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RPI-1

CAS No. : 269730-03-2

MCE 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：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Lenvatinib  |  Regorafenib  |  Pralsetinib  |  Selpercatinib  |  Amuvatinib  |  BT-13  |  TG101209  |  Ilorasertib hydrochloride  |  AST 487  |  BBT594  |  AD80  |  GSK3179106  |  SPP-86  |  WHI-P180  |  RET-IN-3  |  RET V804M-IN-1  |  WF-47-JS03  |  Pz-1  |  JNJ-38158471  |  ML786 dihydrochloride  |  RET-IN-4  |  RET-IN-1

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