产品
编 号：F238638
分子式：C21H18N2O5S
分子量：410.44
分子式：C21H18N2O5S
分子量：410.44
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1913291-02-7
产品详情
生物活性：
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice.
体内研究：
WRG-28 (10 mg/kg；iv；单次) 在体内减弱乳腺肿瘤中 DDR2 的生化信号。 WRG-28 (10 mg/kg；iv；单次) 每天一次，持续 7 天) 减少乳腺肿瘤细胞的转移性肺定植。 WRG-28 (10 mg/kg；静脉注射；每天一次，持续 21 天) 减少炎症反应胶原抗体诱导的关节炎 (CAIA) 小鼠的关节破坏。Animal Model:Female BALB/cJ mice (8-week-old; 4T1-Snail-CBG tumor-bearing mice model).
Dosage:10 mg/kg
Administration:Intravenous injection, single.
Result:Reduced 60% SNAIL1-clic beetle green (SNAIL1.CBG) level within the tumor in mice.
Animal Model:Female BALB/cJ mice (8-week-old; injected with 4T1 GFP-luc expressing cells).
Dosage:10 mg/kg
Administration:Intravenous injection, single daily for 7 days.
Result:Reduced lung colonization to a level comparable to shDDR2-depleted cells.
Animal Model:Male DBA/1 mice (8-week-old; CAIA model).
Dosage:10 mg/kg
Administration:Intravenous injection, single daily for 21 days.
Result:Significantly ameliorated arthritis in the mice (reduced production of IL-15 and Dkk-1), the hind- paw thickness of the mice was also reduced.Inhibited inflammatory cell infiltration and destruction of cartilage in mouse ankle and serum. Significantly alleviated bone destruction, reduced the extent of joint space enlargement and bone mineral density, as well as decreased the severity of bone loss.
体外研究：
WRG-28 (1、2 μM；4 小时) 减弱胶原蛋白 I 介导的 DDR2 酪氨酸磷酸化和 (1 μM；7 小时) 在 HEK293 细胞 (表达 DDR2) 中的 ERK 激活和 SNAIL1 蛋白稳定性 (IC50=286 nM)。 WRG-28 (1 μM；48 小时) 通过抑制 BT549 和 4T1 乳腺癌细胞中的 DDR2 来抑制肿瘤细胞的侵袭和迁移。 WRG-28 (1 μM；4 天) 抑制 CAF 的促肿瘤作用。 WRG-28 (0.5，1 μM；4 h) 维持对 TKIs 耐药的获得性 DDR2 突变的抑制作用。
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice.
体内研究：
WRG-28 (10 mg/kg；iv；单次) 在体内减弱乳腺肿瘤中 DDR2 的生化信号。 WRG-28 (10 mg/kg；iv；单次) 每天一次，持续 7 天) 减少乳腺肿瘤细胞的转移性肺定植。 WRG-28 (10 mg/kg；静脉注射；每天一次，持续 21 天) 减少炎症反应胶原抗体诱导的关节炎 (CAIA) 小鼠的关节破坏。Animal Model:Female BALB/cJ mice (8-week-old; 4T1-Snail-CBG tumor-bearing mice model).
Dosage:10 mg/kg
Administration:Intravenous injection, single.
Result:Reduced 60% SNAIL1-clic beetle green (SNAIL1.CBG) level within the tumor in mice.
Animal Model:Female BALB/cJ mice (8-week-old; injected with 4T1 GFP-luc expressing cells).
Dosage:10 mg/kg
Administration:Intravenous injection, single daily for 7 days.
Result:Reduced lung colonization to a level comparable to shDDR2-depleted cells.
Animal Model:Male DBA/1 mice (8-week-old; CAIA model).
Dosage:10 mg/kg
Administration:Intravenous injection, single daily for 21 days.
Result:Significantly ameliorated arthritis in the mice (reduced production of IL-15 and Dkk-1), the hind- paw thickness of the mice was also reduced.Inhibited inflammatory cell infiltration and destruction of cartilage in mouse ankle and serum. Significantly alleviated bone destruction, reduced the extent of joint space enlargement and bone mineral density, as well as decreased the severity of bone loss.
体外研究：
WRG-28 (1、2 μM；4 小时) 减弱胶原蛋白 I 介导的 DDR2 酪氨酸磷酸化和 (1 μM；7 小时) 在 HEK293 细胞 (表达 DDR2) 中的 ERK 激活和 SNAIL1 蛋白稳定性 (IC50=286 nM)。 WRG-28 (1 μM；48 小时) 通过抑制 BT549 和 4T1 乳腺癌细胞中的 DDR2 来抑制肿瘤细胞的侵袭和迁移。 WRG-28 (1 μM；4 天) 抑制 CAF 的促肿瘤作用。 WRG-28 (0.5，1 μM；4 h) 维持对 TKIs 耐药的获得性 DDR2 突变的抑制作用。
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