1. TGF-beta/Smad
  2. TGF-β Receptor

LY2157299 (Synonyms: Galunisertib)

Cat. No.: HY-13226 Purity: 99.88%
Data Sheet SDS 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 (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $88 In-stock
5 mg $80 In-stock
10 mg $110 In-stock
50 mg $350 In-stock
100 mg $550 In-stock
200 mg $850 In-stock
500 mg $1250 In-stock
1 g   Get quote  
5 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Featured Recommendations

  • 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
NCT Number Sponsor Condition Start Date Phase
NCT02752919 Eli Lilly and Company Healthy April 2016 Phase 1
NCT02304419 Eli Lilly and Company Neoplasm May 2015 Phase 1
NCT02734160 Eli Lilly and Company|AstraZeneca Metastatic Pancreatic Cancer June 2016 Phase 1
NCT02423343 Eli Lilly and Company|Bristol-Myers Squibb Solid Tumor|Non-Small Cell Lung Cancer Recurrent|Hepatocellular Carcinoma Recurrent October 2015 Phase 1|Phase 2
NCT02906397 University of Pennsylvania ADVANCED HEPATOCELLULAR CARCINOMA (HCC) March 30, 2017 Phase 1
NCT02672475 Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma March 2016 Phase 1
NCT03206177 University of Oklahoma|Eli Lilly and Company Carcinosarcoma, Ovarian July 31, 2017 Phase 1
NCT02981342 Eli Lilly and Company Pancreatic Ductal Adenocarcinoma January 2017 Phase 2
NCT02240433 Eli Lilly and Company Hepatocellular Carcinoma November 2014 Phase 1
NCT01722825 Eli Lilly and Company Neoplasms|Neoplasm Metastasis November 2012 Phase 1
NCT01965808 Eli Lilly and Company Healthy Volunteers October 2013 Phase 1
NCT02154646 Eli Lilly and Company Pancreatic Neoplasms May 2014 Phase 1
NCT01746004 Eli Lilly and Company Healthy Volunteers January 2013 Phase 1
NCT02452008 Sidney Kimmel Comprehensive Cancer Center Prostate Cancer April 2016 Phase 2
NCT02688712 Providence Health & Services|Eli Lilly and Company Rectal Adenocarcinoma June 2016 Phase 2
NCT02008318 Eli Lilly and Company Myelodysplastic Syndromes March 2014 Phase 2|Phase 3
NCT02178358 Eli Lilly and Company Hepatocellular Carcinoma August 2014 Phase 2
NCT01582269 Eli Lilly and Company Glioblastoma April 2012 Phase 2
NCT01220271 Eli Lilly and Company Glioma April 2011 Phase 1|Phase 2
NCT01246986 Eli Lilly and Company Carcinoma, Hepatocellular March 2011 Phase 2
NCT01682187 Eli Lilly and Company Glioma December 2005 Phase 1
NCT01373164 Eli Lilly and Company Neoplasms|Neoplasm Metastasis|Pancreatic Cancer June 2011 Phase 1|Phase 2
View MoreCollapse
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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

References
Molecular Weight

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

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.88%

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

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