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MedKoo Cat#: 407385 | Name: RPI-1
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

RPI-1 is an ATP-dependent RET kinase inhibitor. Oral treatment with RPI-1 caused growth arrest or regression in 81% treated tumors. Following treatment suspension, tumor inhibition was maintained (51%, P<0.05, 100 days) and cures were achieved in 2/11 mice. In vivo effects of RPI-1 were reflected in activation of BAD, cleavage of caspases, apoptotic DNA fragmentation and inhibition of VEGF production observed in in vitro RPI-1-treated TT cells..

Chemical Structure

RPI-1
RPI-1
CAS#269730-03-2

Theoretical Analysis

MedKoo Cat#: 407385

Name: RPI-1

CAS#: 269730-03-2

Chemical Formula: C17H15NO4

Exact Mass: 297.1001

Molecular Weight: 297.31

Elemental Analysis: C, 68.68; H, 5.09; N, 4.71; O, 21.53

Price and Availability

Size Price Availability Quantity
10mg USD 300.00 2 Weeks
25mg USD 550.00 2 Weeks
50mg USD 850.00 2 Weeks
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Related CAS #
No Data
Synonym
RPI-1; RPI1; RPI 1.
IUPAC/Chemical Name
1,3-dihydro-3-[(4-hydroxyphenyl)methylene]-5,6-dimethoxy-2H-indol-2-one
InChi Key
JGSMCYNBVCGIHC-QPEQYQDCSA-N
InChi Code
InChI=1S/C17H15NO4/c1-21-15-8-12-13(7-10-3-5-11(19)6-4-10)17(20)18-14(12)9-16(15)22-2/h3-9,19H,1-2H3,(H,18,20)/b13-7-
SMILES Code
O=C1NC2=C(C=C(OC)C(OC)=C2)/C1=C/C3=CC=C(O)C=C3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 297.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Rangra GS, Singh Y, Thapa K, Khattar JIS, Singh DP. Spatiotemporal distribution of cyanobacteria in relation to water chemistry of Sutlej River, Punjab (India). Environ Monit Assess. 2024 Sep 17;196(10):937. doi: 10.1007/s10661-024-13011-4. PMID: 39285104. 2: Kaplan OI. RPI-1 (human DCDC2) displays functional redundancy with Nephronophthisis 4 in regulating cilia biogenesis in C. elegans. Turk J Biol. 2022 Nov 21;47(1):74-83. doi: 10.55730/1300-0152.2642. PMID: 37529113; PMCID: PMC10388106. 3: Ohishi K, Hosono K, Obana A, Noda A, Hiramitsu T, Hotta Y, Minoshima S. Identification of susceptibility loci for light-induced visual impairment in rats. Exp Eye Res. 2021 Sep;210:108688. doi: 10.1016/j.exer.2021.108688. Epub 2021 Jul 5. PMID: 34237304. 4: Cha JW, Yoon IS, Lee GW, Kang SI, Park SY, Kim JS, Heu MS. Food functionalities and bioactivities of protein isolates recovered from skipjack tuna roe by isoelectric solubilization and precipitation. Food Sci Nutr. 2020 Feb 20;8(4):1874-1887. doi: 10.1002/fsn3.1470. PMID: 32328253; PMCID: PMC7174228. 5: Giardino E, Catalano R, Barbieri AM, Treppiedi D, Mangili F, Spada A, Arosio M, Mantovani G, Peverelli E. Cofilin is a mediator of RET-promoted medullary thyroid carcinoma cell migration, invasion and proliferation. Mol Cell Endocrinol. 2019 Sep 15;495:110519. doi: 10.1016/j.mce.2019.110519. Epub 2019 Jul 25. PMID: 31352037. 6: Yoon IS, Lee HJ, Kang SI, Park SY, Kang YM, Kim JS, Heu MS. Food functionality of protein isolates extracted from Yellowfin Tuna (Thunnus albacares) roe using alkaline solubilization and acid precipitation process. Food Sci Nutr. 2019 Jan 28;7(2):412-424. doi: 10.1002/fsn3.793. PMID: 30847118; PMCID: PMC6392840. 7: Jensen VL, Carter S, Sanders AA, Li C, Kennedy J, Timbers TA, Cai J, Scheidel N, Kennedy BN, Morin RD, Leroux MR, Blacque OE. Whole-Organism Developmental Expression Profiling Identifies RAB-28 as a Novel Ciliary GTPase Associated with the BBSome and Intraflagellar Transport. PLoS Genet. 2016 Dec 8;12(12):e1006469. doi: 10.1371/journal.pgen.1006469. PMID: 27930654; PMCID: PMC5145144. 8: Zhong Z, Gu H, Peng J, Wang W, Johnstone BH, March KL, Farlow MR, Du Y. GDNF secreted from adipose-derived stem cells stimulates VEGF-independent angiogenesis. Oncotarget. 2016 Jun 14;7(24):36829-36841. doi: 10.18632/oncotarget.9208. PMID: 27167204; PMCID: PMC5095042. 