磷酸依托泊苷
|
|
|
- CAS号:
- 117091-64-2
- 英文名:
- Etoposide phosphate
- 英文别名:
- ETOPOPHOS;Etopofos;BMY 40481;ETOPOSIDE PHOSPHATE;ETOPOSIDE PHOSPHONATE;Etoposide 4'-Phosphate;ETOPOSIDEPHOSPHATE,ETOPOPHOS;Etoposide Phosphate (200 mg);Etoposide phosphate≥ 98% (HPLC);ETOPOSIDE PHOSPHONATE, ETOPOPHOS
- 中文名:
- 磷酸依托泊苷
- 中文别名:
- 磷酸依托泊苷;磷酸依托泊甙;依托泊甙磷酸酯;依托泊苷磷酸酯;依托泊苷磷酸酯(磷酸依托泊甙、磷酸依托泊苷)
- CBNumber:
- CB5671214
- 分子式:
- C29H33O16P
- 分子量:
- 668.54
- MOL File:
- 117091-64-2.mol
|
|
|
磷酸依托泊苷化学性质
-
沸点:
-
907.7±75.0 °C(Predicted)
-
|
-
密度:
-
1?+-.0.1 g/cm3(Predicted)
-
|
-
储存条件:
-
-20°C
-
|
-
酸度系数(pKa):
-
1.13±0.50(Predicted)
-
|
-
水溶解性:
-
Water: 125 mg/mL (186.97 mM)
-
|
磷酸依托泊苷性质、用途与生产工艺
磷酸依托泊苷是依托泊苷的磷酸盐，依托泊苷是鬼臼毒素的半合成衍生物，一种细胞周期特异性抗肿瘤药物，作用于晚S期或G2期，其作用位点是拓扑异构酶Ⅱ，形成一种药物-酶-DNA三者之间稳定的可裂性复合物，使DNA复制过程中产生的瞬间链的断裂难以修复，导致细胞产生依托泊苷剂量依赖性的DNA损伤，促进细胞凋亡。广泛用于治疗各种恶性肿瘤，包括白血病、淋巴瘤和实体瘤，但要注意该药物存在比较严重的骨髓抑制、胃肠道反应。
依托泊苷由美国医药巨头时美施贵宝公司研发上市，是国际上公认的新型抗肿瘤药物，也是迄今为止最成功的鬼臼毒素类抗肿瘤药物。依托泊苷为鬼臼毒素的糖代谢产物，属细胞周期特异性抗肿瘤药物，作用于DNA拓扑异构酶II，形成药物-酶-DNA稳定的可逆性复合物，阻碍DNA修复，发挥抗肿瘤效果。采用依托泊苷联合治疗复发卵巢癌，临床取得了较顺铂或卡铂为基础的联合化疗更为理想的近期疗效，老年人晚期胃癌的治疗一直是比较棘手的问题，依托泊苷显示了较好的治疗前景。2020年3月，“I药”度伐利尤单抗联合标准治疗（SoC），依托泊苷+卡铂或顺铂化疗方案获FDA批准，用于广泛期小细胞肺癌（ES-SCLC）成人患者的一线治疗。2018年，依托泊苷胶囊全球总销售额约为2623万美元，国内销售额约为262万美元。
Etoposide phosphate (BMY-40481) 是一种有效的抗癌 (anti-cancer) 化疗试剂和一种选择性拓扑异构酶 II (topoisomerase II) 抑制剂，可以防止 DNA 链的重新连接。Etoposide phosphate 是依托泊苷的磷酸酯前药，被认为与 Etoposide 活性相当。Etoposide phosphate 诱导细胞周期阻滞、凋亡 (apoptosis) 和自噬 (autophagy)。
Etoposide phosphate is a water-soluble derivative and probable prodrug of etoposide characterized by the presence of a phosphate group in position 4' of the E ring of the etoposide molecule.Etoposide phosphate (0-1 μM; 72 hours) inhibits HCT116 FBXW
+/+
, FBXW
-/-
and p53
-/-
as a dose-dependent manner, exhibits IC
50
values of 0.945 μM; 0.375 μM; and 1.437 μM, respectively.Etoposide phosphate (25 μM; 6 hours) delays p53 recover in FBXW7-deficient cells. In addition, FBXW7 expression is disappeared in FBXW7
-/-
cells.
