1. TGF-beta/Smad
  2. TGF-β Receptor
  3. Galunisertib

Galunisertib (Synonyms: LY2157299)

Cat. No.: HY-13226 Purity: 99.95%
Handling Instructions

Galunisertib (LY2157299) is a oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.

For research use only. We do not sell to patients.

Galunisertib Chemical Structure

Galunisertib Chemical Structure

CAS No. : 700874-72-2

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 70 In-stock
Estimated Time of Arrival: December 31
50 mg USD 150 In-stock
Estimated Time of Arrival: December 31
100 mg USD 250 In-stock
Estimated Time of Arrival: December 31
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Based on 10 publication(s) in Google Scholar

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Description

Galunisertib (LY2157299) is a oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.

IC50 & Target

IC50: 56 nM (TGF-βRI)[4]

In Vitro

Galunisertib (LY2157299) (0.1, 1, 10, and 100 μM) displays a slight dose-dependent potentiation of Bay 43-9006 in SK-Sora, HepG2, and Hep3B cell lines but not in JHH6, SK-HEP1, and HuH7 cell lines[2].

In Vivo

Human 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[3].

Clinical Trial
Molecular Weight

369.42

Formula

C₂₂H₁₉N₅O

CAS No.

700874-72-2

SMILES

CC1=CC=CC(C2=NN3C(CCC3)=C2C4=CC=NC5=C4C=C(C=C5)C(N)=O)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (270.69 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7069 mL 13.5347 mL 27.0695 mL
5 mM 0.5414 mL 2.7069 mL 5.4139 mL
10 mM 0.2707 mL 1.3535 mL 2.7069 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

Cell survival is determined using the MTT assay. The conversion of yellow water-soluble tetrazolium MTT into purple insoluble formazan is catalyzed by mitochondrial dehydrogenases and used to estimate the number of viable cells. In brief, cells are seeded in 96-well tissue culture plates at a density of 2×103 cells/well. After drug exposure, cells are incubated with 0.4 mg/mL MTT for 4 hours at 37°C. After incubation, the supernatant is discarded, insoluble formazan precipitates are dissolved in 0.1 mL of DMSO, and the absorbance is measured at 560 nm by use of a microplate reader. Wells with untreated cells or with drug-containing medium without cells are used as positive and negative controls respectively. For proliferation assay, MTT assay is done daily to determine the number of viable cells in untreated control andGalunisertib (LY2157299) (0.1, 1, 10, and 10 μM)-treated group[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Mice[3]
Charles River nude mice (weight 25 mg) are used. Galunisertib (LY2157299) is given orally as a single dose or in a multiple dosing design. The value of the dose levels given in a single dose manner is 10 (n=3), 30 (n=8), 50 (n=26), 75 (n=69), 100 (n=3), 150 (n=21) and 300 (n=3) mg/kg. Animals are sacrificed at the following times: 0.5, 1, 1.5, 2, 4, 8 and 16 h after administration, then the tumor is removed and blood is recovered. In the multiple dosing study, Galunisertib (LY2157299) is administered twice a day (bid) at the dose of 75 mg/kg every 12 h for 20 consecutive days to 31 mice. Animals are sacrificed at 2 h after the last administration at days 10, 15, 20 and 25, and the tumor is removed for pSmad determination and the blood is recovered for determination of drug levels in plasma.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.95%

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Keywords:

GalunisertibLY2157299LY 2157299LY-2157299TGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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