货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T93585-1ml促销	10mM in DMSO	￥974.00 ￥972.00 T93585-1ml ￥972.00 现货	1 1	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T93585-1ml促销

10mM in DMSO

￥974.00 ￥972.00

产品描述：

TGFβRI/ALK5 选择性抑制剂;TGFβRI/ALK5 Selective Inhibitors;;InformationLY 3200882 is a potent, highly selective inhibitor ofTGF-β receptor type 1 (TGFβRI). It potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion.TargetsTGFβRIIn vitroLY3200882 inhibits various pro-tumorigenic activities. LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion. In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed naïve T cell activity and restore proliferation. It acts as an immune modulatory agent.In vivoIn preclinical tumor models, LY3200882 showed 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. Durable tumor regressions in the orthotopic 4T1-LP model were observed and rechallenge of congenic tumors resulted in complete rejection in all mice. LY3200882 has shown anti-metastatic activity in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer). In addition, LY3200882 shows combinatorial anti-tumor benefits with checkpoint inhibition (anti-PD-L1) in the syngeneic CT26 model.

靶点：

IC50: 38.2 nM (TGF-β receptor type 1 (ALK5))

体内研究：

LY3200882 (60 mg/kg；口服管饲；每日两次；持续 21 天；BALB/C 雌性小鼠) 治疗可显著延缓 CT26 模型中的肿瘤生长。
LY3200882 以剂量依赖性方式强效抑制皮下肿瘤中 TGFβ 介导的 SMAD 磷酸化。
LY3200882 在实验转移性肿瘤模型 (三阴性乳腺癌静脉注射 EMT6-LM2 模型) 中表现出体内抗转移活性。

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.296 ml	11.481 ml	22.961 ml
5 mM	0.459 ml	2.296 ml	4.592 ml
10 mM	0.23 ml	1.148 ml	2.296 ml
50 mM	0.046 ml	0.23 ml	0.459 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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