RC-3095

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

Hodoodo CAT#: H202430

CAS#: 138147-78-1

Description: RC-3095 is a gastrin-releasing peptide receptor antagonist, synergizes with gemcitabine to inhibit the growth of human pancreatic cancer CFPAC-1 in vitro and in vivo. RC-3095 inhibit the growth of human glioblastomas in vitro and in vivo. RC3095 inhibits tumor growth and decrease the levels and mRNA expression of epidermal growth factor receptors in H-69 small cell lung carcinoma.

Chemical Structure

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RC-3095
CAS# 138147-78-1
Instruction

Theoretical Analysis

Hodoodo Cat#: H202430
Name: RC-3095
CAS#: 138147-78-1
Chemical Formula: C56H79N15O9
Exact Mass: 1,105.62
Molecular Weight: 1,106.320
Elemental Analysis: C, 60.80; H, 7.20; N, 18.99; O, 13.02

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Synonym: RC3095; RC-3095; RC 3095; Amino acid sequences: (D-TPI6, LEU13 y(CH2-NH)-LEU14)BOMBESIN (6-14).

IUPAC/Chemical Name: (S)-N1-((2S,5S,8S,14S,17S,20S)-14-((1H-imidazol-5-yl)methyl)-20-carbamoyl-1-(1H-indol-3-yl)-17-isobutyl-8-isopropyl-5,22-dimethyl-3,6,9,12,15-pentaoxo-4,7,10,13,16,19-hexaazatricosan-2-yl)-2-((R)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole-3-carboxamido)pentanediamide

InChi Key: IUYCRRDHLJIJBB-QAGBKCHLSA-N

InChi Code: InChI=1S/C56H79N15O9/c1-29(2)18-35(25-61-42(50(58)74)19-30(3)4)66-55(79)45(21-34-24-59-28-64-34)68-48(73)27-63-56(80)49(31(5)6)71-51(75)32(7)65-54(78)44(20-33-23-60-39-14-10-8-12-36(33)39)70-52(76)41(16-17-47(57)72)69-53(77)43-22-38-37-13-9-11-15-40(37)67-46(38)26-62-43/h8-15,23-24,28-32,35,41-45,49,60-62,67H,16-22,25-27H2,1-7H3,(H2,57,72)(H2,58,74)(H,59,64)(H,63,80)(H,65,78)(H,66,79)(H,68,73)(H,69,77)(H,70,76)(H,71,75)/t32-,35-,41-,42-,43+,44-,45-,49-/m0/s1

SMILES Code: O=C(N[C@H](C(N[C@@H](C)C(N[C@@H](C(C)C)C(NCC(N[C@@H](CC1=CN=CN1)C(N[C@@H](CC(C)C)CN[C@H](C(N)=O)CC(C)C)=O)=O)=O)=O)=O)CC2=CNC3=C2C=CC=C3)[C@@H](NC([C@H]4CC5=C(CN4)NC6=C5C=CC=C6)=O)CCC(N)=O

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, not in water

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: RC-3095 is a potent BB2 (GRP-preferring) bombesin receptor antagonist.        

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 1,106.32 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Hong SK, Yang SY, Yin SH, Yang KX. RC-3095, a gastrin-releasing peptide receptor antagonist, synergizes with gemcitabine to inhibit the growth of human pancreatic cancer CFPAC-1 in vitro and in vivo. Pancreas. 2014 Jan;43(1):15-21. doi: 10.1097/MPA.0b013e3182a714cf. PubMed PMID: 24326363.

2: Oliveira PG, Grespan R, Pinto LG, Meurer L, Brenol JC, Roesler R, Schwartsmann G, Cunha FQ, Xavier RM. Protective effect of RC-3095, an antagonist of the gastrin-releasing peptide receptor, in experimental arthritis. Arthritis Rheum. 2011 Oct;63(10):2956-65. doi: 10.1002/art.30486. PubMed PMID: 21953084.

3: Merali Z, Mountney C, Kent P, Anisman H. Effects of intracerebral ventricular administration of gastrin-releasing peptide and its receptor antagonist RC-3095 on learned fear responses in the rat. Behav Brain Res. 2011 Jan 20;216(2):519-24. doi: 10.1016/j.bbr.2010.08.027. Epub 2010 Aug 27. PubMed PMID: 20801162.

4: Cassol OJ Jr, Rezin GT, Petronilho FC, Scaini G, Gonçalves CL, Ferreira GK, Roesler R, Schwartsmann G, Dal-Pizzol F, Streck EL. Effects of N-acetylcysteine/deferoxamine, taurine and RC-3095 on respiratory chain complexes and creatine kinase activities in rat brain after sepsis. Neurochem Res. 2010 Apr;35(4):515-21. doi: 10.1007/s11064-009-0089-3. PubMed PMID: 20238483.

5: Sotomayor S, Muñoz-Moreno L, Carmena MJ, Schally AV, Sánchez-Chapado M, Prieto JC, Bajo AM. Regulation of HER expression and transactivation in human prostate cancer cells by a targeted cytotoxic bombesin analog (AN-215) and a bombesin antagonist (RC-3095). Int J Cancer. 2010 Oct 15;127(8):1813-22. doi: 10.1002/ijc.25192. PubMed PMID: 20099275.

6: Damin DC, Santos FS, Heck R, Rosito MA, Meurer L, Kliemann LM, Roesler R, Schwartsmann G. Effects of the gastrin-releasing peptide antagonist RC-3095 in a rat model of ulcerative colitis. Dig Dis Sci. 2010 Aug;55(8):2203-10. doi: 10.1007/s10620-009-1032-9. Epub 2009 Nov 6. PubMed PMID: 19894117.