9: Burdine LJ, Burdine MS, Moreland L, Fogel B, Orr LM, James J, Turnage RH, Tackett AJ. Proteomic Identification of DNA-PK Involvement within the RET Signaling Pathway. PLoS One. 2015 Jun 11;10(6):e0127943. doi: 10.1371/journal.pone.0127943. PMID: 26065416; PMCID: PMC4466258. 10: Goto K, Kawahara I, Kuniyasu H, Takaki M. A protein tyrosine kinase receptor, c-RET signaling pathway contributes to the enteric neurogenesis induced by a 5-HT4 receptor agonist at an anastomosis after transection of the gut in rodents. J Physiol Sci. 2015 Jul;65(4):377-83. doi: 10.1007/s12576-015-0377-4. Epub 2015 Apr 8. PMID: 25850922; PMCID: PMC10717718. 11: Caccia D, Zanetti Domingues L, Miccichè F, De Bortoli M, Carniti C, Mondellini P, Bongarzone I. Secretome compartment is a valuable source of biomarkers for cancer-relevant pathways. J Proteome Res. 2011 Sep 2;10(9):4196-207. doi: 10.1021/pr200344n. Epub 2011 Jul 29. PMID: 21751813. 12: Nicolini V, Cassinelli G, Cuccuru G, Bongarzone I, Petrangolini G, Tortoreto M, Mondellini P, Casalini P, Favini E, Zaffaroni N, Zunino F, Lanzi C. Interplay between Ret and Fap-1 regulates CD95-mediated apoptosis in medullary thyroid cancer cells. Biochem Pharmacol. 2011 Oct 1;82(7):778-88. doi: 10.1016/j.bcp.2011.06.037. Epub 2011 Jul 2. PMID: 21741956. 13: Caccia D, Miccichè F, Cassinelli G, Mondellini P, Casalini P, Bongarzone I. Dasatinib reduces FAK phosphorylation increasing the effects of RPI-1 inhibition in a RET/PTC1-expressing cell line. Mol Cancer. 2010 Oct 18;9:278. doi: 10.1186/1476-4598-9-278. PMID: 20955590; PMCID: PMC2967544. 14: Cassinelli G, Ronchetti D, Laccabue D, Mattioli M, Cuccuru G, Favini E, Nicolini V, Greco A, Neri A, Zunino F, Lanzi C. Concomitant downregulation of proliferation/survival pathways dependent on FGF-R3, JAK2 and BCMA in human multiple myeloma cells by multi-kinase targeting. Biochem Pharmacol. 2009 Nov 1;78(9):1139-47. doi: 10.1016/j.bcp.2009.06.023. Epub 2009 Jun 23. PMID: 19555670. 15: Cassinelli G, Favini E, Degl'Innocenti D, Salvi A, De Petro G, Pierotti MA, Zunino F, Borrello MG, Lanzi C. RET/PTC1-driven neoplastic transformation and proinvasive phenotype of human thyrocytes involve Met induction and beta-catenin nuclear translocation. Neoplasia. 2009 Jan;11(1):10-21. doi: 10.1593/neo.08916. PMID: 19107227; PMCID: PMC2606114. 16: Cincinelli R, Cassinelli G, Dallavalle S, Lanzi C, Merlini L, Botta M, Tuccinardi T, Martinelli A, Penco S, Zunino F. Synthesis, modeling, and RET protein kinase inhibitory activity of 3- and 4-substituted beta-carbolin-1-ones. J Med Chem. 2008 Dec 25;51(24):7777-87. doi: 10.1021/jm8007823. PMID: 19053769. 17: Gorla L, Mondellini P, Cuccuru G, Miccichè F, Cassinelli G, Cremona M, Pierotti MA, Lanzi C, Bongarzone I. Proteomics study of medullary thyroid carcinomas expressing RET germ-line mutations: identification of new signaling elements. Mol Carcinog. 2009 Mar;48(3):220-231. doi: 10.1002/mc.20474. PMID: 18756447. 18: Rizzi E, Cassinelli G, Dallavalle S, Lanzi C, Cincinelli R, Nannei R, Cuccuru G, Zunino F. Synthesis and RET protein kinase inhibitory activity of 3-arylureidobenzylidene-indolin-2-ones. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3962-8. doi: 10.1016/j.bmcl.2007.04.091. Epub 2007 Apr 30. PMID: 17499504. 19: Cassinelli G, Lanzi C, Petrangolini G, Tortoreto M, Pratesi G, Cuccuru G, Laccabue D, Supino R, Belluco S, Favini E, Poletti A, Zunino F. Inhibition of c-Met and prevention of spontaneous metastatic spreading by the 2-indolinone RPI-1. Mol Cancer Ther. 2006 Sep;5(9):2388-97. doi: 10.1158/1535-7163.MCT-06-0245. PMID: 16985073. 20: Petrangolini G, Cuccuru G, Lanzi C, Tortoreto M, Belluco S, Pratesi G, Cassinelli G, Zunino F. Apoptotic cell death induction and angiogenesis inhibition in large established medullary thyroid carcinoma xenografts by Ret inhibitor RPI-1. Biochem Pharmacol. 2006 Aug 14;72(4):405-14. doi: 10.1016/j.bcp.2006.05.002. Epub 2006 Jun 6. PMID: 16756963.

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