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My CartCAS：700874-72-2
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to yellow Solid
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| CAS | 700874-72-2 |
| Name | Galunisertib |
| Molecular Formula | C22H19N5O |
| Molecular Weight | 369.42 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00001881 |
| SMILES | CC1=CC=CC(C2=NN3C(CCC3)=C2C4=CC=NC5=C4C=C(C=C5)C(N)=O)=N1 |
| InChIKey | IVRXNBXKWIJUQB-UHFFFAOYSA-N |
| InChI | InChI=1S/C22H19N5O/c1-13-4-2-5-18(25-13)21-20(19-6-3-11-27(19)26-21)15-9-10-24-17-8-7-14(22(23)28)12-16(15)17/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,23,28) |
| PubChem CID | 10090485 |
| Target Point | TGF-β Receptor |
| Passage | TGF-beta/Smad |
| Background | Galunisertib/LY2157299 is a selective TGF-β receptor inhibitor. |
| Biological Activity | Galunisertib 是一种选择性的 TGF-β 受体抑制剂，IC50 为 56 nM[1]。 |
| IC50 | 56nM(TGF-βR)[1] |
| In Vitro | Galunisertib(0.1，1，10和100μM)显示在SK-Sora，HepG2中的轻微剂量依赖性增强[2]。 |
| In Vivo | 将人异种移植物Calu6(非小细胞肺癌)和MX1(乳腺癌)皮下植入裸鼠中。在口服施用75mg/kg后，Galunisertib诱导两种类型细胞系的pSmad降低70％。 pSmad恢复80％基线的时间约为给药后6小时[3]。 |
| Cell Experiment | 使用MTT测定确定细胞存活。具有未处理细胞的孔或含有不含细胞的含药物培养基分别用作阳性和阴性对照。对于增殖测定，每天进行MTT测定以确定未处理对照和Galunisertib(0.1，1，10和10μM)处理组中的活细胞数[2]。 |
| Animal Experiment | 使用小鼠[3] Charles River裸鼠(体重25mg)。 Galunisertib以单剂量或多剂量设计口服给药。以单剂量方式给予的剂量水平的值是10(n = 3)，30(n = 8)，50(n = 26)，75(n = 69)，100(n = 3)，150(n = 21)和300(n = 3)mg/kg。在以下时间处死动物：给药后0.5，1，1.5，2，4，8和16小时，然后除去肿瘤并回收血液。在多次给药研究中，Galunisertib每天两次(bid)以75mg/kg的剂量每12小时施用，连续20天给予31只小鼠。在第10，15，20和25天最后一次给药后2小时处死动物，取出肿瘤用于pSmad测定，并回收血液以测定血浆中的药物水平。 |
| Data Literature Source | [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 inhibition with galunisertib (LY2157299) in hepatocellular carcinoma models and in ex vivo whole tumor tissue samples from patients. Oncotarget. 2015 Aug 28;6(25):21614-27 [3]. Bueno L，et al. Semi-mechanistic modelling of the tumour growth inhibitory effects of LY2157299，a new type I receptor TGF-beta kinase antagonist，in mice. Eur J Cancer. 2008 Jan;44(1):142-50. |
| Unit | Bottle |
| Specification | 5mg 10mg 50mg |
是一种选择性的 TGF-β 受体抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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