FR180204 | CAS#865362-74-9 | ERK inhibitor

MedKoo Cat#: 406556 | Name: FR180204

Description:

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

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).

Chemical Structure

FR180204

CAS#865362-74-9

Theoretical Analysis

MedKoo Cat#: 406556

Name: FR180204

CAS#: 865362-74-9

Chemical Formula: C18H13N7

Exact Mass: 327.1232

Molecular Weight: 327.34

Elemental Analysis: C, 66.04; H, 4.00; N, 29.95

Price and Availability

Size	Price	Availability
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 1,950.00	2 Weeks
1g	USD 2,950.00	2 Weeks
2g	USD 5,450.00	2 Weeks

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Related CAS #

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Synonym

FR180204; FR-180204; FR 180204; ERK Inhibitor II

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

Product Data

Product Data

Instruction

View handling instruction

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	mg/mL	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

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 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:

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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