2. Cell Cycle/DNA Damage Neuronal Signaling Apoptosis
  3. CDK Cholinesterase (ChE) Apoptosis
  4. 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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ZLMT-12 Chemical Structure

ZLMT-12 Chemical Structure

CAS No. : 2841473-39-8

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ZLMT-12 Related Antibodies

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Description

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[1].

IC50 & Target[1]

CDK9

0.002 μM (IC50)

CDK2

0.011 μM (IC50)

BChE

2.768 μM (IC50)

AChE

19.023 μM (IC50)

In Vitro

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.

ZLMT-12 Related Antibodies

Cell Viability Assay[1]

Cell Line: HCT116, SW480, A549, and MCF-7 cells
Concentration: 500 nM
Incubation Time: 72 hours
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.

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 10 and 20 nM
Incubation Time: 48 hours
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.

Cell Cycle Analysis[1]

Cell Line: HCT116 cells
Concentration: 10 and 20 nM
Incubation Time: 48 hours
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.
In Vivo

ZLMT-12 (compound 35; 10 mg/kg; p.o.; daily, for 21 d) has antitumor efficacy and inhibits tumor growth, without causing liver harm in the HCT116 xenograft model[1].

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

Animal Model: Male BALB/cA-nu mice with HCT116 xenografts (18-25 g, 6-8 weeks of age)[1]
Dosage: 10 mg/kg
Administration: Oral administration; daily, for 21 days
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.
Animal Model: Male Sprague-Dawley rats (240±20 g)[1]
Dosage: 2 mg/kg (i.v.) and 20 mg/kg (p.o.) (Pharmacokinetic Analysis)
Administration: Intravenous injection and oral administration; once
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
Molecular Weight

479.02

Formula

C26H31ClN6O
CAS No.
SMILES

O=C(C1CC1)NC2=NC=CC(C3=CC=C4N=C5C(CCCCC5)=C(N6C[C@@H](N)CC6)C4=C3)=N2.[H]Cl
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-12 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-122841473-39-8ZLMT12ZLMT 12CDKCholinesterase (ChE)ApoptosisCyclin dependent kinasetacrine derivativeanticancerlow toxicityHCT116 cellscell cycleInhibitorinhibitorinhibit

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