SU14813 maleate
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
100mg | $450 | Check With Us |
200mg | $675 | Check With Us |
500mg | $1140 | Check With Us |
Cat #: V29102 CAS #: 849643-15-8 Purity ≥ 99%
Description: SU14813 maleate is a novel, orally bioavailable, multi-targeted tyrosine kinase inhibitor (TKI) with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT, respectively.
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Molecular Weight (MW) | 558.56 |
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Molecular Formula | C27H31FN4O8 |
CAS No. | 849643-15-8 |
SMILES Code | O=C(NC[C@@H](CN1CCOCC1)O)C2=C(NC(/C=C3C(NC4=C\3C=C(C=C4)F)=O)=C2C)C.O=C(/C=C\C(O)=O)O |
Synonyms | SU14813 maleate; SU 14813; SU-14813; SU014813; SU-014813; SU 014813 |
Protocol | In Vitro | SU14813 inhibits ligand-dependent and ligand-independent proliferation, migration, and survival of endothelial cells and/or tumor cells expressing these targets. SU14813 inhibits cellular ligand-dependent phosphorylation of VEGFR-2 (transfected NIH 3T3 cells), PDGFR-β (transfected NIH 3T3 cells), KIT (Mo7e cells), and FLT3-internal tandem duplication (FLT3-ITD; MV4;11 cells) as well as FMS/CSF1R (transfected NIH 3T3 cells). SU14813 inhibits VEGFR-2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells overexpressing these targets, with cellular IC50 values of 5.2, 9.9, and 11.2 nM, respectively. SU14813 inhibits the growth of U-118MG with an IC50 of 50 to 100 nM. |
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In Vivo | SU14813 inhibits VEGFR-2, PDGFR-β, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent fashion. The plasma concentration required for in vivo target inhibition is estimated to be 100 to 200 ng/mL. Used as monotherapy, SU14813 exhibits broad and potent antitumor activity resulting in regression, growth arrest, or substantially reduced growth of various established xenografts derived from human or rat tumor cell lines. Treatment in combination with docetaxel significantly enhances both the inhibition of primary tumor growth and the survival of the tumor-bearing mice compared with administration of either agent alone. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.7903 mL | 8.9516 mL | 17.9032 mL | 35.8064 mL |
5mM | 0.3581 mL | 1.7903 mL | 3.5806 mL | 7.1613 mL |
10mM | 0.1790 mL | 0.8952 mL | 1.7903 mL | 3.5806 mL |
20mM | 0.0895 mL | 0.4476 mL | 0.8952 mL | 1.7903 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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