1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. Vatalanib succinate

Vatalanib succinate  (Synonyms: PTK787 succinate; ZK-222584 succinate; CGP-79787 succinate)

目录号: HY-110272
产品使用指南

Vatalanib (PTK787) succinate 是一种有效的具有口服活性的 VEGFR 抑制剂,对 KDR、Flt-1、Flk、Flt-4、c-Kit、c-Fms 和 PDGFR-β 的 IC50 值分别为 37 nM,77 nM,270 nM,660 nM,730 nM,1400 nM 和 580 nM。

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Vatalanib succinate Chemical Structure

Vatalanib succinate Chemical Structure

CAS No. : 212142-18-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Vatalanib (PTK787) succinate is a potent and orally active VEGFR inhibitor with IC50s of 37 nM, 77 nM, 270 nM, 660 nM, 730 nM, 1400 nM, and 580 nM for KDR, Flt-1, Flk, Flt-4, c-Kit, c-Fms, and PDGFR-β, respectively[1].

IC50 & Target[1]

KDR

37 nM (IC50)

Flt-1

77 nM (IC50)

Flt-4

730 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
> 10 μM
Compound: PKT787; ZK222584
Antiproliferative activity against mouse BaF3 cells expressing Bcr-ABL assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Bcr-ABL assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: PKT787; ZK222584
Antiproliferative activity against mouse BaF3 cells expressing ERBB2 V659E mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing ERBB2 V659E mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: PKT787; ZK222584
Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: PKT787; ZK222584
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: PKT787; ZK222584
Antiproliferative activity against mouse BaF3 cells expressing Tel-IGF-1R assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Tel-IGF-1R assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: PKT787; ZK222584
Antiproliferative activity against mouse BaF3 cells expressing KIT D816V mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing KIT D816V mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: PKT787; ZK222584
Antiproliferative activity against mouse BaF3 cells expressing Trp-MET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Trp-MET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: PKT787; ZK222584
Antiproliferative activity against mouse BaF3 cells expressing PTC3-RET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing PTC3-RET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: PKT787; ZK222584
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: PKT787; ZK222584
Antiproliferative activity against mouse BaF3 cells expressing NPM-ALK assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing NPM-ALK assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
0.076 μM
Compound: PKT787; ZK222584
Antiproliferative activity against mouse BaF3 cells expressing Tel-PDGFRbeta assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Tel-PDGFRbeta assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
0.215 μM
Compound: PKT787; ZK222584
Antiproliferative activity against mouse BaF3 cells expressing Tel-KDR-myc1.3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Tel-KDR-myc1.3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
Caco-2 IC50
18.27 μM
Compound: VATALANIB
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
10.21203/rs.3.rs-23951/v1
Caco-2 CC50
64.18 μM
Compound: VATALANIB
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
10.21203/rs.3.rs-23951/v1
HUVEC IC50
> 3 μM
Compound: PKT787; ZK222584
Antiproliferative activity against bFGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
Antiproliferative activity against bFGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
[PMID: 26629594]
HUVEC IC50
7.1 nM
Compound: PKT787; ZK222584
Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
[PMID: 26629594]
体外研究
(In Vitro)

在基于细胞的检测中,Vatalanib (PTK787) 在纳摩尔范围内抑制 VEGF 诱导的激酶插入结构域受体 (KDR) 自身磷酸化、内皮细胞增殖、迁移和存活。在浓度高达 1 µM 时,Vatalanib (PTK787) 对不表达 VEGF 受体的细胞没有任何细胞毒性或抗增殖作用[1]

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

体内研究
(In Vivo)

小鼠口服给药(50 mg/kg)后,Vatalanib (PTK787) 的血浆浓度在 8 小时以上保持在 1 μM 以上。Vatalanib (PTK787) 在生长因子植入模型以及每日口服一次(25-100 mg/kg)后的肿瘤细胞驱动的血管生成模型中诱导 VEGFPDGF 诱导的血管生成的剂量依赖性抑制[1]

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

分子量

464.90

Formula

C24H21ClN4O4

CAS 号
中文名称

瓦他拉尼琥珀酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

Vatalanib succinate 相关分类

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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.

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Vatalanib succinate
目录号:
HY-110272
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