CASIN 是一个选择性的GTPase Cdc42抑制剂，其IC50值是 2 uM。CASIN 可用于癌症的研究。
| 生物活性 | CASIN is a selectiveGTPase Cdc42inhibitor with anIC50of 2 uM. CASIN can be used for the research ofcancer[1][2]. |
| IC50& Target | IC50: 2 μM (GTPase Cdc42)[1] |
体外研究
(In Vitro) | CASIN (0-10 μM; 3 d) inhibits the growth of AMO-1, ARH-77, IM-9 , JJN-3, L-363, MOLP-8 and RPMI-8226/S cells[1].CASIN (0-10 μM; 16 h) inhibits melphalan induced FANCD2 mono-ubiquitination in LR5 cells but shows no effect to S cells[1].CASIN (5 μM; 2 d) increases cell apoptosis of bortezomib-resistant MM patient cells[1].
Cell Viability Assay[3] | Cell Line: | AMO-1, ARH-77, IM-9 , JJN-3, L-363, MOLP-8 and RPMI-8226/S cells | | Concentration: | 0-10 μM | | Incubation Time: | 3 days | | Result: | Inhibited MM cell lines including AMO-1, ARH-77, IM-9 , JJN-3, L-363, MOLP-8 and RPMI-8226/S cells with GI50s vof 3.23, 4.31, 4.87, 2.56, 4.64, 4.67 and 3.97 μM, respectively. |
Western Blot Analysis[3] | Cell Line: | MM (S) and melphalan-resistant (LR5) MM cells | | Concentration: | 5 μM | | Incubation Time: | 16 hours | | Result: | Abolished melphalan induced FANCD2 mono-ubiquitination and DNA damage in LR5, sensitized LR5 to melphalan-induced cell death by blocking FANCD2-mediated DNA damage repair. |
Apoptosis Analysis[3] | Cell Line: | Bortezomib-resistant MM patients cells | | Concentration: | 5 μM | | Incubation Time: | 2 days | | Result: | 2-fold increased cell apoptosis in the cell derived from bortezomib-resistant MM patients. |
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体内研究
(In Vivo) | CASIN (20 mg/kg; i.p. 2 times a day) prolongs lifetime of mice with busulfan injection[1].
| Animal Model: | NSG mice with busulfan injection[3] | | Dosage: | 20 mg/kg | | Administration: | Intraperitoneal injection; 20 mg/kg 2 times a day | | Result: | Significantly prolonged the lifespan of xenografts mice better than bortezomib, and showed a leading position when combined with bortezomib. |
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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 : ≥ 31 mg/mL(101.17 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.2637 mL | 16.3185 mL | 32.6371 mL | | 5 mM | 0.6527 mL | 3.2637 mL | 6.5274 mL | | 10 mM | 0.3264 mL | 1.6319 mL | 3.2637 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 (6.79 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.79 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 (6.79 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.79 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 (6.79 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.79 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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