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FIIN-2
CAS No. 1633044-56-0
FIIN-2( FIIN2 | FIIN 2 | FIIN-2 )
Catalog No. M17351 CAS No. 1633044-56-0
FIIN-2, an irreversible, pan-FGFR inhibitor, inhibits FGFR1/2/3/4 with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 86 | In Stock |
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| 2MG | 46 | In Stock |
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| 5MG | 61 | In Stock |
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| 10MG | 93 | In Stock |
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| 25MG | 198 | In Stock |
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| 50MG | 295 | In Stock |
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| 100MG | Get Quote | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameFIIN-2
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NoteResearch use only, not for human use.
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Brief DescriptionFIIN-2, an irreversible, pan-FGFR inhibitor, inhibits FGFR1/2/3/4 with IC50 of 3.09 nM, 4.3 nM, 27 nM and 45.3 nM, respectively.
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DescriptionFIIN-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. FIIN-2 also binds in the DFG-out mode despite lacking a functional group necessary to occupy the pocket vacated upon the DFG-out flip.
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In VitroFIIN-2 potently inhibits WT FGFRs (EC50s in the 1- to 93-nM range) and the gatekeeper mutant of FGFR2 (EC50 of 58 nM). FIIN-2 also moderately inhibits EGFR, with an IC50 of 204 nM. FIIN-2 inhibits proliferation of FGFR1-4 Ba/F3 cells with EC50s in the single- to double-digit nanomolar range and are especially potent against FGFR2, with EC50s in the 1-nM range. FIIN-2 shows good potency against gatekeeper mutant V564F.
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In VivoTreatment of fish in the embryonic state with either FIIN-2 causes defects to the posterior mesoderm similar to the phenotypes reported following genetic knockdown of FGFR or treatment with other reported FGFR inhibitors. FIIN-2 causes mild or severe phenotypes to the tail morphogenesis in all treated embryonic zebrafish.
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SynonymsFIIN2 | FIIN 2 | FIIN-2
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PathwayGPCR/G Protein
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TargetDopamine Receptor
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RecptorFGFR1| FGFR2| FGFR3| FGFR4
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number1633044-56-0
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Formula Weight634.73
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Molecular FormulaC35H38N8O4
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 30 mg/mL 47.26 mM
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SMILESCN1CCN(CC1)c1ccc(cc1)Nc1ncc2CN(C(=O)N(c2n1)Cc1ccc(cc1)NC(=O)C=C)c1cc(cc(c1)OC)OC
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Chemical NameN-(4-((3-(3,5-dimethoxyphenyl)-7-((4-(4-methylpiperazin-1-yl)phenyl)amino)-2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidin-1(2H)-yl)methyl)phenyl)acrylamide
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Tan L, et al. Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors. Proc Natl Acad Sci U S A. 2014 Nov 11;111(45):E4869-4877.
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