IACS-13909|cas:2160546-07-4|西域试剂

IACS-13909,99.93%

产品编号：Bellancom-137092| CAS NO：2160546-07-4| 分子式：C₁₇H₁₈Cl₂N₆| 分子量：377.27

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货号	价格	库存与货期
Bellancom-137092	￥3000.00	杭州北京（现货）
Bellancom-137092	￥5000.00	杭州北京（现货）
Bellancom-137092	￥10500.00	杭州北京（现货）

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IACS-13909

产品介绍

IACS-13909 是一种有效的选择性的，具有口服活性的 SHP2 变构抑制剂，其 IC₅₀ 为 15.7 nM，K_d 为 32 nM。与其他磷酸酶 (包括 SHP1) 相比，IACS-13909 对 SHP2 的选择性更高。IACS-13909 抑制受体酪氨酸激酶 (RTK)/MAPK 途径的信号传导，并具有抗癌作用。

生物活性

IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC₅₀ of 15.7 nM and a K_d of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers.

体外研究

IACS-13909 (10 nM-10 μM; 14 days) treatment potently suppresses the proliferation of wild-type SHP2 and KYSE-520 cells.
IACS-13909 (1-5 μM; 2 hours) treatment potently suppresses pERK and pMEK levels in wild-type SHP2 and KYSE-520 cells.
IACS-13909 potently suppresses the proliferation of both the parental cells and NCI-H1975 CS cells in a dose-dependent manner, with similar potency (GI50 ~1 μM). IACS-13909 (0.041-3.3 μM) suppresses pERK in NCI-H1975 CS cells in a dose-dependent manner.

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

Cell Proliferation Assay

Cell Line:	Wild-type SHP2 and KYSE-520 cells
Concentration:	10 nM, 100 nM, 1 μM, 10 μM
Incubation Time:	14 days
Result:	Potently suppressed the cell proliferation.

Western Blot Analysis

Cell Line:	Wild-type SHP2 and KYSE-520 cells
Concentration:	1 μM, 5 μM
Incubation Time:	2 hours
Result:	Potently suppressed pERK and pMEK levels.

体内研究
(In Vivo)

IACS-13909 (70 mg/kg; oral administration; daily; for 21 days) treatment potently suppresses tumor growth in mice, with 100% tumor growth inhibition (TGI) observed following 21 days of dosing.

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

Animal Model:	NSG mice (20-28 g) injected with KYSE-520 cells
Dosage:	70 mg/kg
Administration:	Oral administration; daily; for 21 days
Result:	Potently suppressed tumor growth in mice.

体内研究

IACS-13909 (70 mg/kg; oral administration; daily; for 21 days) treatment potently suppresses tumor growth in mice, with 100% tumor growth inhibition (TGI) observed following 21 days of dosing.

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

Animal Model:	NSG mice (20-28 g) injected with KYSE-520 cells
Dosage:	70 mg/kg
Administration:	Oral administration; daily; for 21 days
Result:	Potently suppressed tumor growth in mice.

体内研究

IACS-13909 (70 mg/kg; oral administration; daily; for 21 days) treatment potently suppresses tumor growth in mice, with 100% tumor growth inhibition (TGI) observed following 21 days of dosing.

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

Animal Model:	NSG mice (20-28 g) injected with KYSE-520 cells
Dosage:	70 mg/kg
Administration:	Oral administration; daily; for 21 days
Result:	Potently suppressed tumor growth in mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 10 mg/mL (26.51 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6506 mL	13.2531 mL	26.5062 mL
5 mM	0.5301 mL	2.6506 mL	5.3012 mL
10 mM	0.2651 mL	1.3253 mL	2.6506 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: ≥ 1 mg/mL (2.65 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.65 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 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