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SILA-123

Chemical Structure : SILA-123

CAS No.: 2911585-37-8

SILA-123 (SILA123)

Catalog No.: PC-23628Not For Human Use, Lab Use Only.

SILA-123 (SILA123) is a potent, selective type II FLT3 inhibitor with IC50 of 2.1 nM and 1.0 nM for FLT3-WT and FLT3-ITD respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SILA-123 (SILA123) is a potent, selective type II FLT3 inhibitor with IC50 of 2.1 nM and 1.0 nM for FLT3-WT and FLT3-ITD respectively.
SILA-123 exhibits promising kinome selectivity against 310 kinases (S score (10) = 0.06).
SILA-123 potently inhibits tumor cells with the FLT3-ITD mutant such as MOLM-13 (IC50 = 0.98 nM) and MV4-11 (IC50 = 0.19 nM), as well as BaF3 cells associated with the FLT3-ITD mutant and point mutations like BaF3-FLT3-ITD-G697R (IC50 = 3.0 nM).
SILA-123 significantly suppressed the tumor growth in MV4-11 (50 mg/kg/d, TGI = 87.3%) and BaF3-FLT3-ITD-G697R (50 mg/kg/d, TGI = 60.0%) cell-inoculated allograft models.

Physicochemical Properties

M.Wt 415.50
Formula C24H25N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(4-(3-Amino-6-methylisoxazolo[5,4-b]pyridin-4-yl)phenyl)-3-(4-(tert-butyl)phenyl)urea

References

1. Wei TH, et al. J Med Chem. 2024 Sep 11. doi: 10.1021/acs.jmedchem.4c00529.

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