concentration: 1 nM, 3.3 nM, 10 nM
Incubation Time: 24 hours
Result: Significantly inhibited HCT116 cell migration at 10 nM and 3.3 nM, with a reduced migration rate.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 10 nM, 3.3 nM, 1 nM
Incubation Time: 48 hours
Result: Significantly downregulated the levels of phosphorylated Rb (p-Rb) and inhibited the phosphorylation of RNA polymerase II at the Ser2 site, indicating CDK2/9 inhibition.
Also reduced the expression of antiapoptotic proteins (MCL-1 and XIAP).
Parmacokinetics
Species Dose Route Note T1/2 Cmax AUC0-t Tmax CL F
Rat[1] 4 mg/kg i.v. 文献审核 3.47 h 930.73 ng/mL 2682.79 ng·h/mL 0.25 h 1.49 kg·h/L /
Rat[1] 40 mg/kg p.o. 文献审核 6.40 h 266.00 ng/mL 2476.49 ng·h/mL 1.67 h / 9.23 %
In Vivo

ZLMT-72 (1.1-10 mg/kg, oral, twice daily for 14 days) exhibits robust antitumor efficacy in HCT116 xenograft models with favorable safety in subcutaneous and orthotopic tumor models[1].

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

Animal Model: Balb/c nude mice bearing HCT116 cells (subcutaneous and orthotopic xenograft tumor models)[1]
Dosage: 10 mg/kg, 3.3 mg/kg, 1.1 mg/kg
Administration: Oral, oral, twice daily, for 14 days
Result: Tumor growth was significantly inhibited in both subcutaneous and orthotopic models.
At 10 mg/kg, tumor growth inhibition (TGI) was 50.6% in subcutaneous models and 84.3% in orthotopic models.
Revealed a significantred reduction in Ki67-positive and CDK20-positive cells.
Tumor weight and volume were significantly reduced, and no significant toxicity was observed.
Molecular Weight

485.60

Formula

C29H32FN5O
SMILES

O=C([C@@H]1[C@@H](F)C1)NC2=CC(C3=CC=C(N=C(CCCCC4)C4=C5N6C[C@@H](CNC7)[C@@H]7C6)C5=C3)=CC=N2
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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ZLMT-72 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:

ZLMT-72ZLMT72ZLMT 72CDKApoptosisDNA/RNA SynthesisBcl-2 FamilyIAPCyclin dependent kinasecolorectal cancertherapeutic potentialantitumor efficacyCRCHCT116dual CDK2/9 inhibitorCDK2CDK9Inhibitorinhibitorinhibit

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