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商品描述
LY2157299
- Catalog No.：MC0277
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo：
- 700874-72-2
- MolecularFormula：
- C22H19N5O
- Purity：
- >98%
- Target：
- TGF-β Receptor
- IC50：
- 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].
- Fields：
- LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2.
- Specificity：
- Target:TGF-β Receptor. Fields: LY2157299 is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM. Phase 2.
- Source：
- Rabbit
- Dilution：
- IC50: 56 nM (TGF-βR)[1]
- Concentration：
- >98%
- Storage Stability：
- 2 years -20°C powder,2 weeks 4°C in DMSO,6 months -80°C in DMSO
- Other Name：
- LY-2157299,LY 2157299
- MolecularWeight(Da)：
- 369.42
- References：
- [1]. Cong L, et al. Targeting the TGF-β receptor with kinase inhibitors for scleroderma therapy. Arch Pharm (Weinheim). 2014 Sep;347(9):609-15.[2]. Serova M, et al. Effects of TGF-beta signalling inh
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