RBN-2397|cas:2381037-82-5|西域试剂

RBN-2397,99.86%

产品编号：Bellancom-136174| CAS NO：2381037-82-5| 分子式：C₂₀H₂₃F₆N₇O₃| 分子量：523.43

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-136174	￥5000.00	杭州北京（现货）
Bellancom-136174	￥8500.00	杭州北京（现货）
Bellancom-136174	￥12500.00	杭州北京（现货）
Bellancom-136174	￥0.00	杭州北京（现货）
Bellancom-136174	￥0.00	杭州北京（现货）

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RBN-2397

产品介绍

RBN-2397 是一种强效的，跨物种的，且具有口服活性的 NAD⁺ 竞争性 PARP7 抑制剂，IC₅₀ 值小于 3 nM。RBN-2397 有选择性地结合 PARP7 (K_d=0.001 μM) 并可以恢复干扰素 I 型信号转导。RBN-2397 有潜力用于研究晚期或转移性实体肿瘤。

生物活性

RBN-2397 is a potent, accross species and orally active NAD⁺ competitive inhibitor of PARP7 (IC₅₀<3 nM). RBN-2397 selectively binds to PARP7 (K_d=0.001 μM) and restores IFN signaling. RBN-2397 has the potential for the study of advanced or metastatic solid tumors.

体外研究

RBN-2397 (0.0001-100 μM; 24 hours) inhibits cells proliferation with an IC₅₀ value of 20 nM in NCI-H1373 lung cancer cells.
RBN-2397 (0.4 nM-1 μM; 24 hours) shows a restoration of type I IFN response by an increase in STAT1 phosphorylation as a dose-dependent manner in NCI-H1373 human lung cancer cells.
RBN-2397 (0.0001-1 μM; 24 hours) inhibits cell MARylation in a cell biochemial assay with an EC₅₀ value of 1 nM.

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

Cell Proliferation Assay

Cell Line:	NCI-H1373 lung cancer cells
Concentration:	0.0001 μM; 0.001 μM; 0.001 μM; 0.1 μM; 1 μM; 10 μM; 100 μM
Incubation Time:	24 hours
Result:	Blocked cell proliferation.

Western Blot Analysis

Cell Line:	NCI-H1373 lung cancer cells
Concentration:	0.4 nM-1 μM
Incubation Time:	24 hours
Result:	Increased p-STAT1 protein expression.

体内研究
(In Vivo)

RBN-2397 (oral administration; 3-100 mg/kg; once daily; 24-32 days) induces tumor-specific adaptive immune memory in CT26 syngeneic model with durable complete responses in CT26 tumor-bearing BALB/c mice.
RBN-2397 (oral administration; 3-100 mg/kg; once daily; 32 days) causes complete regressions at the dose 100 mg/kg and exerts a dose-dependent effects on tumor growth at dose levels of ≥30 mg/kg.
The half-life (t_1/2) of RBN-2397 in vivo is 325 mins.

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

Animal Model:	CB17 SCID mice with NCI-H1373 xenografts
Dosage:	3 mg/kg, 10mg/kg, 30 mg/kg, 100 mg/kg
Administration:	Oral administration; once daily; 24-32 days
Result:	Decreased tumor volume and exerted anti-tumor effects.

体内研究

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

Animal Model:	CB17 SCID mice with NCI-H1373 xenografts
Dosage:	3 mg/kg, 10mg/kg, 30 mg/kg, 100 mg/kg
Administration:	Oral administration; once daily; 24-32 days
Result:	Decreased tumor volume and exerted anti-tumor effects.

体内研究

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

Animal Model:	CB17 SCID mice with NCI-H1373 xenografts
Dosage:	3 mg/kg, 10mg/kg, 30 mg/kg, 100 mg/kg
Administration:	Oral administration; once daily; 24-32 days
Result:	Decreased tumor volume and exerted anti-tumor effects.

性状

Solid

溶解性数据

In Vitro:

DMSO : 200 mg/mL (382.10 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9105 mL	9.5524 mL	19.1048 mL
5 mM	0.3821 mL	1.9105 mL	3.8210 mL
10 mM	0.1910 mL	0.9552 mL	1.9105 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： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.78 mM); Clear solution
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.97 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.97 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
4.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.97 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.97 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
5.

请依序添加每种溶剂： 1% DMSO 99% saline
Solubility: ≥ 0.5 mg/mL (0.96 mM); Clear solution