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别名 MYF03-176, MYF-03176, MYF03176
MYF-03-176 is an orally active TEAD1/3/4 inhibitor with IC₅₀ values of 47/32/71 nM, respectively. It also inhibits TEAD transcriptional activity and cell growth in NCI-H226 cells, exhibiting antitumour activity in malignant pleural mesothelioma (MPM) cells with defective Hippo signalling and in mouse xenograft models.

MYF-03-176 is an orally active TEAD1/3/4 inhibitor with IC₅₀ values of 47/32/71 nM, respectively. It also inhibits TEAD transcriptional activity and cell growth in NCI-H226 cells, exhibiting antitumour activity in malignant pleural mesothelioma (MPM) cells with defective Hippo signalling and in mouse xenograft models.
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 928 | 现货 | |
| 5 mg | ¥ 2,799 | 现货 |
MYF-03-176 相关产品
| 产品描述 | MYF-03-176 是一种具有口服活性的TEAD1/3/4抑制剂,IC50分别为47/32/71nM,还能够在NCI-H226细胞中抑制TEAD转录活性和细胞生长,在hippo信号传导缺陷的恶性胸膜间皮瘤(MPM)细胞和小鼠异种移植模型中具有抗肿瘤活性。 |
| 靶点活性 | TEAD4:71 nM, TEAD2:275 nM, TEAD3:32 nM, TEAD1:47 nM |
| 体外活性 | MYF-03-176 (0.1-10⁵ nM)作用 NCI-H226 细胞 72 小时,可抑制 TEAD 转录活性,其IC₅₀为 11 nM [1]。 |
| 体内活性 | 在人类间皮瘤 NCI-H226 细胞衍生异种移植(CDX)模型中,MYF-03-176 以 30-75 mg/kg 的剂量口服给药,每日两次、持续 28 天,展现出强效的抗肿瘤活性 [1]。 |
| 别名 | MYF03-176, MYF-03176, MYF03176 |
| 分子量 | 410.37 |
| 分子式 | C19H18F4N4O2 |
| CAS No. | 2857937-59-6 |
| Smiles | O(CC1=CC=C(C(F)(F)F)C=C1)[C@H]2[C@H](NC=3N=CC=CN3)CN(C(C(=C)F)=O)C2 |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 80 mg/mL (194.95 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+90% Corn Oil: 3.3 mg/mL (8.04 mM), Sonication is recommeded. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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