VORELOXIN
|
|
|
- CAS号:
- 175414-77-4
- 英文名:
- Voreloxin
- 英文别名:
- SPC-595;SNS-595;AG-7352;CS-1489;VOSAROXIN;Voreloxin;Voreloxin, >=98%;Voreloxin (SNS-595);Voreloxin USP/EP/BP;SNS-595; VOSAROXIN; AG 7352
- 中文名:
- VORELOXIN
- 中文别名:
- 白血病孤儿药;VORELOXIN,拓扑异构酶 II抑制剂;VOSAROXIN|||AG 7352|||SNS-595
- CBNumber:
- CB92538816
- 分子式:
- C18H19N5O4S
- 分子量:
- 401.44
- MOL File:
- 175414-77-4.mol
|
|
|
VORELOXIN化学性质
-
沸点:
-
652.0±65.0 °C(Predicted)
-
|
-
密度:
-
1.52±0.1 g/cm3(Predicted)
-
|
-
储存条件:
-
Store at -20°C
-
|
-
溶解度:
-
insoluble in H2O; insoluble in EtOH; insoluble in DMSO
-
|
-
形态:
-
solid
-
|
-
酸度系数(pKa):
-
5.68±0.70(Predicted)
-
|
VORELOXIN性质、用途与生产工艺
Voreloxin (SNS-595; Vosaroxin; AG 7352) 是一种新创的拓扑异构酶 II (topoisomerase II) 抑制剂，能够诱导 DNA 双链断裂，阻滞 G2 期，最终细胞凋亡。
Voreloxin is a first-in-class topoisomerase II poison and inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis. Voreloxin (0.1-20 µM) inhibits topoisomerase II activity and induces site-selective DNA DSB in CCRF-CEM cells. Voreloxin (0.11, 0.33, 1, 3 µM) induces G2 arrest partially through topoisomerase II in A549 lung cancer cell line. Voreloxin cytotoxic activity requires DNA intercalation. However, Voreloxin (1-9 µM) does not generate significant levels of ROS. Voreloxin has potent cytotoxic activity in AML cell lines MV4-11 and HL-60, with IC
50
s of 95 ± 8 nM and 884 ± 114 nM, respectively. Voreloxin in combination with cytarabine shows additive or synergistic activity in acute leukemia cell lines. Voreloxin is active on the primary acute myeloid leukemia (AML) with a mean LD
50
of 2.3 μM. The LD
50
for voreloxin in myeloid cell lines NB4 and HL-60 is 0.59 μM ± 0.25 μM. Voreloxin causes accumulation of cells in the S and G2 phases of the cell cycle and acts on topoisomerase II.
Voreloxin (20 mg/kg, i.v.) alone results in 80% reduction in bone marrow cellularity of CD-1 mice by administration one dose every 4 days repeated twice (q4d ×2). voreloxin at 10 mg/kg in combination with cytarabine causes ablation of the marrow, dilation of sinusoids, and infiltration of adipocytes in mice. Voreloxin (20 mg/kg, i.v.) combined with cytarabine causes a reversible decrease in myeloid and lymphoid cells in bone marrow and peripheral blood CD-1 mice. voreloxin (10 mg/kg, q4d ×2) and cytarabine in combination causes reversible neutropenia with a more modest impact on platelets CD-1 mice.
VORELOXIN
上下游产品信息
上游原料
下游产品
175414-77-4, VORELOXIN 相关搜索:
- Inhibitors
- API
- 药靶配体
- 细胞周期
- 吡咯烷
- 萘啶
- 噻唑
- 原料药
- 小分子抑制剂，天然产物
- VOSAROXIN|||AG 7352|||SNS-595
- VORELOXIN,拓扑异构酶 II抑制剂
- 白血病孤儿药
- 175414-77-4
- Voreloxin USP/EP/BP
- CS-1489
- SNS-595; VOSAROXIN; AG 7352
- 7-[(3S,4S)-3-methoxy-4-(methylamino)pyrrolidin-1-yl]-4-oxo-1-(1,3-thiazol-2-yl)-1,8-naphthyridine-3-carboxylic acid
- 1,4-Dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid
- 7-((3S,4S)-3-Methoxy-4-(MethylaMino)pyrrolidin-1-yl)-4-oxo-1-(thiazol-2-yl)-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
- VOSAROXIN
- AG-7352, 1,4-dihydro-7-[(S,S)-3-Methoxy-4-MethylaMino-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic, (+)-1,4-dihydro-7-[(3S,4S)-3-Methoxy-4-(MethylaMino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid
- SPC-595
- SNS-595
- AG-7352
- Voreloxin
- Voreloxin, >=98%
- Voreloxin (SNS-595)
- 1,8-Naphthyridine-3-carboxylic acid, 1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo -1-(2-thiazolyl)-