Chemical Structure : SOMCL-286
CAS No.:
2126751-06-0
SOMCL-286
(SOMCL286 )
Catalog No.: PC-26356Not For Human Use, Lab Use Only.
SOMCL-286 (Compound 25a) is a highly potent dual FGFR/VEGFR inhibitor with IC50 of 1.0 nM against FGFR1, shows nearly equally high potency against FGFR1, FGFR2 and VEGFR-2 with IC50 values of 1.0, 4.5 and 2.9 nM, respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
SOMCL-286 (Compound 25a) is a highly potent dual FGFR/VEGFR inhibitor with IC50 of 1.0 nM against FGFR1, shows nearly equally high potency against FGFR1, FGFR2 and VEGFR-2 with IC50 values of 1.0, 4.5 and 2.9 nM, respectively.
SOMCL-286 has <0.5 nM against the FGFR1-positive KG-1cancer cell.
SOMCL-286 inhibited the proliferation of BAF3/VEGFR2 cell lines with an IC50 less than 1.5 nM.
SOMCL-286 demonstrated greater antiproliferative effects in all these FGFR1-3 subtype-selective cell lines than AZD4547, including FGFR1-amplified H1581 cells, FGFR1-translocated KG1 cells, FGFR2-amplified SNU-16 cells, FGFR3-amplified RT112 cells and FGFR3-mutated UMUC14 cells.
SOMCL-286 suppressed tumor growth in a dose-dependent manner, with tumor growth inhibition rate (TGI) of 25.0% and 81.0% at doses of 10 mg/kg and 50 mg/kg (i.p.), respectively, in SNU-16 xenograft models.
Physicochemical Properties
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M.Wt
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495.58
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Formula
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C29H29N5O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-methyl-6-((2-(4-(4-methylpiperazin-1-yl)benzamido)pyridin-4-yl)oxy)-1-naphthamide
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References
1. Manman Wei, et al. Eur J Med Chem. 2018 Jun 25:154:9-28.
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