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NCT-58是一种有效的C 端HSP90抑制剂。NCT-58不会引起热休克反应(HSR)。NCT-58通过同时下调HER 家族成员以及抑制Akt 磷酸化来激发抗肿瘤活性。NCT-58杀死对曲妥珠单抗耐药的乳腺癌干细胞样细胞。NCT-58诱导HER2阳性乳腺癌细胞凋亡。
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NCT-58是一种有效的C 端HSP90抑制剂。NCT-58不会引起热休克反应(HSR)。NCT-58通过同时下调HER 家族成员以及抑制Akt 磷酸化来激发抗肿瘤活性。NCT-58杀死对曲妥珠单抗耐药的乳腺癌干细胞样细胞。NCT-58诱导HER2阳性乳腺癌细胞凋亡。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 542 | 现货 | |
5 mg | ¥ 1,320 | 现货 | |
10 mg | ¥ 2,150 | 现货 | |
25 mg | ¥ 4,560 | 现货 | |
50 mg | ¥ 6,390 | 现货 | |
100 mg | ¥ 8,620 | 现货 | |
200 mg | ¥ 11,600 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 3,650 | 现货 |
产品描述 | NCT-58 is a potent C-terminal HSP90 inhibitor. NCT-58 does not induce the heat shock response (HSR). NCT-58 elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells. |
体外活性 | NCT-58处理(0.1-10 μM;72小时)在HER2阳性的BT474和SKBR3细胞中增加早期和晚期凋亡细胞的数量。NCT-58处理(0.1-20 μM;72小时)呈剂量依赖性地降低HER2阳性BT474和SKBR3细胞的活力。NCT-58处理(2-10 μM;72小时)有效降低了JIMT-1和MDA-MB-453细胞中截短的p95HER2及其磷酸化形式的水平,以及Akt和磷酸化Akt(Ser473)蛋白含量的下调[1]。 |
体内活性 | NCT-58(30 mg/kg;i.p.;每隔一天,共47天)显著抑制肿瘤生长,并显著减少肿瘤重量。NCT-58(30 mg/kg;i.p.;每隔一天,共47天)抑制Trastuzumab耐药性肿瘤生长[1]。 |
别名 | NCT58 |
分子量 | 466.57 |
分子式 | C27H34N2O5 |
CAS No. | 2411429-33-7 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 40 mg/mL (85. mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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