Cell Viability Assay
|
Cell Line:
|
FBXW
+/+
, FBXW
-/-
and p53
-/-
cell
|
|
Concentration:
|
0.025 μM, 0.05 μM, 0.075 μM, 0.1 μM, 0.2 μM, 0.4 μM, 0.6 μM, 0.8 μM, 1 μM
|
|
Incubation Time:
|
72 hours
|
|
Result:
|
Inhibited HCT116 FBXW
+/+
, FBXW
-/-
and p53
-/-
cell growth as a concentration manner.
|
Western Blot Analysis
|
Cell Line:
|
HCT116 FBXW7
+/+
or FBXW7
-/-
cells
|
|
Concentration:
|
25 μM
|
|
Incubation Time:
|
6 hours
|
|
Result:
|
Exhibited that the recovery of p53 levels after DNA damage is mediated by FBXW7.
|
Etoposide phosphate (intravenous injection; 50, 100, or 150 mg/kg; single dose) has clinical symptomology of progressive ataxia, impaired righting reflex, and splaying and paresis of fore- and hindlimbs at day 8 in female CD-1 mice.
|
Animal Model:
|
Female CD-1 mice
|
|
Dosage:
|
50, 100, or 150 mg/kg
|
|
Administration:
|
Intravenous injection; single dose
|
|
Result:
|
Observed degeneration of dorsal root ganglion cells and axonal degeneration of their distal and proximal processes in peripheral nerves, dorsal spinal roots, and dorsal funiculi of the spinal cord at all doses under light microscopy (LM).
|
磷酸依托泊苷
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/16 | HY-13630 | 磷酸依托泊苷
Etoposide phosphate | 117091-64-2 | 5mg | 800元 |
| 2024/01/16 | HY-13630 | 磷酸依托泊苷
Etoposide phosphate | 117091-64-2 | 10mM * 1mLin Water | 1177元 |
磷酸依托泊苷
生产厂家
全球有 96家供应商
磷酸依托泊苷国内生产厂家
117091-64-2, 磷酸依托泊苷 相关搜索:
- API
- Pharmaceuticals
- Intermediates & Fine Chemicals
- Inhibitors
- Heterocycles
- Drug Analogues
- Carbohydrates & Derivatives
- Antineoplastic
- 原料药
- 抑制剂
- 信号转导通路激酶抑制剂
- C29H33O16P
- 依托泊甙磷酸酯
- 磷酸依托泊苷
- 磷酸依托泊甙
- 依托泊苷磷酸酯
- 依托泊苷磷酸酯(磷酸依托泊甙、磷酸依托泊苷)
- 117091-64-2
- Etoposide Phosphate (200 mg)
- ETOPOPHOS
- Furo[3',4':6,7]naphtho[2,3-d]-1,3-dioxol-6(5aH)-one, 5-[3,5-dimethoxy-4-(phosphonooxy)phenyl]-9-[[4,6-O-(1R)-ethylidene-β-D-glucopyranosyl]oxy]-5,8,8a,9-tetrahydro-, (5R,5aR,8aR,9S)-
- Etoposide phosphate≥ 98% (HPLC)
- ETOPOSIDEPHOSPHATE,ETOPOPHOS
- Furo[3',4':6,7]naphtho[2,3-d]-1,3-dioxol-6(5aH)-one, 5-[3,5-dimethoxy-4-(phosphonooxy)phenyl]-9-[[4,6-O-(1R)-ethylidene-b-D-glucopyranosyl]oxy]-5,8,8a,9-tetrahydro-, (5R,5aR,8aR,9S)-
- Etopofos
- BMY 40481
- [5R-[5α,5aβ,8aα,9β(R*)]]-5-[3,5-DiMethoxy-4-(phosphonooxy)phenyl]-9-[(4,6-O-ethylidene-β-D-glucopyranosyl)oxy]-5,8,8a,9-tetrahydrofuro[3',4':6,7]naphtho[2,3-d]-1,3-dioxol-6(5aH)-one
- (5R,5aR,8aR,9S)-5-[3,5-DiMethoxy-4-(phosphonooxy)phenyl]-9-[[4,6-O-(1R)-ethylidene-β-D-glucopyranosyl]oxy]-5,8,8a,9-tetrahydrofuro[3',4':6,7]naphtho[2,3-d]-1,3-dioxol-6(5aH)-one
- Etoposide 4'-Phosphate
- BMY-40481, Etoposide 4'-Dihydrogenphosphate
- ETOPOSIDE PHOSPHONATE, ETOPOPHOS
- ETOPOSIDE PHOSPHONATE
- ETOPOSIDE PHOSPHATE