S55746 hydrochloride (BCL201 hydrochloride) 是一种有效、可口服、选择性的BCL-2抑制剂，其Ki值和Kd值分别为 1.3 nM 和 3.9 nM。S55746 hydrochloride (BCL201 hydrochloride) 具有抗肿瘤活性且毒性低。
| 生物活性 | S55746 hydrochloride (BCL201 hydrochloride) is a potent, orally active and selectiveBCL-2inhibitor, with aKiof 1.3 nM and aKdof 3.9 nM. S55746 hydrochloride (BCL201 hydrochloride) has antitumor activity with low toxicity[1]. |
| IC50& Target[1] | Bcl-2 1.3 nM (Ki) | Bcl-xL 520 nM (Ki) | Bcl-2 3.9 nM (Kd) | Bcl-xL 186 nM (Kd) |
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体外研究
(In Vitro) | S55746 (0-1 μM) potently and selectively induces cell death[1].
S55746 selectively induces apoptosis through BCL-2 inhibition in a BAX/BAK-dependent manner[1].
Western Blot Analysis[1] | Cell Line: | H146 and RS4;11 cell lines. | | Concentration: | 0, 0.1, 0.3 and 1 μM. | | Incubation Time: | 72 hours. | | Result: | Potently induced RS4;11 cell killing after 72 h of treatment with an IC50of 71.6 nM. |
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体内研究
(In Vivo) | S55746 is a highly efficacious and well-tolerated (even at doses up to 300 mg/kg) orally active BCL-2 inhibitor[1].
S55746 (20-100 mg/kg, p.o.) inhibits xenograft growth in RS4;11 and Toledo models time- and dose-dependently[1].
| Animal Model: | Female SCID/beige mice implanted subcutaneously with 3×106Toledo or RS4;11[1]. | | Dosage: | 20, 50, 100 mg/kg. | | Administration: | Oral gavage daily for 7 consecutive days. | | Result: | Induced significant anti-tumor activity time- and dose-dependently. |
| Animal Model: | SCID/beige female mice with RS4;11 tumor xenografts[1]. | | Dosage: | 25 and 100 mg/kg. | | Administration: | Single oral gavage treatment. | | Result: | Did not induce platelet loss in vivo at 25 and 100 mg/kg. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| 溶解性数据 | In Vitro: DMSO : 200 mg/mL(267.64 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.3382 mL | 6.6909 mL | 13.3819 mL | | 5 mM | 0.2676 mL | 1.3382 mL | 2.6764 mL | | 10 mM | 0.1338 mL | 0.6691 mL | 1.3382 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 (stored under nitrogen)。-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 90% (20%SBE-β-CDin saline) Solubility: ≥ 5 mg/mL (6.69 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (6.69 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 50.0 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。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 5 mg/mL (6.69 mM); Clear solution
此方案可获得 ≥ 5 mg/mL (6.69 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 50.0 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。 |
