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抑制剂/激活剂

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凋亡与自噬

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Galunisertib LY2157299

Galunisertib (LY2157299) 是一种选择性的 TGF-β 受体 I 型 (TGF-βRI) 激酶抑制剂，IC50 为 56 nM。

货号：
TK0493
规格：

1mg

2mg

5mg

10mg

25mg
价格：
￥0.00

产品参数

CAS No.	700874-72-2
生物活性	Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
分子式	C22H19N5O
分子量	369.42
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : 100 mg/mL (270.69 mM; Need ultrasonic)
体内研究	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, Galunisertib (LY2157299) 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.
体外研究	Galunisertib (LY2157299) (0.1, 1, 10, and 100 μM) displays a slight dose-dependent potentiation of Bay 43-9006 in SK-Sora, HepG2, and Hep3B cell lines but not in JHH6, SK-HEP1, and HuH7 cell lines.
文献	•Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •OncoImmunology. 2020 Sep 22;9(1):1824631. •Cell Oncol. 2021 Feb;44(1):193-204. •Cells. 2022, 11(2), 237. •Breast Cancer Res. 2019 Nov 21;21(1):123. •Breast Cancer Res. 2019 Nov 21;21(1):123. •J Cell Physiol. 2019 Jul;234(7):10554-10565. •J Nutr Biochem. 2021 Jan;87:108518. •Front Pharmacol. 2021 Apr 30;12:644886. •J Cell Mol Med. 2020 Mar;24(6):3656-3668. •Bioorg Chem. 2021, 105222. •Liver Int. 2021 Mar 31. •J Immunol Res. 2018 Sep 3;2018:6248590. •J Tissue Eng Regen Med. 2021 Aug 7. •Int J Parasitol. 2018 Nov;48(13):1023-1033. •Brain Sci. 2019 Dec 30;10(1):20. •Pathol Oncol Res. 2021 Nov 19;27:1609997. •Evid-Based Compl Alt. 2021 Feb 12. •Int J Clin Exp Med. 2020;13(2):396-406. •Programa de Doctorado en Biomedicina. 2020 Sep. •bioRxiv. 2020 Apr.
纯度及产品资料	98%

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