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CAS No. : 269730-03-2
MCE 国际站:RPI-1
产品活性:RPI-1 是一种特异的口服 2-吲哚啉酮 Ret 酪氨酸激酶抑制剂。RPI-1 抑制人甲状腺髓样癌 TT 细胞增殖、Ret 酪氨酸磷酸化、Ret 蛋白表达及 PLCgamma、ERKs 和 AKT 的活化。具有抗肿瘤活性。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:RET
In Vitro: TPC-1 cells are sensitive to the growth inhibitory effect of RPI-1 with an IC50 of 5.1 μM, following 72 hours of treatment. RPI-1 (7.5-60 µM) inhibits Ret/Ptc1 autophosphorylation in TPC-1 cells. RPI-1 inhibitory effects in the TPC-1 cell culture conditions lead to inhibition of pathways involving JNK2 and AKT.
The RPI-1 IC50 value for cell proliferation is 3.6 µM in NIH3T3 cells expressing the Ret mutant compared with 16 µM in non-transfected NIH3T3 cells, and that for colony formation in soft agar was 2.4 µM and 26 µM in RET mutant-transfected and H-RAS-transfected NIH3T3 cells, respectively. In NIH3T3 cells expressing the Ret mutant, Ret protein and tyrosine phosphorylation were undetectable after 24 hours of RPI-1 treatment. In TT cells, RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT.
In Vivo: RPI-1 (50, 100 mg/kg; p.o.; twice a day for 10 days) inhibits the tumor growth of TT xenografts by 81%.
相关产品:Natural Product-like Compound Library | Bioactive Compound Library Plus | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Liver Cancer Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | trans-Pralsetinib | RET-IN-24 | BT-13 | RET-IN-16 | WF-47-JS03 | Pyrazoloadenine | GSK3179106 | RET-IN-1 | Lenvatinib-d5 | Pz-1 | Regorafenib monohydrate | RET-IN-14 | AD57 | AD80 | FLT3/ITD-IN-4 | RET-IN-18 | Regorafenib-13C,d3 | RET V804M-IN-1 | RET-IN-19 | Enbezotinib | RET-IN-6 | BT44 | TG101209 | Regorafenib-d3 | Amuvatinib | WHI-P180 | RET-IN-10
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
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货号: HY-101246
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