WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H406556
CAS#: 865362-74-9
Description: FR180204 is a novel and selective inhibitor of extracellular signal-regulated kinase (ERK), which may be a potential new therapy for rheumatoid arthritis.FR180204 showed activity to inhibit ERKs (IC50 values are 0.14 and 0.31 μ M for ERK2 and ERK1 respectively).
Hodoodo Cat#: H406556
Name: FR180204
CAS#: 865362-74-9
Chemical Formula: C18H13N7
Exact Mass: 327.12
Molecular Weight: 327.340
Elemental Analysis: C, 66.04; H, 4.00; N, 29.95
Synonym: FR180204; FR-180204; FR 180204.
IUPAC/Chemical Name: 5-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1H-pyrazolo[3,4-c]pyridazin-3-amine
InChi Key: XVECMUKVOMUNLE-UHFFFAOYSA-N
InChi Code: InChI=1S/C18H13N7/c19-17-12-10-13(20-22-18(12)23-21-17)15-14-8-4-5-9-25(14)24-16(15)11-6-2-1-3-7-11/h1-10H,(H3,19,21,22,23)
SMILES Code: NC1=NNC2=NN=C(C3=C4C=CC=CN4N=C3C5=CC=CC=C5)C=C21
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:
| Biological target: | FR 180204 is an ATP-competitive and selective ERK inhibitor. |
| In vitro activity: | As shown in Fig. 3A, treatment with 2 µM API-1 caused an increase in cytotoxicity at 24 h in DLD-1 cells (P=0.027), whereas treatment with 10 µM FR (FR180204) alone for 48 h increased cytotoxic effects compared with control LoVo cells. Reference: Oncol Lett. 2016 Oct; 12(4): 2463–2474. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5038487/ |
| In vivo activity: | Preventive administration of FR180204 (100 mg/kg, i.p., b.i.d.) significantly ameliorated the clinical arthritis and body weight loss occurring in the CIA mice. Further, FR180204-treated mice showed a significant decrease in plasma anti-CII antibody levels (62%). Reference: Naunyn Schmiedebergs Arch Pharmacol. 2007 Jan;374(4):311-6. https://pubmed.ncbi.nlm.nih.gov/17123065/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.2 | 131.91 | |
| DMF | 30.0 | 91.65 | |
| DMF:PBS (pH 7.2) (1:1) | 0.5 | 1.53 | |
| Ethanol | 2.0 | 6.11 |
The following data is based on the product molecular weight 327.34 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. Saglam AS, Alp E, Elmazoglu Z, Menevse ES. Effect of API-1 and FR180204 on cell proliferation and apoptosis in human DLD-1 and LoVo colorectal cancer cells. Oncol Lett. 2016 Oct;12(4):2463-2474. doi: 10.3892/ol.2016.4995. Epub 2016 Aug 10. PMID: 27698814; PMCID: PMC5038487. 2. Ohori M, Takeuchi M, Maruki R, Nakajima H, Miyake H. FR180204, a novel and selective inhibitor of extracellular signal-regulated kinase, ameliorates collagen-induced arthritis in mice. Naunyn Schmiedebergs Arch Pharmacol. 2007 Jan;374(4):311-6. doi: 10.1007/s00210-006-0117-7. Epub 2006 Nov 23. PMID: 17123065. |
| In vitro protocol: | 1. Saglam AS, Alp E, Elmazoglu Z, Menevse ES. Effect of API-1 and FR180204 on cell proliferation and apoptosis in human DLD-1 and LoVo colorectal cancer cells. Oncol Lett. 2016 Oct;12(4):2463-2474. doi: 10.3892/ol.2016.4995. Epub 2016 Aug 10. PMID: 27698814; PMCID: PMC5038487. |
| In vivo protocol: | 1. Ohori M, Takeuchi M, Maruki R, Nakajima H, Miyake H. FR180204, a novel and selective inhibitor of extracellular signal-regulated kinase, ameliorates collagen-induced arthritis in mice. Naunyn Schmiedebergs Arch Pharmacol. 2007 Jan;374(4):311-6. doi: 10.1007/s00210-006-0117-7. Epub 2006 Nov 23. PMID: 17123065. |
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