Galunisertib (LY2157299)

This product is for research use only, not for human use. We do not sell to patients.

Galunisertib (LY2157299)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
500mg$550In Stock
1g$840In Stock
5g$2270In Stock

Cat #: V1360 CAS #: 700874-72-2 Purity ≥ 98%

Description: Galunisertib (formerly known as LY2157299; LY-2157299) is a selective, ATP-mimetic, and orally bioavailable small molecule inhibitor of the TGFβ receptor I (TβRI) with potential anticancer activity.

References: Bueno L, et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299, a new type I receptor TGF-beta kinase antagonist, in mice. Eur J Cancer. 2008 Jan;44(1):142-50.

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Molecular Weight (MW)369.42
Molecular FormulaC22H19N5O
CAS No.700874-72-2
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 74 mg/mL (200.3 mM)r
Water: <1 mg/mLr
Ethanol:<1 mg/mL
Solubility In Vivo2% DMSO+30% PEG 300+ddH2O: 5 mg/mL
SynonymsLY2157299; LY2157299; LY 2157299 SMILES Code: O=C(C1=CC=C2N=CC=C(C3=C(CCC4)N4N=C3C5=NC(C)=CC=C5)C2=C1)N Chemical Name: 4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide
ProtocolIn VivoHuman xenografts Calu6 (non-small cell lung cancer) and MX1 (breast cancer) are implanted subcutaneously in nude mice. After oral administration of 75 mg/kg, Galunisertib (LY2157299) induces a 70% decrease in pSmad for both types of cell lines. The time at which pSmad recovered 80% of baseline is approximately 6 h after administration
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
1mM2.7069 mL13.5347 mL27.0695 mL54.1389 mL
5mM0.5414 mL2.7069 mL5.4139 mL10.8278 mL
10mM0.2707 mL1.3535 mL2.7069 mL5.4139 mL
20mM0.1353 mL0.6767 mL1.3535 mL2.7069 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.