ZLMT-12
ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9 inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase.
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- CAS No.: 2841473-39-8
- Formule: C26H31ClN6O
- Masse moléculaire:479.02
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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CDK9 0.002 μM (IC50) |
CDK2 0.011 μM (IC50) |
BChE 2.768 μM (IC50) |
AChE 19.023 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
0.009 μM
Compound: 35; ZLMT-12
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Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay
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[PMID: 36054949] |
| HCT-116 | GI50 |
0.006 μM
Compound: 35; ZLMT-12
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Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition after 72 hrs by MTT assay
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[PMID: 36054949] |
| MCF7 | GI50 |
0.006 μM
Compound: 35; ZLMT-12
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Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 72 hrs by MTT assay
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[PMID: 36054949] |
| SW480 | GI50 |
0.013 μM
Compound: 35; ZLMT-12
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Antiproliferative activity against human SW480 cells assessed as cell growth inhibition after 72 hrs by MTT assay
Antiproliferative activity against human SW480 cells assessed as cell growth inhibition after 72 hrs by MTT assay
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[PMID: 36054949] |
ZLMT-12 (compound 35; 500 nM; 72 h) has antiproliferative activity in cancer cells[1].
ZLMT-12 (500 nM; 72 h) induces apoptosis and arrests the cell cycle in the S phase and G2/M phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116, SW480, A549, and MCF-7 cells
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Concentration:500 nM
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Incubation Time:72 hours
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Result:Inhibited cell proliferative with GI50 values of 0.029, 0.328, 0.051, and 0.109 μM for HCT116, SW480, A549, and MCF-7 cells, respectively.
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Cell Line:HCT116 cells
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Concentration:10 and 20 nM
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Incubation Time:48 hours
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Result:Increased apoptotic cells rate from 9.22% in the control to 23.77% at 10 nM and increased apoptotic cells rate to 46.2% at 20 nM.
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Cell Line:HCT116 cells
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Concentration:10 and 20 nM
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Incubation Time:48 hours
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Result:Increased the percentage of the S phase from 31.43% to 42.75% (10 nM) and 49.38% (20 nM) respectively, and the percentage of the G2/M phase from 6.39% to 10.60% (10 nM) and 13.11% (20 nM), respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/cA-nu mice with HCT116 xenografts (18-25 g, 6-8 weeks of age)[1]
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Dosage:10 mg/kg
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Administration:Oral administration; daily, for 21 days
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Result:Inhibited tumor growth with GI (tumor volume growth inhibition)=47.66% and TGI (tumor weight growth inhibition)=62.39%.
Exhibited no significant changes in behavior or body weight in mice.
Had no obvious liver injury.
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Animal Model:Male Sprague-Dawley rats (240±20 g)[1]
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Dosage:2 mg/kg (i.v.) and 20 mg/kg (p.o.) (Pharmacokinetic Analysis)
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Administration:Intravenous injection and oral administration; once
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Result:
1.19 Parameter 2 mg/kg (i.v.) 20 mg/kg (p.o.) T1/2 (h) 0.461 1.77 Tmax (h) 0.083/td> 1.00 Cmax (ng/mL) 206 67.8 AUCo-t (h*ng/mL) 110 302 AUCo-∞ (h*ng/mL) 115 316 CL (L/h/kg) 18.7 Vss(L/Kg) 12.6 F (%) 27.47
Chemical Information
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CAS No. 2841473-39-8
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Masse moléculaire 479.02
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Formule C26H31ClN6O
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SMILES
O=C(C1CC1)NC2=NC=CC(C3=CC=C4N=C5C(CCCCC5)=C(N6C[C@@H](N)CC6)C4=C3)=N2.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ZLMT-12 Related Classifications
HY-151436 Related Classifications
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