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JHU395 is an orally-bioavailable prodrug of a lipophilic glutamine antagonist (GA), 6-diazo-5-oxo-L-norleucine (DON). It demonstrates delivery of DON to malignant peripheral nerve sheath tumor (MPNST) both in vitro and in vivo, resulting in significant antitumor activity in MPNST. Additionally, JHU395 exhibits plasma stability.
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JHU395 is an orally-bioavailable prodrug of a lipophilic glutamine antagonist (GA), 6-diazo-5-oxo-L-norleucine (DON). It demonstrates delivery of DON to malignant peripheral nerve sheath tumor (MPNST) both in vitro and in vivo, resulting in significant antitumor activity in MPNST. Additionally, JHU395 exhibits plasma stability.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 593 | 现货 | |
5 mg | ¥ 1,490 | 现货 | |
10 mg | ¥ 2,570 | 现货 | |
25 mg | ¥ 4,890 | 现货 | |
50 mg | ¥ 6,780 | 现货 | |
100 mg | ¥ 9,130 | 现货 | |
200 mg | ¥ 12,300 | 现货 |
产品描述 | JHU395 is an orally-bioavailable prodrug of a lipophilic glutamine antagonist (GA), 6-diazo-5-oxo-L-norleucine (DON). It demonstrates delivery of DON to malignant peripheral nerve sheath tumor (MPNST) both in vitro and in vivo, resulting in significant antitumor activity in MPNST. Additionally, JHU395 exhibits plasma stability. |
体外活性 | JHU395(1、10、100 μmol/L)通过抑制(MPNST)肿瘤细胞多种生物合成过程的生长,而对于永生的施万细胞的生长影响微乎其微。在人MPNST细胞中,JHU395诱导的PARP裂解作为细胞凋亡标志物相对较少。JHU395是一种在血浆中稳定的亲脂性GA前药,能够通过体外血浆至肿瘤细胞隔离测定实验[1]将DON传递至MPNST。 |
体内活性 | JHU395(口腔灌胃;1.2 mg/kg × 5天,0.5 mg/kg × 9天)向肿瘤输送活性GA,肿瘤至血浆暴露量提高两倍多,并在小鼠侧腹部MPNST模型上显著抑制肿瘤生长,未观察到毒性。[1] |
分子量 | 447.48 |
分子式 | C22H29N3O7 |
CAS No. | 2079938-92-2 |
Smiles | C(OC(C(C)(C)C)=O)(OC(N[C@H](C(OC(C)C)=O)CCC(C=[N+]=[N-])=O)=O)C1=CC=CC=C1 |
密度 | no data available |
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: 90.0 mg/mL (201.1 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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