(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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% 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 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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