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ZLMT-12
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ZLMT-12图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
ZLMT-12 (compound 35) 是他克宁衍生物,是一种有效的CDK2/9抑制剂,抑制 CDK9 和 CDK2 的IC50值分别为 0.002 和 0.011 μM。ZLMT-12 对AChE(IC50=19.023 μM) 和BuChE(IC50=2.768 μM) 有弱抑制作用。ZLMT-12 具有低毒和抗增殖活性。ZLMT-12 诱导细胞凋亡 (apoptosis),阻滞细胞周期在 S 期和 G2/M 期。
生物活性

ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally activeCDK2/9inhibitor withIC50values of 0.002 and 0.011 μM forCDK9andCDK2, respectively. ZLMT-12 has a weak inhibitory effect onAChE(IC50=19.023 μM) andBChE(IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 inducesapoptosisand 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)

体外研究
(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].

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 GI50values 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.
体内研究
(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].

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
Parameter2 mg/kg (i.v.)20 mg/kg (p.o.)
T1/2(h)0.4611.77
Tmax(h)0.083/td>1.00
Cmax(ng/mL)20667.8
AUCo-t(h*ng/mL)110302
AUCo-∞(h*ng/mL)115316
CL (L/h/kg)18.7
Vss(L/Kg)12.6
F (%)27.47
分子量

479.02

Formula

C26H31ClN6O

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.