LY3200882
目录号 : KM2454 CAS No. : 1898283-02-7 纯度 : 98%

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。

规格 价格 是否有货 数量
5mg
In-stock
10mg
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50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

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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.

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).

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.
分子式
C24H29N5O3
分子量
435.52
CAS号
1898283-02-7
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 : 130 mg/mL (298.49 mM; Need ultrasonic and warming)

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。

  • 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。

  • 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。

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