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Nintedanib (Vargatef; BIBF 1120)

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Nintedanib (Vargatef; BIBF 1120)
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Size Price Stock
1g$390Check With Us
2g$650Check With Us
5g$1095Check With Us

Cat #: V0530 CAS #: 656247-17-5 Purity ≥ 98%

Description: Nintedanib (formerly BIBF-1120; trade name: Vargatef) is an orally bioavailable multi-kinase inhibitor with potential antineoplastic and anti-fibrotic activity.

References: Hilberg F, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res, 2008, 68(12), 4774-4782.

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Molecular Weight (MW)539.62
Molecular FormulaC31H33N5O4
CAS No.656247-17-5
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 6 mg/mL (11.11mM)r
Water:<1 mg/mLr
Ethanol: 3 mg/mL (5.6 mM)
Solubility In Vivo30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
SMILES CodeO=C(C1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(N(C)C(CN4CCN(C)CC4)=O)C=C3)/C5=CC=CC=C5)OC
SynonymsNintedanib; BIBF-1120; Intedanib, BIBF 1120; BIBF1120;trade name: Vargatef.
ProtocolIn VitroNintedanib (BIBF 1120) binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain. Nintedanib (BIBF 1120) inhibits proliferation of PDGF-BB stimulated BRPs with EC50 of 79 nM in cell assays. Nintedanib (BIBF 1120) (100 nM) blocks activation of MAPK after stimulation with 5% serum plus PDGF-BB. Nintedanib (BIBF 1120) prevents PDGF-BB stimulated proliferation with an EC50 of 69 nM in cultures of human vascular smooth muscle cells (HUASMC).
In VivoNintedanib (BIBF 1120) (25-100 mg/kg daily p.o.) is highly active in all tumor models, including human tumor xenografts growing in nude mice and a syngeneic rat tumor model. This is evident in the magnetic resonance imaging of tumor perfusion after 3 days, reducing vessel density and vessel integrity after 5 days, and profound growth inhibition.
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
1mM1.8532 mL9.2658 mL18.5316 mL37.0631 mL
5mM0.3706 mL1.8532 mL3.7063 mL7.4126 mL
10mM0.1853 mL0.9266 mL1.8532 mL3.7063 mL
20mM0.0927 mL0.4633 mL0.9266 mL1.8532 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.