FIIN3|CAS 1637735-84-2|DC Chemicals

Cas No.:	1637735-84-2
Chemical Name:	FIIN-3
Synonyms:	FIIN-3;FIIN 3
SMILES:	C=CC(NC1=CC=C(CN(C(NC2=C(Cl)C(OC)=CC(OC)=C2Cl)=O)C3=NC=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=C3)C=C1)=O
Formula:	C₃₄H₃₆Cl₂N₈O₄
M.Wt:	691.606844902039
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

FIIN-3 is an irreversible inhibitor of FGFR with an IC50 of 13.1, 21, 31.4, and 35.3 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively.

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[1].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

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