| 名称 | Navtemadlin |
| 描述 | Navtemadlin (AMG232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction (IC50: 0.6 nM). It binds to MDM2 with a Kd of 0.045 nM. |
| 细胞实验 | Cell Line: SJSA-1, HCT116, ACHN, NCI-H460, MOLM-13, RKO, MCF7, 22RV1, HT-29, PC-3, NCI-H82, NCI-SNU1, MG-63, NCI-H2452, SW982, C32, SK-HEP-1, A375, RT4, RPMI2650, MDA-MB-134-VI, NCI-H2347, and A427 cells. Concentration: 0-10 μM [1]. Incubation Time: 72 hours. |
| 动物实验 | Animal Model: Female athymic nude mice (n=10) based cancer models. Dosage: 10, 25, 75 mg/kg. Administration: Once daily by oral gavage [1]. |
| 体外活性 | 方法：Navtemadlin（0.1,1,10μM）处理B16-F10细胞，Navtemadlin 重新激活 p53 是否会诱导肿瘤生长停滞。
结果：Navtemadlin 在 B16-F10 细胞中诱导显著的 p53 依赖性生长停滞，但细胞凋亡很少。[1] |
| 体内活性 | 方法：Navtemadlin (AMG232)（20 mg / kg（ip））治疗B16-F10黑色素瘤肿瘤的C57Bl / 6小鼠，观察是否抑制小鼠体内肿瘤生长。
结果：从第3天开始每天给药Navtemadlin (AMG232)时，p53肿瘤大小减少了约30%-50%。[1]
方法：Navtemadlin (AMG232)（10、25、75 mg/kg，每日一次，口服）观察是否可以抑制小鼠肿瘤异种移植瘤的生长。
结果：Navtemadlin (AMG232)可激活体内 p53 通路活性，并有效抑制小鼠肿瘤异种移植瘤的生长。它还可阻断 DNA 合成并诱导体内细胞凋亡[2]。 |
| 存储条件 | Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.52 mM), Sonication is recommended.
H2O : Insoluble
DMSO : 150 mg/mL (263.83 mM), Sonication is recommended.
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| 关键字 | Ubiquitin ligase | Ubiquitin conjugating enzyme | Ubiquitin activating enzyme | p53-MDM2 | Navtemadlin | MDM-2/p53 | MDM2 | KRT-232 | KRT232 | KRT 232 | Inhibitor | inhibit | E3Enzyme | E3 ligating enzyme | E3 Enzyme | E2Enzyme | E2 Enzyme | E2 conjugating enzyme | E1Enzyme | E1/E2/E3 Enzyme | E1 Enzyme | E1 activating enzyme | CS1300 | CS 1300 | AMG-232 | AMG 232 |
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