DDR1-IN-1

A selective discoidin domain receptor 1 inhibitor

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库存: 现货

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5mg

￥1037.00

830.00

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10mg

￥1637.00

1310.00

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50mg

￥7337.00

5870.00

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100mg

￥11875.00

9500.00

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货号: ajci18972
CAS: 1449685-96-4
别名: N-[3-[(2,3-二氢-2-氧代-1H-吲哚-5-基)氧基]-4-甲基苯基]-4-[(4-乙基-1-哌嗪基)甲基]-3-(三氟甲基)苯甲酰胺
分子式: C30H31F3N4O3
分子量: 552.59
纯度: >98%
溶解度: Soluble in DMSO
储存: Store at -20°C
库存: 现货

Background

DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM)[1].

DDR1-IN-1 effectively blocks collagen-induced DDR1 pY513 autophosphorylation in U2OS cells (EC50 = 86.76 nM) with excellent selectivity over a panel of >380 kinases. DDR1-IN-1 inhibits DDR2-mediated MT1-MMP activation in human rheumatoid synovial fibroblasts (RASF) upon collagen stimulation (IC50 < 2.5 μM) and enhances PI3K/mTOR inhibitor GSK2126458 antiproliferation efficacy in SNU-1040 colorectal cancer culture[1].

参考文献:
[1]. Kim HG, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18;8(10):2145-50.