FIIN-4
SIGMA/SML1956 - ≥98% (HPLC)
Synonym: FIIN4; N-
CAS Number: 2093088-81-2
Empirical Formula (Hill Notation): C35H38N8O4
Molecular Weight: 634.73
Linear Formula: C35H38N8O4
Product Type: Chemical
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| assay | ≥98% (HPLC) |
| color | white to beige |
| form | powder |
| Quality Level | 100  |
| solubility | DMSO: 10 mg/mL, clear |
| storage condition | protect from light |
| storage temp. | 2-8°C |
| Biochem/physiol Actions: | A potent covalent type II inhibitor against FGFR with in vitro and in vivo anti-breast cancer efficacy. |
| Biochem/physiol Actions: | FIIN-4 is a potent, irreversible, type II inhibitor against FGFR (IC50 = 2.6, 2.6, 5.6, 9.2 nM, respectively, against FGFR1-4) whose 4-acrylamidebenzyl moiety covalently modifies FGFR P-loop cysteine in its DFG-out conformation with good target selectivity based on a 456-kinase panel (354 non-mutants kinases) kinome profiling. FIIN-4 effectively inhibits FGF2-induced Erk1/2 phosphorylation in serum-starved D2.A1 murine mammary carcinoma cells (by 100% wtih 18-hr 250 nM pretreatment) and D2.A1 growth in 3D cultures (by 54% at 100 nM) without affecting EGF-dependent Erk phosphorylation or 3D growth of NMuMG murine mammary epithelial cells. Oral administration (25 mg/kg q.o.d.) is efficacious in suppressing the growths of tumors-derived from murine mammary carcinoma 4T1 lung metastases and patient TNBC brain metastases xenografts in mice in vivo with good pharmacokinetics (Tmax = 0.5 hr, T1/2 = 2.4 hr, AUC = 935 h·ng/mL; 10 mg/kg p.o.) and without overt toxicity to the animals. |
| RIDADR | NONH for all modes of transport |
| WGK Germany | WGK 3 |
| Flash Point(F) | Not applicable |
| Flash Point(C) | Not applicable |
| Purity | ≥98% (HPLC) |
| Storage Temp. | 2-8°C |
| UNSPSC | 12352200 |