2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. Tivozanib hydrochloride hydrate

Tivozanib hydrochloride hydrate  (Synonyms: AV-951 hydrochloride hydrate; KRN951 hydrochloride hydrate)

目录号: HY-10977A 纯度: 99.88%
COA 产品使用指南

摩尔计算器

Tivozanib hydrochloride hydrate (AV-951 hydrate; KRN951 hydrate) 是 Tivozanib (HY-10977) 的水合盐酸盐形式。Tivozanib hydrochloride hydrate 是口服有效的血管内皮生长因子受体 (VEGFR)-1, 2 3 抑制剂，IC50 为 30，6.5 和 15 nM。Tivozanib hydrochloride hydrate 具有抗肿瘤活性。

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Tivozanib hydrochloride hydrate Chemical Structure

Tivozanib hydrochloride hydrate Chemical Structure

CAS No. : 682745-41-1

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Customer Review

Other Forms of Tivozanib hydrochloride hydrate:

Tivozanib hydrochloride hydrate 相关抗体

Top Publications Citing Use of Products

查看 VEGFR 亚型特异性产品:

查看所有亚型
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrochloride hydrate exhibits antitumor efficacy[1].

IC50 & Target[3]

VEGFR-2

6.5 nM (IC50)

VEGFR-3

15 nM (IC50)

VEGFR-1

30 nM (IC50)

体外研究
(In Vitro)

Tivozanib hydrochloride hydrate 抑制 VEGFR-1、VEGFR-2 和 VEGFR-3 的磷酸化，IC50 为 0.16-0.24 nM[1]。
Tivozanib hydrochloride hydrate (0-100 nM，24 h) 抑制 VEGF 诱导的 HUVEC 增殖，IC50 为 0.67 nM，并以剂量依赖性的方式抑制 HUVEC 迁移[1]。
Tivozanib hydrochloride hydrate (0-300 nM, 1 h) 配体依赖性地选择性抑制内皮细胞中 VEGF 刺激的 MAPK 磷酸化，抑制 ERK1 和 ERK2 活性，IC50 为 0.13 和 0.18 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Tivozanib hydrochloride hydrate 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HUVECs
Concentration: 0-100 nM
Incubation Time: 24 h
Result: Inhibited Proliferation.

Cell Migration Assay [1]

Cell Line: HUVECs
Concentration: 0-100 nM
Incubation Time: 22 h
Result: Inhibited migration.

Western Blot Analysis[1]

Cell Line: HUVECs
Concentration: 0-300 nM
Incubation Time: 1 h
Result: Inhibited VEGR-dependent phosphorylation of ERK1 and ERK2.
体内研究
(In Vivo)

Tivozanib hydrochloride hydrate (0.04-1 mg/kg，口服 14 天) 在无胸腺小鼠模型对乳腺癌、结肠癌、肝癌、肺癌、卵巢癌、胰腺癌和前列腺癌具有抗癌活性[1]。
Tivozanib hydrochloride hydrate (0.2-1 mg/kg，口服 21 天) 可逆性抑制 Calu-6 荷瘤大鼠模型中的血管通透性和血管生成[1].
Tivozanib hydrochloride hydrate (5 mg/kg，口服，单剂量) 在无胸腺小鼠模型中的药代动力学特征为 AUCinf 为 44.5 μg·h/mL，Cmax 为 2823 ng/mL[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Calu-6 tumor bearing athymic mice model[1]
Dosage: 0.04-1 mg/kg/day
Administration: p.o., for 14-21 days
Result: Inhibited tumor growth, angiogenesis and vascular permeability.
Clinical Trial
分子量

509.34

Formula

C22H22Cl2N4O6
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (245.42 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9633 mL 9.8166 mL 19.6333 mL
5 mM 0.3927 mL 1.9633 mL 3.9267 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.88%

COA (202 KB) HNMR (289 KB) LCMS (268 KB)

产品使用指南 (1538 KB)
参考文献

Tivozanib hydrochloride hydrate 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9633 mL 9.8166 mL 19.6333 mL 49.0831 mL
5 mM 0.3927 mL 1.9633 mL 3.9267 mL 9.8166 mL
10 mM 0.1963 mL 0.9817 mL 1.9633 mL 4.9083 mL
15 mM 0.1309 mL 0.6544 mL 1.3089 mL 3.2722 mL
20 mM 0.0982 mL 0.4908 mL 0.9817 mL 2.4542 mL
25 mM 0.0785 mL 0.3927 mL 0.7853 mL 1.9633 mL
30 mM 0.0654 mL 0.3272 mL 0.6544 mL 1.6361 mL
40 mM 0.0491 mL 0.2454 mL 0.4908 mL 1.2271 mL
50 mM 0.0393 mL 0.1963 mL 0.3927 mL 0.9817 mL
60 mM 0.0327 mL 0.1636 mL 0.3272 mL 0.8181 mL
80 mM 0.0245 mL 0.1227 mL 0.2454 mL 0.6135 mL
100 mM 0.0196 mL 0.0982 mL 0.1963 mL 0.4908 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tivozanib hydrochloride682745-41-1AV-951 hydrochlorideKRN951 hydrochlorideVEGFRVascular endothelial growth factor receptororally activeangiogenesisvascular permeabilityantitumorrenal cell carcinomaInhibitorinhibitorinhibit

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目录号：
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