(E/Z)-Zotiraciclib ((E/Z)-TG02) 是一种强效的CDK2,JAK2和FLT3的抑制剂,IC50值分别为 13,73 和 56 nM。(E/Z)-Zotiraciclib 有效的抑制癌细胞的增殖,可用于癌症的研究。
生物活性 | (E/Z)-Zotiraciclib ((E/Z)-TG02) is a potent inhibitor ofCDK2,JAK2andFLT3withIC50s of 13, 73 and 56 nM, respectively. (E/Z)-Zotiraciclib effectively inhibits the proliferation ofcancercells, it can be used for the research ofcancer[1][2]. |
IC50& Target[1] | CDK2 13 nM (IC50) | JAK2 73 nM (IC50) | FLT3 56 nM (IC50) |
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体外研究 (In Vitro) | (E/Z)-Zotiraciclib (0-10 μM) shows potent inhibition to CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM, respectively[1].(E/Z)-Zotiraciclib (0-10 μM; 48 h) inhibits proliferation of cancer cells[1].(E/Z)-Zotiraciclib (8-1000 nM; 24 h) potently inhibits the CDK2 biomarker pRb in HCT-116 cells and potently againsts pRb in MV4-11 cells with an IC50value of 0.13 μM[1].
Cell Proliferation Assay[1] Cell Line: | HL-60, HCT-116, RAMOS, COLO205 and DU145 cell lines | Concentration: | 0-10 μM | Incubation Time: | 48 h | Result: | Inhibited proliferation of HL-60, HCT-116, RAMOS, COLO205 and DU145 cells with IC50s of 0.059, 0.079, 0.033, 0.072 and 0.14 μM, respectively. |
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体内研究 (In Vivo) | (E/Z)-Zotiraciclib (50 and 75 mg/kg; p.o. once daily for 3 weeks) inhibits tumor growth[1].(E/Z)-Zotiraciclib (15 and 75 mg/kg; p.o. once daily 2 days on and 5 days off; i.p. once daily 5 days on 5 days off) inhibits tumor growth in two manners[1].
Animal Model: | Male BALB/c mice with HCT-116 colon cancer cells xenografts[1] | Dosage: | 50 and 75 mg/kg | Administration: | Oral gavage; 50 and 75 mg/kg once daily for 3 weeks | Result: | Significantly inhibited the growth of tumors with a mean TGI of 82%. |
Animal Model: | Male BALB/c mice with lymphoma Ramos cells xenografts[1] | Dosage: | 15 and 75 mg/kg | Administration: | Oral gavage and intraperitoneal injection ; 75 mg/kg once daily 2 days on and 5 days off (p.o.) and 15 mg/kg once daily 5 days on 5 days off (i.p.) | Result: | Significantly inhibited the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 26.5 mg/mL(71.15 mM;Need ultrasonic and warming) 配制储备液 1 mM | 2.6849 mL | 13.4243 mL | 26.8485 mL | 5 mM | 0.5370 mL | 2.6849 mL | 5.3697 mL | 10 mM | 0.2685 mL | 1.3424 mL | 2.6849 mL |
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此方案可获得 ≥ 2.08 mg/mL (5.58 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.58 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.58 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.58 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.58 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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