WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407124
CAS#: 1229611-73-7
Description: LCRF-0004 is a potent and selective RON receptor tyrosine kinase inhibitor. The RON receptor tyrosine kinase has been identified as an important mediator of KRAS oncogene addiction and is overexpressed in the majority of pancreatic cancers. Preclinical studies show that inhibition of RON function decreases pancreatic cancer cell migration, invasion, and survival and can sensitize pancreatic cancer cells to chemotherapy. RON receptor tyrosine kinase is a potential as a therapeutic target.
MedKoo Cat#: 407124
Name: LCRF-0004
CAS#: 1229611-73-7
Chemical Formula: C28H18F4N6O2S
Exact Mass: 578.11481
Molecular Weight: 578.55
Elemental Analysis: C, 58.13; H, 3.14; F, 13.14; N, 14.53; O, 5.53; S, 5.54
Synonym: LCRF-0004; LCRF 0004; LCRF0004.
IUPAC/Chemical Name: N-(3-fluoro-4-((2-(1-methyl-1H-imidazol-4-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)-1-phenyl-5-(trifluoromethyl)-1H-pyrazole-4-carboxamide
InChi Key: DVRMYRDLCLUXQP-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H18F4N6O2S/c1-37-14-21(34-15-37)24-12-20-25(41-24)23(9-10-33-20)40-22-8-7-16(11-19(22)29)36-27(39)18-13-35-38(26(18)28(30,31)32)17-5-3-2-4-6-17/h2-15H,1H3,(H,36,39)
SMILES Code: O=C(C1=C(C(F)(F)F)N(C2=CC=CC=C2)N=C1)NC3=CC=C(OC4=C5C(C=C(C6=CN(C)C=N6)S5)=NC=C4)C(F)=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, 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
The following data is based on the product molecular weight 578.55 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 |
1: Raeppel F, Raeppel SL, Therrien E. Design, synthesis and RON receptor tyrosine kinase inhibitory activity of new head groups analogs of LCRF-0004. Bioorg Med Chem Lett. 2015 Jul 29. pii: S0960-894X(15)00784-2. doi: 10.1016/j.bmcl.2015.07.080. [Epub ahead of print] PubMed PMID: 26243370.
2: Raeppel SL, Therrien E, Raeppel F. Design and synthesis of constrained analogs of LCRF-0004 as potent RON tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3706-10. doi: 10.1016/j.bmcl.2015.06.034. Epub 2015 Jun 15. PubMed PMID: 26112445.
3: Raeppel SL, Raeppel F, Therrien E. Design and synthesis of close analogs of LCRF-0004, a potent and selective RON receptor tyrosine kinase inhibitor. Bioorg Med Chem Lett. 2015 Jun 15;25(12):2527-31. doi: 10.1016/j.bmcl.2015.04.056. Epub 2015 Apr 23. PubMed PMID: 25953155.
