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CAS号: | 914471-09-3 |
英文名称: | INCB024360 |
英文同义词: | IDO-IN-2;INCB024360;INCB-24360;INCB-024360;INCB 024360;INCB024360 analogue;INCB024360/INCB-024360;indoleaMine-2,3-dioxygenase inhibitor INCB024360;(4E)-4-[(3-chloro-4-fluoroanilino)-nitrosomethylidene]-1,2,5-oxadiazol-3-amine;4-Amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide |
中文名称: | INCB024360 |
中文同义词: | 4-氨基-N-(3-氯-4-氟苯基)-N'-羟基-1,2,5-恶二唑-3-甲脒 |
CBNumber: | CB22666639 |
分子式: | C9H7ClFN5O2 |
分子量: | 271.6355832 |
MOL File: | 914471-09-3.mol |
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INCB024360 性质、用途与生产工艺 |
生物活性
INCB024360是一个强效的竞争性IDO1 (indoleamine-(2,3)-dioxygenase)抑制剂,其IC50为67 nM。Phase 2。
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体外研究
在HeLa细胞中,INCB024360对IDO1显示出较高的抑制活性,IC50 为19 nM。在人同种异基因淋巴细胞的树突细胞或肿瘤细胞的共培养体系中,INCB024360,通过IDO1抑制,逆转IDO表达的HeLa细胞或DCs介导的T细胞抑制,并增加CD4+ T细胞,CD8+ T 细胞,和NK细胞的分化和功能活性。
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体内研究
负荷GM-CSF-分泌型B16肿瘤的小鼠体内,INCB024360 (75 mg/kg b.i.d)引起肿瘤生长的剂量依赖性抑制。 INCB024360显著抑制具有免疫活性的小鼠体内的肿瘤生长,但是对免疫缺陷的小鼠,没有抑制作用。
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INCB024360 上下游产品信息 |
上游原料
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下游产品
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914471-09-3, INCB024360 相关搜索: |
司美替尼
塞卡替尼
DMH1
泊马度胺
1-CYCLOHEXYL-2-(5H-IMIDAZO[5,1-A]ISOINDOL-5-YL)ETHANOL
AZD-9291
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C9H7ClFN5O2
4-氨基-N-(3-氯-4-氟苯基)-N'-羟基-1,2,5-恶二唑-3-甲脒
914471-09-3
(E)-4-Amino-N'-(3-chloro-4-fluorophenyl)-N-hydroxy-1,2,5-oxadiazole-3-carboximidamide
INCB024360 analogue
IDO-IN-2
4-Amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide INCB024360
(4E)-4-[(3-chloro-4-fluoroanilino)-nitrosomethylidene]-1,2,5-oxadiazol-3-amine
4-Amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide
INCB024360/INCB-024360
indoleaMine-2,3-dioxygenase inhibitor INCB024360
INCB-24360
INCB-024360
INCB024360
INCB 024360
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