7: de Oliveira MS, Cechim G, Braganhol E, Santos DG, Meurer L, de Castro CG Jr, Brunetto AL, Schwartsmann G, Battastini AM, Lenz G, Roesler R. Anti-proliferative effect of the gastrin-release peptide receptor antagonist RC-3095 plus temozolomide in experimental glioblastoma models. J Neurooncol. 2009 Jun;93(2):191-201. doi: 10.1007/s11060-008-9775-2. Epub 2009 Jan 8. Erratum in: J Neurooncol. 2009 Jun;93(2):203. Schwarstmann, Gilberto [corrected to Schwartsmann, Gilberto]. PubMed PMID: 19129973.

8: Dantas Ados S, Luft T, Henriques JA, Schwartsmann G, Roesler R. Opposite effects of low and high doses of the gastrin-releasing peptide receptor antagonist RC-3095 on memory consolidation in the hippocampus: possible involvement of the GABAergic system. Peptides. 2006 Sep;27(9):2307-12. Epub 2006 May 2. PubMed PMID: 16650508.

9: Martins MR, Reinke A, Valvassori SS, Machado RA, Quevedo J, Schwartsmann G, Roesler R. Non-associative learning and anxiety in rats treated with a single systemic administration of the gastrin-releasing peptide receptor antagonist RC-3095. Peptides. 2005 Dec;26(12):2525-9. Epub 2005 Jul 14. PubMed PMID: 16023260.

10: Pereira AS, DiLeone L, Souza FH, Lilla S, Richter M, Schwartsmann G, De Nucci G. Quantification of the bombesin/gastrin releasing peptide antagonist RC-3095 by liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2005 Feb 25;816(1-2):321-6. PubMed PMID: 15664365.

11: Meller CA, Henriques JA, Schwartsmann G, Roesler R. The bombesin/gastrin releasing peptide receptor antagonist RC-3095 blocks apomorphine but not MK-801-induced stereotypy in mice. Peptides. 2004 Apr;25(4):585-8. PubMed PMID: 15165713.

12: Roesler R, Kopschina MI, Rosa RM, Henriques JA, Souza DO, Schwartsmann G. RC-3095, a bombesin/gastrin-releasing peptide receptor antagonist, impairs aversive but not recognition memory in rats. Eur J Pharmacol. 2004 Feb 13;486(1):35-41. PubMed PMID: 14751406.

13: Roesler R, Meller CA, Kopschina MI, Souza DO, Henriques JA, Schwartsmann G. Intrahippocampal infusion of the bombesin/gastrin-releasing peptide antagonist RC-3095 impairs inhibitory avoidance retention. Peptides. 2003 Jul;24(7):1069-74. PubMed PMID: 14499286.

14: Chatzistamou I, Schally AV, Szepeshazi K, Groot K, Hebert F, Arencibia JM. Inhibition of growth of ES-2 human ovarian cancers by bombesin antagonist RC-3095, and luteinizing hormone-releasing hormone antagonist Cetrorelix. Cancer Lett. 2001 Sep 28;171(1):37-45. PubMed PMID: 11485826.

15: Kahán Z, Sun B, Schally AV, Arencibia JM, Cai RZ, Groot K, Halmos G. Inhibition of growth of MDA-MB-468 estrogen-independent human breast carcinoma by bombesin/gastrin-releasing peptide antagonists RC-3095 and RC-3940-II. Cancer. 2000 Mar 15;88(6):1384-92. PubMed PMID: 10717621.

16: Koppán M, Halmos G, Arencibia JM, Lamharzi N, Schally AV. Bombesin/gastrin-releasing peptide antagonists RC-3095 and RC-3940-II inhibit tumor growth and decrease the levels and mRNA expression of epidermal growth factor receptors in H-69 small cell lung carcinoma. Cancer. 1998 Oct 1;83(7):1335-43. PubMed PMID: 9762934.

17: Miyazaki M, Lamharzi N, Schally AV, Halmos G, Szepeshazi K, Groot K, Cai RZ. Inhibition of growth of MDA-MB-231 human breast cancer xenografts in nude mice by bombesin/gastrin-releasing peptide (GRP) antagonists RC-3940-II and RC-3095. Eur J Cancer. 1998 Apr;34(5):710-7. PubMed PMID: 9713279.

18: Szepeshazi K, Schally AV, Halmos G, Lamharzi N, Groot K, Horvath JE. A single in vivo administration of bombesin antagonist RC-3095 reduces the levels and mRNA expression of epidermal growth factor receptors in MXT mouse mammary cancers. Proc Natl Acad Sci U S A. 1997 Sep 30;94(20):10913-8. PubMed PMID: 9380734; PubMed Central PMCID: PMC23529.

19: Halmos G, Schally AV. Reduction in receptors for bombesin and epidermal growth factor in xenografts of human small-cell lung cancer after treatment with bombesin antagonist RC-3095. Proc Natl Acad Sci U S A. 1997 Feb 4;94(3):956-60. PubMed PMID: 9023364; PubMed Central PMCID: PMC19621.

20: Pinski J, Schally AV, Halmos G, Szepeshazi K, Groot K. Somatostatin analogues and bombesin/gastrin-releasing peptide antagonist RC-3095 inhibit the growth of human glioblastomas in vitro and in vivo. Cancer Res. 1994 Nov 15;54(22):5895-901. PubMed PMID: 7954420.