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

ZLMT-12 Chemical Structure

CAS No. : 2841473-39-8

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ZLMT-12 Related Antibodies

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AChE BChE

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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)

Cellular Effect
Cell Line Type Value Description References
A549 GI50
0.009 μM
Compound: 35; ZLMT-12
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
[PMID: 36054949]
HCT-116 GI50
0.006 μM
Compound: 35; ZLMT-12
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
[PMID: 36054949]
MCF7 GI50
0.006 μM
Compound: 35; ZLMT-12
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
[PMID: 36054949]
SW480 GI50
0.013 μM
Compound: 35; ZLMT-12
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
[PMID: 36054949]
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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