SIAIS178

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SIAIS178  纯度: 99.48%

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。

SIAIS178

SIAIS178 Chemical Structure

CAS No. : 2376047-73-1

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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[1].

IC50 & Target[1]

VHL

 

Bcr-Abl

24 nM (IC50)

体外研究
(In Vitro)

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[1].
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[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: 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 [1].
SIAIS178 (iv or ip; 2 mg/kg; 24 hours) has T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively[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: NOD/SCID mice with termed K562-Luc[1]
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[1]
Dosage: 2 mg/kg (Pharmacokinetic Analysis)
Administration: Iv or ip; 24 hours
Result: Had T1/2 of 3.82 and 12.35 hours and Cmax of 1165.2 nM and 30 nM for iv and ip, respectively.

分子量

1012.68

Formula

C50H62ClN11O6S2

CAS 号

2376047-73-1

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
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

*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]. Zhao Q, et al. Discovery of SIAIS178 as an Effective BCR-ABL Degrader by Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase. J Med Chem. 2019 Oct 24;62(20):9281-9298.

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