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JND4135, 一种II型TRK抑制剂,对TRKA, TRKB, TRKC的IC50值分别为2.79, 3.19 和3.01 nM。该化合物能有效克服BaF3稳定模型中的TRKxDFG以及其他突变体的抗性,抑制TRKs WT与xDFG突变和其下游信号分子的磷酸化。此外,JND4135能诱导BaF3–CD74-TRKA-G667C细胞G0/G1期阻滞及细胞凋亡 (apoptosis),并在BaF3-CD74-TRKA-G667C小鼠异种移植模型中展示了抑制肿瘤生长的活性。
JND4135, 一种II型TRK抑制剂,对TRKA, TRKB, TRKC的IC50值分别为2.79, 3.19 和3.01 nM。该化合物能有效克服BaF3稳定模型中的TRKxDFG以及其他突变体的抗性,抑制TRKs WT与xDFG突变和其下游信号分子的磷酸化。此外,JND4135能诱导BaF3–CD74-TRKA-G667C细胞G0/G1期阻滞及细胞凋亡 (apoptosis),并在BaF3-CD74-TRKA-G667C小鼠异种移植模型中展示了抑制肿瘤生长的活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 10-14周 | |
50 mg | 询价 | 10-14周 |
产品描述 | JND4135, a type II TRK inhibitor, exhibits IC50 values targeting TRKA, TRKB, and TRKC at 2.79, 3.19, and 3.01 nM, respectively. It can overcome resistance due to TRKxDFG and other mutations in the BaF3 stable model, inhibiting the phosphorylation of TRKs WT, xDFG mutations, and their downstream signaling molecules. Additionally, JND4135 induces G0/G1 phase arrest and cell apoptosis (apoptosis) in BaF3–CD74-TRKA-G667C cells. This compound also demonstrates antitumor activity in a BaF3-CD74-TRKA-G667C mouse xenograft model by suppressing tumor growth. |
分子量 | 597.75 |
分子式 | C37H39N7O |
CAS No. | 2366216-76-2 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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