S55746 hydrochloride(Synonyms: BCL201 hydrochloride)

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S55746 hydrochloride (Synonyms: BCL201 hydrochloride) 纯度: 98.69%

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。

S55746 hydrochloride(Synonyms: BCL201 hydrochloride)

S55746 hydrochloride Chemical Structure

CAS No. : 1448525-91-4

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生物活性

S55746 hydrochloride (BCL201 hydrochloride) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 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)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC50 of 71.6 nM.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female SCID/beige mice implanted subcutaneously with 3×106 Toledo 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.

Clinical Trial

分子量

747.28

Formula

C43H43ClN4O6
CAS 号

1448525-91-4
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
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 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-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Casara P, et al. S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth. Oncotarget. 2018 Apr 13;9(28):20075-20088.

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