1. TGF-beta/Smad
  2. TGF-β Receptor

LY2157299 (Synonyms: Galunisertib; LY-2157299; LY 2157299)

Cat. No.: HY-13226 Purity: 99.88%
Handling Instructions

LY2157299 is a selective TGF-βR inhibitor with IC50 of 56 nM.

For research use only. We do not sell to patients.
LY2157299 Chemical Structure

LY2157299 Chemical Structure

CAS No. : 700874-72-2

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $109 In-stock
5 mg $99 In-stock
10 mg $135 In-stock
50 mg $405 In-stock
100 mg $750 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

LY2157299 is a selective TGF-βR inhibitor with IC50 of 56 nM.

IC50 & Target

IC50: 56 nM (TGF-βR)[1]

In Vitro

LY2157299 (Galunisertib) is a selective ATP-mimetic inhibitor of TGF-β receptor (TβR)-I activation LY2157299 (0.1, 1, 10, and 100 μM) displays a slight dose-dependent potentiation of Sorafenib 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, LY2157299 (Galunisertib) 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
Sponsor Condition Start Date Phase
Eli Lilly & Co Hepatocellular carcinoma 2011-03-31 Phase 2
Eli Lilly & Co Glioma 2011-04-30 Phase 2
Eli Lilly & Co 2013-10-31 Phase 1
Eli Lilly & Co 2013-01-31 Phase 1
Eli Lilly & Co Advanced solid tumor 2012-11-30 Phase 1
References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Cell Assay
[2]

LY2157299 (Galunisertib) is dissolved in stock solutions, and then diluted with appropriate media before use[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 and LY2157299 (0.1, 1, 10, and 10 μM)-treated group[2].

Animal Administration
[3]

LY2157299 (Galunisertib) is prepared in saline (Mice)[3].

Mice[3]
Charles River nude mice (weight 25 mg) are used. 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, 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.

References
M.Wt

369.42

Formula

C₂₂H₁₉N₅O

CAS No.

700874-72-2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 47 mg/mL

Purity: 99.88%

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Product Name:
LY2157299
Cat. No.:
HY-13226
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