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Tefinostat (CHR-2845) 是一种有效的单核细胞/巨噬细胞靶向组蛋白脱乙酰酶 (HDAC) 抑制剂。 Tefinostat 可被胞内酯酶人羧酸酯酶-1 (hCE-1) 裂解成活性酸 CHR-2847。Tefinostat 具有抗肿瘤活性,可用于研究白血病和晚期血液系统恶性肿瘤。
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Tefinostat (CHR-2845) 是一种有效的单核细胞/巨噬细胞靶向组蛋白脱乙酰酶 (HDAC) 抑制剂。 Tefinostat 可被胞内酯酶人羧酸酯酶-1 (hCE-1) 裂解成活性酸 CHR-2847。Tefinostat 具有抗肿瘤活性,可用于研究白血病和晚期血液系统恶性肿瘤。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 953 | 现货 | |
5 mg | ¥ 2,380 | 现货 | |
10 mg | ¥ 3,520 | 现货 | |
25 mg | ¥ 5,650 | 现货 | |
50 mg | ¥ 7,670 | 现货 | |
100 mg | ¥ 9,870 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 2,620 | 现货 |
产品描述 | Tefinostat (CHR-2845) is a potent monocyte/macrophage-targeted histone deacetylase (HDAC) inhibitor. Tefinostat is cleaved to the active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1).Tefinostat exhibits antitumor activity and can be used in the study of leukemia and advanced hematologic malignancies. |
体外活性 | Tefinostat (1-4 nM; AML cell lines) demonstrates efficacy in AML cell lines, including HL60 (M2 FAB type), MV411 (M4, FLT3-ITD), OCIAML3 (M4 NPM1mut), and THP1 (M5), with EC50 values of 2.3 μM, 57 nM, 110 nM, and 560 nM, respectively. |
别名 | 特诺司他, CHR-2845 |
分子量 | 495.61 |
分子式 | C28H37N3O5 |
CAS No. | 914382-60-8 |
Smiles | ONC(=O)CCCCCCC(=O)Nc1ccc(CN[C@H](C(=O)OC2CCCC2)c2ccccc2)cc1 |
密度 | 1.21 g/cm3 (Predicted) |
存储 | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 90 mg/mL (181.59 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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