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Dovitinib (TKI258; CHIR-258 ) Lactate

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Dovitinib (TKI258; CHIR-258 ) Lactate
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500mg$900Check With Us
1g$1450Check With Us
5g$3670Check With Us

Cat #: V0498 CAS #: 915769-50-5 Purity ≥ 98%

Description: Dovitinib Lactate (formerly TKI-258 lactate; CHIR-258 lactate), a benzimidazole-quinolinone analog, is a potent, orally bioavailable and multitargeted RTK inhibitor with potential antineoplastic activity.

References: Trudel S, et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 2005, 105(7), 2941-2948.

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Molecular Weight (MW)482.51
Molecular FormulaC24H27FN6O4
CAS No.915769-50-5
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 100 mg/mL (207.2 mM)r
Water: 66 mg/mL warmed (136.7 mM)r
Ethanol: 1 mg/mL warmed (2.1 mM)
SMILES CodeO=C1NC2=C(C(F)=CC=C2)C(N)=C1C3=NC4=CC=C(N5CCN(C)CC5)C=C4N3.CC(O)C(O)=O
SynonymsCHIR 258; TKI258; TKI-258; CHIR-258; CHIR258; TKI 258; Dovitinib lactate
ProtocolIn VitroDovitinib (100 nM) augments Dexamethasone (0.5 μM) cytotoxicity in KMS11 cells. Dovitinib (72 hours) inhibits cell proliferation of KMS11 (FGFR3-Y373C), OPM2 (FGFR3-K650E), and KMS18 (FGFR3-G384D) cells with IC50 of values of 90 nM (KMS11 and OPM2) and 550 nM, respectively. Dovitinib (100, 500 nM; 96 hours) inhibits FGF-mediated ERK1/2 phosphorylation and induces apoptosis of FGFR3-expressing human myeloma cell lines. μM), Tie2 (IC50=4 μM), IGFR1 (IC50>10 μM), and HER2 (IC50>10 μM)[1]. Dovitinib (12.5-400 nM; 48 hours) potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50 values of 25 nM. Dovitinib (CHIR-258) shows more than 10-fold inhibition InsR (IC50=2 μM), EGFR1 (IC50=2 μM), c-Met (IC50>3 μM), EphrinA2 (EphA2; IC50=4 μM), Tie2 (IC50=4 μM), IGFR1 (IC50>10 μM), and HER2 (IC50>10 μM)
In VivoDovitinib (CHIR-258; 10-60 mg/kg/day; gavage; for 21 days) has a significant antitumor effect.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.0725 mL10.3625 mL20.7250 mL41.4499 mL
5mM0.4145 mL2.0725 mL4.1450 mL8.2900 mL
10mM0.2072 mL1.0362 mL2.0725 mL4.1450 mL
20mM0.1036 mL0.5181 mL1.0362 mL2.0725 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
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.
  • (2) Be sure to add the solvent(s) in order.