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FIIN-2

SKU: orb1223255

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. 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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Images & Validation

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FIIN-2

Key Properties

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CAS Number1633044-56-0
MW634.73
Purity>98% (HPLC)
FormulaC35H38N8O4
SMILESCN1CCN(CC1)c1ccc(cc1)Nc1ncc2CN(C(=O)N(c2n1)Cc1ccc(cc1)NC(=O)C=C)c1cc(cc(c1)OC)OC
TargetDopamine Receptor
SolubilityDMSO : ≥ 30 mg/mL 47.26 mM

Bioactivity

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In Vivo
Treatment 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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In Vitro
FIIN-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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Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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FIIN2 | FIIN 2 | FIIN-2

Similar Products

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  • FIIN-2

    FIIN-2 [orb1300421]

    99.34%

    1633044-56-0

    634.73

    C35H38N8O4

    2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 1 mg, 1 ml x 10 mM (in DMSO)
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Gene Symbol
Dopamine Receptor

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FIIN-2 (orb1223255)

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2 mg
$ 90.00
5 mg
$ 150.00
10 mg
$ 230.00
25 mg
$ 420.00
50 mg
$ 730.00
100 mg
$ 1,030.00
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