RPI-1
new
featured

We are open as normal during COVID-19 pandemic. Order online, same day shipping out from North Carolina, USA

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

MedKoo CAT#: 407385

CAS#: 269730-03-2

Description: 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..


Price and Availability

Size Price Shipping out time Quantity
100mg USD 450 2 Weeks
200mg USD 750 2 Weeks
500mg USD 1450 2 Weeks
1g USD 2450 2 Weeks
5g USD 5250 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-23. Prices are subject to change without notice.

RPI-1, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

img

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


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


Technical Data

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


References

1: 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. PubMed PMID: 20955590; PubMed Central PMCID: PMC2967544.

2: 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. PubMed PMID: 16985073.

3: 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. PubMed PMID: 16756963.

4: Cuccuru G, Lanzi C, Cassinelli G, Pratesi G, Tortoreto M, Petrangolini G, Seregni E, Martinetti A, Laccabue D, Zanchi C, Zunino F. Cellular effects and antitumor activity of RET inhibitor RPI-1 on MEN2A-associated medullary thyroid carcinoma. J Natl Cancer Inst. 2004 Jul 7;96(13):1006-14. PubMed PMID: 15240784.

5: Lanzi C, Cassinelli G, Cuccuru G, Zaffaroni N, Supino R, Vignati S, Zanchi C, Yamamoto M, Zunino F. Inactivation of Ret/Ptc1 oncoprotein and inhibition of papillary thyroid carcinoma cell proliferation by indolinone RPI-1. Cell Mol Life Sci. 2003 Jul;60(7):1449-59. PubMed PMID: 12943231.

6: 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. PubMed PMID: 25850922.

7: 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. PubMed PMID: 21741956.

8: 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. PubMed PMID: 19555670.

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. PubMed PMID: 26065416; PubMed Central PMCID: PMC4466258.

10: Lanzi C, Cassinelli G, Cuccuru G, Zanchi C, Laccabue D, Zunino F. RET/PTC oncoproteins: molecular targets of new drugs. Tumori. 2003 Sep-Oct;89(5):520-2. PubMed PMID: 14870776.

11: 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):220-31. doi: 10.1002/mc.20474. PubMed PMID: 18756447.

12: 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. PubMed PMID: 27930654; PubMed Central PMCID: PMC5145144.

13: 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. PubMed PMID: 27167204; PubMed Central PMCID: PMC5095042.

14: 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. PubMed PMID: 21751813.

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. PubMed PMID: 19107227; PubMed Central 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. PubMed PMID: 19053769.

17: 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. PubMed PMID: 17499504.

18: Peden-McAlpine C, Tomlinson PS, Forneris SG, Genck G, Meiers SJ. Evaluation of a reflective practice intervention to enhance family care. J Adv Nurs. 2005 Mar;49(5):494-501. PubMed PMID: 15713181.

19: Stanisich VA, Bennett PM, Oritz JM. A molecular analysis of transductional marker rescue involving P-group plasmids in Pseudomonas aeruginosa. Mol Gen Genet. 1976 Feb 2;143(3):333-7. PubMed PMID: 814405.