FIIN-2 - CAS 1633044-56-0
Catalog number: 1633044-56-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C35H38N8O4
Molecular Weight:
634.73
COA:
Inquire
Targets:
FGFR
Description:
FIIN-2 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor. FIIN-2 is the first inhibitor that can potently inhibit the proliferation of cells dependent upon the gatekeeper mutants of FGFR1 or FGFR2, which confer resistance to first-generation clinical FGFR inhibitors such as NVP-BGJ398 and AZD4547.
Purity:
98%
Appearance:
Solid powder
Synonyms:
FIIN2; FIIN 2; FIIN-2.
Solubility:
Soluble in DMSO, not in water
Storage:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years if stored properly
Canonical SMILES:
O=C(NC1=CC=C(C=C1)CN2C(N(CC3=CN=C(N=C32)NC4=CC=C(C=C4)N5CCN(CC5)C)C6=CC(OC)=CC(OC)=C6)=O)C=C
1.FGFR inhibitors: Effects on cancer cells, tumor microenvironment and whole-body homeostasis (Review).
Katoh M Int J Mol Med. 2016 Jul;38(1):3-15. doi: 10.3892/ijmm.2016.2620. Epub 2016 May 31.
Fibroblast growth factor (FGF)2, FGF4, FGF7 and FGF20 are representative paracrine FGFs binding to heparan-sulfate proteoglycan and fibroblast growth factor receptors (FGFRs), whereas FGF19, FGF21 and FGF23 are endocrine FGFs binding to Klotho and FGFRs. FGFR1 is relatively frequently amplified and overexpressed in breast and lung cancer, and FGFR2 in gastric cancer. BCR-FGFR1, CNTRL-FGFR1, CUX1-FGFR1, FGFR1OP-FGFR1, MYO18A-FGFR1 and ZMYM2-FGFR1 fusions in myeloproliferative neoplasms are non-receptor-type FGFR kinases, whereas FGFR1-TACC1, FGFR2-AFF3, FGFR2-BICC1, FGFR2-PPHLN1, FGFR3-BAIAP2L1 and FGFR3-TACC3 fusions in solid tumors are transmembrane-type FGFRs with C-terminal alterations. AZD4547, BGJ398 (infigratinib), Debio-1347 and dovitinib are FGFR1/2/3 inhibitors; BLU9931 is a selective FGFR4 inhibitor; FIIN-2, JNJ-42756493, LY2874455 and ponatinib are pan-FGFR inhibitors. AZD4547, dovitinib and ponatinib are multi-kinase inhibitors targeting FGFRs, colony stimulating factor 1 receptor (CSF1R), vascular endothelial growth factor (VEGF)R2, and others. The tumor microenvironment consists of cancer cells and stromal/immune cells, such as cancer-associated fibroblasts (CAFs), endothelial cells, M2-type tumor-associating macrophages (M2-TAMs), myeloid-derived suppressor cells (MDSCs) and regulatory T cells.
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