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FIIN-3

SKU: orb1223253

Description

FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor. FIIN-3 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-3 has the unprecedented ability to inhibit both the EGF receptor (EGFR) and FGFR covalently by targeting two distinct cysteine residues. FIIN-3 bound with FGFR4 V550L and EGFR L858R.
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Images & Validation

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FIIN-3

Key Properties

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CAS Number1637735-84-2
MW691.61
Purity>98% (HPLC)
FormulaC34H36Cl2N8O4
SMILESC(=O)(C=C)Nc1ccc(cc1)CN(c1ncnc(c1)Nc1ccc(cc1)N1CCN(CC1)C)C(=O)Nc1c(c(cc(c1Cl)OC)OC)Cl
TargetSirtuin
SolubilityDMSO : 10 mg/mL 14.46 mM;

Bioactivity

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In Vitro
FIIN-3 potently inhibits both WT FGFRs (EC50 in the 1- to 41-nM range) and the gatekeeper mutant of FGFR2 (EC50 of 64 nM). FIIN-3 also strongly inhibits EGFR, with an EC50 of 43 nM. FIIN-3 shows good potency against gatekeeper mutant V564F; FIIN-3 also is potent against the gatekeeper-plus-1 mutant E565K; FIIN-3 also displays antiproliferative activity (with an EC50 of 135 nM) against Ba/F3 cells transformed by the EGFR vIII fusion protein, which has a WT EGFR kinase domain. FIIN-3 shows even better activity against EGFR mutant L858R (EC50 of 17 nM) and moderate activity, displaying an EC50 of 231 nM, against the EGFR mutant L858R/T790M mutant. In WT FGFR2 Ba/F3 cells, FIIN-3 completely inhibits the FGFR2 autophosphorylation on Tyr656/657 at concentrations as low as 3 nM. In FGFR2 V564M Ba/F3 cells, FIIN-3 is capable of inhibiting the FGFR2 mutant V564M autophosphorylation with partial inhibition at 100 nM and complete inhibition observed at 300 nM.
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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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FIIN3 | FIIN 3 | FIIN-3

Similar Products

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  • FIIN-3

    FIIN-3 [orb1304176]

    98.92% (May vary between batches)

    1637735-84-2

    691.61

    C34H36Cl2N8O4

    1 mg, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg
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Gene Symbol
Sirtuin

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FIIN-3 (orb1223253)

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2 mg
$ 130.00
5 mg
$ 190.00
10 mg
$ 290.00
25 mg
$ 600.00
50 mg
$ 870.00
100 mg
$ 1,220.00
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