SIAIS178|cas:2376047-73-1|西域试剂

SIAIS178,99.36%

产品编号：Bellancom-128756| CAS NO：2376047-73-1| 分子式：C₅₀H₆₂ClN₁₁O₆S₂| 分子量：1012.68

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货号	价格	库存与货期
Bellancom-128756	￥2000.00	杭州北京（现货）
Bellancom-128756	￥4800.00	杭州北京（现货）
Bellancom-128756	￥6500.00	杭州北京（现货）
Bellancom-128756	￥19500.00	杭州北京（现货）
Bellancom-128756	￥27500.00	杭州北京（现货）

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SIAIS178

产品介绍

SIAIS178 是一种 PROTAC 类的有效的，选择性的 BCR-ABL 降解剂，IC₅₀ 为 24 nM。SIAIS178 通过募集 Von Hippel-Lindau (VHL) E3 泛素连接酶来降解 BCR-ABL 蛋白。SIAIS178 具有抗肿瘤活性。

生物活性

SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC₅₀ of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.

体外研究

SIAIS178 (1-100 nM; for 16 hours) significantly reduces the BCR-ABL protein levels in a concentration dependent manner. SIAIS178 significantly inhibits the phosphorylation of BCR-ABL and the substrates STAT5.
SIAIS178 (1, 10, 100, 1000 nM) exerts significant antiproliferative activity in BCR-ABL driven CML cell lines. SIAIS178 retains potency and selectivity against the BCR-ABL driven cell lines.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	K562 cells
Concentration:	1, 3, 10, 30, 100 nM
Incubation Time:	16 hours
Result:	Significantly reduced the BCR-ABL protein levels in a concentration dependent manner.

体内研究
(In Vivo)

SIAIS178 (ip; 5, 15, and 45 mg/kg; 12 days) attenuates tumor progression in a dose-dependent manner, as determined by serial volumetric measurement .
SIAIS178 (iv or ip; 2 mg/kg; 24 hours) has T_1/2 of 3.82 and 12.35 hours and C_max of 1165.2 nM and 30 nM for iv and ip, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NOD/SCID mice with termed K562-Luc
Dosage:	5, 15, and 45 mg/kg
Administration:	Ip; 12 days
Result:	Attenuated tumor progression in a dose-dependent manner, as determined by serial volumetric measurement.

Animal Model:	Female Wistar rats
Dosage:	2 mg/kg (Pharmacokinetic Analysis)
Administration:	Iv or ip; 24 hours
Result:	Had T_1/2 of 3.82 and 12.35 hours and C_max of 1165.2 nM and 30 nM for iv and ip, respectively.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NOD/SCID mice with termed K562-Luc
Dosage:	5, 15, and 45 mg/kg
Administration:	Ip; 12 days
Result:	Attenuated tumor progression in a dose-dependent manner, as determined by serial volumetric measurement.

Animal Model:	Female Wistar rats
Dosage:	2 mg/kg (Pharmacokinetic Analysis)
Administration:	Iv or ip; 24 hours
Result:	Had T_1/2 of 3.82 and 12.35 hours and C_max of 1165.2 nM and 30 nM for iv and ip, respectively.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NOD/SCID mice with termed K562-Luc
Dosage:	5, 15, and 45 mg/kg
Administration:	Ip; 12 days
Result:	Attenuated tumor progression in a dose-dependent manner, as determined by serial volumetric measurement.

Animal Model:	Female Wistar rats
Dosage:	2 mg/kg (Pharmacokinetic Analysis)
Administration:	Iv or ip; 24 hours
Result:	Had T_1/2 of 3.82 and 12.35 hours and C_max of 1165.2 nM and 30 nM for iv and ip, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 300 mg/mL (296.24 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.9875 mL	4.9374 mL	9.8748 mL
5 mM	0.1975 mL	0.9875 mL	1.9750 mL
10 mM	0.0987 mL	0.4937 mL	0.9875 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。-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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 7.5 mg/mL (7.41 mM); Clear solution

此方案可获得 ≥ 7.5 mg/mL (7.41 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 75.0 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液