Verdinexor (KPT-335)
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- CAS号:
- 1392136-43-4
- 英文名:
- Verdinexor (KPT-335)
- 英文别名:
- CS-1798;KPT-335;Verdinexor;KPT335(Verdinexor);Verdinexor(KPT-335);Verdinexor (KPT-335) USP/EP/BP;Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyridin-;(Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-N'-pyridin-2-ylprop-2-enehydrazide;(Z)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyridin-2-yl)acrylohydrazide;(Z)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyridin-2-yl)acrylohydrazide
- 中文名:
- Verdinexor (KPT-335)
- 中文别名:
- XPO1/CRM1抑制剂;化合物VERDINEXOR;SINE抑制剂(VERDINEXOR);(Z)-3(3-(3,5-双(三氟甲基)苯基)-1H-1,2,4-三唑-1-基)-N'-(吡啶-2-基)丙烯酰肼;(Z)-3(3-(3,5-双(三氟甲基)苯基)-1H-1,2,4-三唑-1-基)-N'-(吡啶-2-基)丙烯酰肼
- CBNumber:
- CB02680705
- 分子式:
- C18H12F6N6O
- 分子量:
- 442.32
- MOL File:
- 1392136-43-4.mol
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Verdinexor (KPT-335)化学性质
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密度:
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1.49±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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≥44.2 mg/mL in DMSO; insoluble in H2O; ≥2.31 mg/mL in EtOH with ultrasonic
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形态:
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solid
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酸度系数(pKa):
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10.04±0.43(Predicted)
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颜色:
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Light yellow to yellow
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CAS 数据库:
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1392136-43-4
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Verdinexor (KPT-335)性质、用途与生产工艺
Verdinexor（KPT-335）是一种口服生物可利用的，选择性XPO1/CRM1抑制剂。
Verdinexor inhibits the viability of Jurkat, OCI-Ly3, OCI-Ly10, and CLBL1 cells with IC50 of 0.3 nM, 2.1 nM, 41.8 nM, and 8.5 nM, respectively. KPT-335 also induces apoptosis in CLBL1 cells and primary canine DLBCL cells that express XPO1 and SINE. Verdinexor potently and selectively inhibits vRNP export and effectively inhibits the replication of various influenza virus A and B strains, including pandemic H1N1 virus, highly pathogenic H5N1 avian influenza virus, and the recently emerged H7N9 strain.
Verdinexor (25 mg/kg twice daily, p.o.) reduces proinflammatory cytokine expression in the lung, produces in vivo antiviral activity by reducing lung virus titers, and thus reduces pulmonary disease pathogenesis and death associated with lethal influenza A virus challenge. In autosomal-dominant polycystic kidney disease model, Verdinexor (5 mg/kg, i.p.) attenuates cyst growth via inhibition of XPO1.
Verdinexor (KPT-335, ATG-527)是一种口服生物可利用的，选择性XPO1/CRM1抑制剂。
Verdinexor抑制Jurkat，OCI-Ly3，OCI-Ly10，和CLBL1细胞的活性，IC50分别为0.3 nM，2.1 nM，41.8 nM，和8.5 nM。KPT-335也会诱导表达XPO1与SINE 的CLBL1和原代犬DLBCL细胞凋亡。 Verdinexor选择性有效抑制vRNP输出，也有效抑制各种流感病毒A和B菌株，包括流行性H1N1病毒，高致病性H5N1禽流感病毒，以及最近出现的H7N9菌株。
Verdinexor (25 mg/kg，每天两次，p.o.)降低肺中促炎性细胞因子的表达，在体内通过减少肺病毒滴度产生抗病毒活性，并且因此降低与致死性甲型流感A病毒相关的肺疾病的发病率和死亡率。 在常染色体显性多囊肾疾病模型中，Verdinexor (5 mg/kg, i.p.)通过抑制XPO1减弱囊肿生长。
Verdinexor (KPT-335)
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 |
|---|
| 2024/08/19 | HY-15970 | Verdinexor | | 2 mg | 979元 |
| 2024/08/19 | HY-15970 | Verdinexor | | 10 mM * 1 mLin DMSO | 1557元 |
Verdinexor (KPT-335)
生产厂家
1392136-43-4, Verdinexor (KPT-335) 相关搜索:
- API
- Inhibitors
- 药靶配体
- 细胞生物学试剂
- 小分子抑制剂，天然产物
- C18H12F6N6O
- (Z)-3(3-(3,5-双(三氟甲基)苯基)-1H-1,2,4-三唑-1-基)-N'-(吡啶-2-基)丙烯酰肼
- 化合物VERDINEXOR
- (Z)-3(3-(3,5-双(三氟甲基)苯基)-1H-1,2,4-三唑-1-基)-N'-(吡啶-2-基)丙烯酰肼
- XPO1/CRM1抑制剂
- SINE抑制剂(VERDINEXOR)
- 1392136-43-4
- (Z)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyridin-2-yl)acrylohydrazide
- (Z)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyridin-2-yl)acrylohydrazide
- Verdinexor (KPT-335) USP/EP/BP
- 2-Propenoic acid, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-, 2-(2-pyridinyl)hydrazide, (2Z)-
- KPT335(Verdinexor)
- (Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-N'-pyridin-2-ylprop-2-enehydrazide
- CS-1798
- (KPT335)(Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyridin-2-yl)acrylohydrazide
- (2Z)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N -(pyridin-2-yl)prop-2-enehydrazide Verdinexor(KPT-335)
- (2Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]- 2-propenoic acid-2-(2-pyridinyl)hydrazide
- Verdinexor(KPT-335)
- Verdinexor
- KPT-335
- Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyridin-