LY3200882|cas:1898283-02-7|西域试剂

LY3200882,99.60%

产品编号：Bellancom-103021| CAS NO：1898283-02-7| 分子式：C₂₄H₂₉N₅O₃| 分子量：435.52

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-103021	￥1200.00	杭州北京（现货）
Bellancom-103021	￥1900.00	杭州北京（现货）
Bellancom-103021	￥6500.00	杭州北京（现货）
Bellancom-103021	￥11000.00	杭州北京（现货）

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LY3200882

产品介绍

LY3200882 是一种有效的，高度选择性的，具有 ATP 竞争性和口服活性的 TGF-β 受体 1 型 (ALK5) 抑制剂，IC₅₀ 为 38.2 nM。LY3200882 可抑制多种促肿瘤活性，还用作免疫调节剂。

生物活性

LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC₅₀ of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent.

体外研究

LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells in a dose dependent fashion.
LY3200882 shows potent anti-tumor activity in the orthotopic 4T1-LP model of triple negative breast cancer and this activity correlated with enhanced tumor infiltrating lymphocytes in the tumor microenvironment.
In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed naive T cell activity and restore proliferation.
LY3200882 inhibits NIH₃T₃ cell viability with an IC₅₀ of 82.9 nM.

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

体内研究

LY3200882 (60 mg/kg; oral gavage; twice a day; for 21 days; BALB/C female mice) treatment significantly delays tumor growth in CT26 model.
LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vivo in subcutaneous tumors in a dose dependent fashion.
LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer).

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

Animal Model:	BALB/C female mice (5-8-week-old) injected with CT26 cells
Dosage:	60 mg/kg
Administration:	Oral gavage; twice a day; for 21 days
Result:	A statistically significant tumor growth delay in CT26 model was observed.

体内研究

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

Animal Model:	BALB/C female mice (5-8-week-old) injected with CT26 cells
Dosage:	60 mg/kg
Administration:	Oral gavage; twice a day; for 21 days
Result:	A statistically significant tumor growth delay in CT26 model was observed.

性状

Solid

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (76.53 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2961 mL	11.4805 mL	22.9611 mL
5 mM	0.4592 mL	2.2961 mL	4.5922 mL
10 mM	0.2296 mL	1.1481 mL	2.2961 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: ≥ 2.5 mg/mL (5.74 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.74 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.74 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.74 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。