Derazantinib


Catalog No. size PriceQuantity
M7106-2 2mg solid $138
M7106-10 10mg solid $556

Description

Cas:1234356-69-4

Product Information

Derazantinib, also known as ARQ-087, is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. FGFR inhibitor ARQ 087 binds to and potently inhibits the activity of FGFR subtypes 1, 2 and 3. This may result in the inhibition of FGFR-mediated signal transduction pathways, tumor cell proliferation, tumor angiogenesis and tumor cell death in FGFR-overexpressing tumor cells. FGFR, a receptor tyrosine kinase, is upregulated in many tumor cell types and plays a key role in tumor cellular proliferation, differentiation, angiogenesis and survival.

 

Chemical Formula: C29H29FN4O

 

Exact Mass: 468.2325

 

Molecular Weight: 468.5764

 

Elemental Analysis: C, 74.34; H, 6.24; F, 4.05; N, 11.96; O, 3.41

 

Synonym: 

 

ARQ 087

ARQ087

ARQ-087

 

Chemical Name: (6R)-6-(2-fluorophenyl)-N-(3-{2-[(2-methoxyethyl)amino]ethyl}phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine

 

InChi Key: 

KPJDVVCDVBFRMU-AREMUKBSSA-N

 

InChi Code: InChI=1S/C29H29FN4O/c1-35-16-15-31-14-13-20-7-6-8-22(17-20)33-29-32-19-21-18-26(24-10-4-5-12-27(24)30)23-9-2-3-11-25(23)28(21)34-29/h2-12,17,19,26,31H,13-16,18H2,1H3,(H,32,33,34)/t26-/m1/s1

 

Smiles Code:

COCCNCCC1=CC(NC2=NC=C3C[C@@H](C4=CC=CC=C4F)C5=CC=CC=C5C3=N2)=CC=C1

Technical Data:

 

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

 

In Vitro:

In cells, inhibition of FGFR2 auto-phosphorylation and other proteins downstream in the FGFR pathway (FRS2α, AKT, ERK) is evident by the response to Derazantinib treatment. Cell proliferation studies demonstrate Derazantinib has anti-proliferative activity in cell lines driven by FGFR dysregulation, including amplifications, fusions, and mutations. Cell cycle studies in cell lines with high levels of FGFR2 protein show a positive relationship between Derazantinib induced G1 cell cycle arrest and subsequent induction of apoptosis. Derazantinib rescues the FGF2-mediated growth arrest with EC50 at about 100 nM, with no significant toxicity detected for up to 500 nM. The concentration range at which Derazantinib significantly suppresses the FGF2 effect is between 70-500 nM. Derazantinib inhibits FGF-mediated loss of extracellular matrix and induction of chondrocyte premature senescence. Derazantinib rescues FGF-mediated inhibition of chondrocyte differentiation in tibia cultures. Derazantinib inhibits FGFR1-4 but no other receptor tyrosine kinases in cell-free kinase assay. Derazantinib inhibits FGFR1 and FGFR2 mutants associated with craniosynostoses. Derazantinib rescues FGFR-mediated bone differentiation in mouse limb bud micromass cultures and ex vivo mouse calvarial organ cultures.

 

In Vivo:

Derazantinib is effective at inhibiting tumor growth in FGFR2 altered, SNU-16 and NCI-H716, xenograft tumor models with gene amplifications and fusions. Most of the embryos exhibit abnormal external phenotype (81.3%) in Derazantinib-injected wings, possibly due to inhibition of proliferation of limb bud mesenchyme. The wings are shorter and thinner, with skeletal phenotype typical for FGFR inhibition, where ulna and radius are shorter or smaller in size, or occasionally missing completely

 

 

References

  1. Rossi LD, Vasconcelos GC, Saliba GR, Magalhaes Lde C, Soares AM, Cordeiro SS, Amorim RH. [Reliability of functional vision assessment in children with low vision from 2 to 6 years old--searching for evidences]. Arq Bras Oftalmol. 2012 Jul-Aug;75(4):259-63. Portuguese. PubMed PMID: 23258657.

 

  1. Ganguli D, Das N, Saha I, Sanapala KR, Chaudhuri D, Ghosh S, Dey S. Association between inflammatory markers and cardiovascular risk factors in women from Kolkata, W.B, India. Arq Bras Cardiol. 2011 Jan;96(1):38-46. Epub 2010 Dec 22. English, Portuguese, Spanish. PubMed PMID: 21180893.

 

  1. Castinheiras-Neto AG, Costa-Filho IR, Farinatti PT. [Cardiovascular responses to resistance exercise are affected by workload and intervals between sets]. Arq Bras Cardiol. 2010 Oct;95(4):493-501. Multiple languages. PubMed PMID: 21180785.

 

  1. Castinheiras-Neto AG, Costa-Filho IR, Farinatti PT. [Cardiovascular responses to resistance exercise are affected by workload and intervals between sets.]. Arq Bras Cardiol. 2010 Sep 3. pii: S0066-782X2010005000119. [Epub ahead of print] Portuguese. PubMed PMID: 20802962.

 

  1. Dantas RO, Alves LM, Cassiani Rde A. Gender differences in proximal esophageal contractions. Arq Gastroenterol. 2009 Oct-Dec;46(4):284-7. PubMed PMID: 20232007.

 

  1. Gonçalves AA, Cardão FL, Soares MG, Weksler A, Weksler C, Tura BR, da Silva PR, da Rocha AS. Predictive value of angina to detect coronary artery disease in patients with severe aortic stenosis aged 50 years or older. Arq Bras Cardiol. 2006 Dec;87(6):701-4. English, Portuguese. PubMed PMID: 17262106.

 

Products are for research use only. Not for human use.

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