Synonym
RON-IN-1; RON IN 1; RONIN1; RON inhibitor 1; RON inhibitor-1; Ron Inhibitor I; Met Kinase Inhbitor IV;
IUPAC/Chemical Name
N-(3-fluoro-4-(7-methoxyquinolin-4-yl)phenyl)-1-(2-hydroxy-2-methylpropyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide
InChi Key
DPJYVCMPSFKLIZ-UHFFFAOYSA-N
InChi Code
InChI=1S/C31H29FN4O4/c1-19-28(30(38)36(21-8-6-5-7-9-21)35(19)18-31(2,3)39)29(37)34-20-10-12-24(26(32)16-20)23-14-15-33-27-17-22(40-4)11-13-25(23)27/h5-17,39H,18H2,1-4H3,(H,34,37)
SMILES Code
COC1=CC2=NC=CC(C3=CC=C(NC(C4=C(C)N(CC(C)(O)C)N(C5=CC=CC=C5)C4=O)=O)C=C3F)=C2C=C1
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 and ethanol
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
Biological target:
RON-IN-1 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC50s ranging from 160 to 710 nM. RON-IN-1 can be used for the research of cancers that RON and c-Met are activated.
In vitro activity:
To be determined
In vivo activity:
In this model of calvarial bone defects in mice, treatment with RON-IN-1 or SGX523 inhibited hepatocyte growth factor-induced c-Met phosphorylation in MC3T3-E1 and C3H10T1/2 cells. Cell proliferation of MC3T3-E1 or C3H10T1/2 was not significantly affected by the concentrations of these inhibitors.
Reference: Eur J Pharmacol. 2017 Jul 5;806:10-17. https://pubmed.ncbi.nlm.nih.gov/28322831/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
100.0 |
179.67 |
| Ethanol |
60.0 |
107.80 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
540.59
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.
| 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:
1. Kim JW, Lee MN, Jeong BC, Oh SH, Kook MS, Koh JT. Chemical inhibitors of c-Met receptor tyrosine kinase stimulate osteoblast differentiation and bone regeneration. Eur J Pharmacol. 2017 Jul 5;806:10-17. doi: 10.1016/j.ejphar.2017.03.032. Epub 2017 Mar 16. PMID: 28322831.
2. Zhang Y, Kaplan-Lefko PJ, Rex K, Yang Y, Moriguchi J, Osgood T, Mattson B, Coxon A, Reese M, Kim TS, Lin J, Chen A, Burgess TL, Dussault I. Identification of a novel recepteur d'origine nantais/c-met small-molecule kinase inhibitor with antitumor activity in vivo. Cancer Res. 2008 Aug 15;68(16):6680-7. doi: 10.1158/0008-5472.CAN-07-6782. PMID: 18701492.
In vitro protocol:
To be determined
In vivo protocol:
1. Kim JW, Lee MN, Jeong BC, Oh SH, Kook MS, Koh JT. Chemical inhibitors of c-Met receptor tyrosine kinase stimulate osteoblast differentiation and bone regeneration. Eur J Pharmacol. 2017 Jul 5;806:10-17. doi: 10.1016/j.ejphar.2017.03.032. Epub 2017 Mar 16. PMID: 28322831.
2. Zhang Y, Kaplan-Lefko PJ, Rex K, Yang Y, Moriguchi J, Osgood T, Mattson B, Coxon A, Reese M, Kim TS, Lin J, Chen A, Burgess TL, Dussault I. Identification of a novel recepteur d'origine nantais/c-met small-molecule kinase inhibitor with antitumor activity in vivo. Cancer Res. 2008 Aug 15;68(16):6680-7. doi: 10.1158/0008-5472.CAN-07-6782. PMID: 18701492.
1: Lipinski MJ, Lee RC, Gaglia MA Jr, Torguson R, Garcia-Garcia HM, Pichard AD, Satler LF, Waksman R. Comparison of heparin, bivalirudin, and different glycoprotein IIb/IIIa inhibitor regimens for anticoagulation during percutaneous coronary intervention: A network meta-analysis. Cardiovasc Revasc Med. 2016 Dec;17(8):535-545. doi: 10.1016/j.carrev.2016.09.011. Epub 2016 Sep 30. Review. PubMed PMID: 27842901.
2: Samis J, Lee P, Zimmerman D, Arceci RJ, Suttorp M, Hijiya N. Recognizing Endocrinopathies Associated With Tyrosine Kinase Inhibitor Therapy in Children With Chronic Myelogenous Leukemia. Pediatr Blood Cancer. 2016 Aug;63(8):1332-8. doi: 10.1002/pbc.26028. Epub 2016 Apr 21. Review. PubMed PMID: 27100618.
3: Lipinski MJ, Benedetto U, Escarcega RO, Biondi-Zoccai G, Lhermusier T, Baker NC, Torguson R, Brewer HB Jr, Waksman R. The impact of proprotein convertase subtilisin-kexin type 9 serine protease inhibitors on lipid levels and outcomes in patients with primary hypercholesterolaemia: a network meta-analysis. Eur Heart J. 2016 Feb 7;37(6):536-45. doi: 10.1093/eurheartj/ehv563. Epub 2015 Nov 17. Review. PubMed PMID: 26578202.
4: Zheng Q, Wu H, Cao J, Ye J. Hepatocyte growth factor activator inhibitor type 1 in cancer: advances and perspectives (Review). Mol Med Rep. 2014 Dec;10(6):2779-85. doi: 10.3892/mmr.2014.2628. Epub 2014 Oct 13. Review. PubMed PMID: 25310042.
5: Kooijman R. Regulation of apoptosis by insulin-like growth factor (IGF)-I. Cytokine Growth Factor Rev. 2006 Aug;17(4):305-23. Epub 2006 Apr 18. Review. PubMed PMID: 16621671.
