Galunisertib (Synonyms: LY2157299) 纯度: 99.84%
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。
Galunisertib Chemical Structure
CAS No. : 700874-72-2
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥610 | In-stock | |
2 mg | ¥500 | In-stock | |
5 mg | ¥750 | In-stock | |
10 mg | ¥1100 | In-stock | |
50 mg | ¥3500 | In-stock | |
100 mg | ¥6300 | In-stock | |
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Galunisertib 相关产品
•相关化合物库:
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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. |
IC50 & Target |
IC50: 56 nM (TGF-βRI)[4] |
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体外研究 (In Vitro) |
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[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (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, 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[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
369.42 |
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Formula |
C22H19N5O |
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CAS 号 |
700874-72-2 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 100 mg/mL (270.69 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [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 andGalunisertib (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. |
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Animal Administration [3] |
Mice[3] MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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