SG3199|cas:1595275-71-0|西域试剂

SG3199,98.94%

产品编号：Bellancom-101161| CAS NO：1595275-71-0| 分子式：C₃₃H₃₆N₄O₆| 分子量：584.66

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-101161		￥8500.00	杭州北京（现货）

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SG3199

产品介绍

SG3199 是一种具有细胞毒性的 DNA 小沟链间交联 PBD 二聚体。SG3199 是 ADC 有效载荷 Tesirine (SG3249) 的组成成分。

生物活性

SG3199 is a cytotoxic DNA minor groove interstrand crosslinking pyrrolobenzodiazepine (PBD) dimer. SG3199 is the released warhead component of the ADC payload Tesirine (SG3249).

体外研究

SG3199 is potently cytotoxic against a panel of human solid tumour and haematological cancer cell lines with a mean GI₅₀ of 151.5 pM. Cells defective in DNA repair protein ERCC1 or homologous recombination repair show increased sensitivity to SG3199 and the drug is only moderately susceptible to multidrug resistance mechanisms.
SG3199 is highly efficient at producing DNA interstrand cross-links in naked linear plasmid DNA and dose-dependent cross-linking is observed in cells.

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

体内研究

The in vitro binding of [³H]-SG3199 to the plasma proteins of rat (Sprague Dawley), cynomolgus monkey and human at concentrations of 0.8, 5 and 50 ng/mL is determined. Plasma protein binding is high in all species; rat ∼97%, cynomolgus monkey ∼90% and human ∼95%.
Following i.v. administration at 0.1 μg/kg, 0.5 μg/kg and 1 μg/kg, SG3199 shows a very rapid clearance in rats. In the 0.5 μg/kg and 1 μg/kg dose groups, the rapid clearance was between 1000 and 1500 mL/h/kg, with a T_1/2 between 8 and 42 minutes.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 130 mg/mL (222.35 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7104 mL	8.5520 mL	17.1040 mL
5 mM	0.3421 mL	1.7104 mL	3.4208 mL
10 mM	0.1710 mL	0.8552 mL	1.7104 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 (protect from light, 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 3.25 mg/mL (5.56 mM); Clear solution

此方案可获得 ≥ 3.25 mg/mL (5.56 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 32.5 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 3.25 mg/mL (5.56 mM); Clear solution

此方案可获得 ≥ 3.25 mg/mL (5.56 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 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。