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RPI-1 | CAS 269730-03-2 | SCBT - Santa Cruz Biotechnology
RPI-1 CAS: 269730-03-2
MF: C17H15NO4
MW: 297.31
A cell-permeable ATP-competitive tyrosine kinase inhibitor.

RPI-1 (CAS 269730-03-2)

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別名: RET Receptor Tyrosine Kinase Inhibitor; 1,3-dihydro-5,6-dimethoxy-3-[(4-hydroxyphenyl)methylene]-H-indol-2-one; (3E)-3-[(4-hydroxyphenyl)methylidene]-5,6-dimethoxy-1H-indol-2-one
アプリケーション: RPI-1 is a cell-permeable ATP-competitive tyrosine kinase inhibitor
CAS 番号: 269730-03-2
Purity: ≥95%
Molecular Weight: 297.31
Molecular Formula: C17H15NO4
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* Refer to Certificate of Analysis for lot specific data (including water content).
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RPI-1 is a cell-permeable, indolinone-based ATP-competitive tyrosine kinase inhibitor that is known to target Ret, EGFR, and Met. Increased tumorigenicity, motility, and invasiveness have been described as biological consequences of HGF/Met deregulation in tumor cells, thus RPI-1 treatment of H460 cells resulted in a strong reduction of both colony number and size. The compound is also active at mouse NSCLC H460 xenograft tumor and metastasis model. Mechanistically RPI-1 inhibits Met phosphorylation at Tyr1234/Tyr1235, known to activate the intrinsic kinase activity. Selectively reverts the morphologic phenotype of ret oncogene- (PTC1 & MEN2A), but not H-Ras-, and transformed NIH3T3 in a reversible manner. RPI-1 effectively inhibits the autophosphorylation of PTC1, MEN2A, and Met against Met in N592 in cancer cells, and concomitant receptor down-regulation has also been reported to occur in NIH3T3MEN2A and in small cell lung carcinoma cell line N592.


参考文献

Cassinelli G., et al., RET/PTC1-driven neoplastic transformation and proinvasive phenotype of human thyrocytes involve Met induction and beta-catenin nuclear translocation Neoplasia 1st ed., 11, 10-21, (2009) Gorla L., et al., Proteomics study of medullary thyroid carcinomas expressing RET germ-line mutations: identification of new signaling elements Mol. Carcinog. 3rd ed., 48, 220-31, (2009) Cassinelli G., et al., Inhibition of c-Met and prevention of spontaneous metastatic spreading by the 2-indolinone RPI-1 Mol. Cancer Ther. 9th ed., 5, 2388-97, (2006)

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO: >20 mg/mL
保存方法 :
Store at 4° C
Boiling Point :
533.6±50.0° C at 760 mmHg (Predicted)
Density :
1.3±0.1 g/cm3 (Predicted)
試験・研究用以外には使用しないでください。 臨床及び体外診断には使用できません。
WGK Germany :
3
PubChem CID :
SMILES :
COC1=C(C=C2C(=C1)C(=CC3=CC=C(C=C3)O)C(=O)N2)OC

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RPI-1 (CAS 269730-03-2)  参考文献

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