| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G407839-1ml |
1ml |
现货  |
|
| 英文别名 | 4-(2-(6-methylpyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl)quinoline-6-carboxamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Galunisertib (LY2157299) |
| 生化机理 | Galunisertib (LY2157299) 是一种强效的 TGFβ 受体 I (TβRI) 抑制剂，在无细胞试验中的 IC50 值为 56 nM。2/3 期 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | TGF-beta 受体 I 型抑制剂 |
| 产品介绍 |
LY2157299是有效的TGFβ receptor I (TβRI)抑制剂，IC50为56 nM。Phase 2/3。A potent TGF beta RI inhibitor. Information Galunisertib (LY2157299) is a potentTGFβ receptor I (TβRI)inhibitor withIC50of 56 nM in a cell-free assay. Phase 2/3. LY2157299 potently inhibits the TGFβ receptor signaling. LY2157299 abolishes the TGFβ induced Smad2 phosphorylation in HUVEC cells. LY2157299 also shows dose dependent potentiation of VEGF or bFGF induced cell proliferation in HUVEC. LY2157299 also promotes VEGF induced HUVEC cell migration. LY2157299 potentiates angiogenesis in the in vitro VEGF-stimulated cord formation assay. LY2157299 inhibits TGF-β-mediated SMAD2 activation and hematopoietic suppression in primary hematopoietic stem cells in a dose-dependent manner. LY2157199 treatment stimulates hematopoiesis from primary MDS bone marrow specimens. In human glioblastoma (GBM) cells, LY2157299 treatment blocks signaling through the heteromeric TGFβ receptor complex to reduce levels of active, phosphorylated SMAD. In vivo Although anti-tumor activity has been observed in several pre-clinical models, LY2157299 fails to show significant in vivo angiogenic effects in the 4T1, Colo205, or A549 xenograft models. Administration of LY2157299 ameliorates anemia in a TGF-β overexpressing transgenic mouse model of bone marrow failure. Oral administration of LY2157299 at 75 mg/kg/day displays significant antitumor activity against both Calu6 and MX1 xenografts in mice. In vivo, LY2157299 induces angiogenesis and enhances VEGF and basic-fibroblast-growth-factor-induced angiogenesis in a Matrigel-plug assay, whereas adding an alpha5-integrin-neutralizing antibody to the Matrigel selectively inhibits this enhanced response. cell lines：MEF cells Concentrations： Incubation Time： Powder Purity:≥99% |
| ALogP | 2.4 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CC1=NC(=CC=C1)C2=NN3CCCC3=C2C4=C5C=C(C=CC5=NC=C4)C(=O)N |
| 分子量 | 369.42 |
| Reaxy-Rn | 14275134 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=14275134&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 47 mg/mL (197.31 mM); Ethanol: -1 mg/mL |
|---|
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