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  2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. Vatalanib

Vatalanib  (Synonyms: 瓦他拉尼堿; PTK787; ZK-222584; CGP-79787)

目錄號: HY-10203 純度: 99.93%
COA 產(chǎn)品使用指南 技術(shù)支持

Vatalanib（PTK787; ZK-222584; CGP-79787）是VEGFR2/KDR的抑制劑，其IC50值為37nM。

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Vatalanib Chemical Structure

Vatalanib Chemical Structure

CAS No. : 212141-54-3

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規(guī)格 價格 是否有貨 數(shù)量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥305
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5 mg ￥400
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10 mg ￥640
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25 mg ￥1160
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50 mg ￥1840
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100 mg ￥2720
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500 mg   詢價  

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Customer Review

Other Forms of Vatalanib:

查看 VEGFR 亞型特異性產(chǎn)品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM.

IC50 & Target[1]

VEGFR2

37 nM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
21.16 μM
Compound: 8; PTK787
Inhibition of human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
Inhibition of human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 26590508]
A549 IC50
21.16 μM
Compound: PTK-787
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
[PMID: 20537434]
CHO IC50
0.016 μM
Compound: A, PTK-787
Inhibition of VEGF-induced VEGFR2 phosphorylation expressed in CHO cells in presence of 8 uM ATP by ELISA
Inhibition of VEGF-induced VEGFR2 phosphorylation expressed in CHO cells in presence of 8 uM ATP by ELISA
[PMID: 19124243]
EA.hy 926 IC50
19.98 μM
Compound: 1
Cytotoxicity against human EAhy926 cells assessed as reduction in cell viability after 72 hrs by presto-blue assay
Cytotoxicity against human EAhy926 cells assessed as reduction in cell viability after 72 hrs by presto-blue assay
[PMID: 30776229]
EA.hy 926 IC50
22.32 μM
Compound: Vatalanib
Cytotoxicity against human EA.hy 926 cells assessed as reduction in cell viability incubated for 72 hrs by PrestoBlue reagent based assay
Cytotoxicity against human EA.hy 926 cells assessed as reduction in cell viability incubated for 72 hrs by PrestoBlue reagent based assay
[PMID: 34459195]
HEK293 IC50
0.021 μM
Compound: A, PTK-787
Inhibition of VEGFR2 expressed in HEK293 cells assessed as inhibition of receptor phosphorylation by ELISA
Inhibition of VEGFR2 expressed in HEK293 cells assessed as inhibition of receptor phosphorylation by ELISA
[PMID: 19124243]
HEK293 IC50
0.021 μM
Compound: A
Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA
Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA
[PMID: 16460936]
HT-29 IC50
22.11 μM
Compound: 8; PTK787
Inhibition of human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay
Inhibition of human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 26590508]
HT-29 IC50
22.11 μM
Compound: PTK-787
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
[PMID: 20537434]
HUVEC IC50
33 nM
Compound: 1, PTK-787
Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced proliferation after 3 days by WST-8 assay
Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced proliferation after 3 days by WST-8 assay
[PMID: 21247763]
HUVEC IC50
33 nM
Compound: 1, PTK-787
Inhibition of VEGF-induced HUVEC proliferation treated 1 hr before VEGF challenge measured 3 days by WST-8 assay
Inhibition of VEGF-induced HUVEC proliferation treated 1 hr before VEGF challenge measured 3 days by WST-8 assay
[PMID: 21074435]
MDA-MB-231 IC50
57.72 μM
Compound: 8; PTK787
Inhibition of human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
Inhibition of human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 26590508]
MDA-MB-231 IC50
57.72 μM
Compound: PTK-787
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
[PMID: 20537434]
PBMC IC50
> 1 μM
Compound: 17 (PTK-787)
In vitro inhibitory concentration on the production of pro-inflammatory cytokine IL-2 in PBMC (Peripheral blood mononuclear cells) determined by IL-2 PBMC assay
In vitro inhibitory concentration on the production of pro-inflammatory cytokine IL-2 in PBMC (Peripheral blood mononuclear cells) determined by IL-2 PBMC assay
[PMID: 16107139]
體外研究
(In Vitro)

Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC50 of 270 nM, 730 nM and 580 nM, respectively. Vatalanib shows the anti-proliferation effect by inhibiting thymidine incorporation induced by VEGF in HUVECs with and IC50 of 7.1 nM, and dose-dependently suppresses VEGF-induced survival and migration of endothelial cells in the same dose range without cytotoxic or antiproliferative effect on cells that do not express VEGF receptors[1]. A recent study shows that Vatalanib significantly inhibits the growth of hepatocellular carcinoma cells and enhances the IFN/5-FU induced apoptosis by increasing proteins levels of Bax and reduced Bcl-xL and Bcl-2[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Vatalanib induces dose-dependent inhibition of the angiogenic response to VEGF and PDGF in both a growth factor implant model and a tumor cell-driven angiogenesis model after once-daily oral dosing (25-100 mg/kg). In the same dose range, Vatalanib also inhibits the growth and metastasesof several human carcinomas in nude mice without significant effect on circulating blood cells or bone marrow leukocytes[1].

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

346.81

Formula

C20H15ClN4
CAS 號
性狀

固體

顏色

Light yellow to yellow

中文名稱

瓦他拉尼堿
運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實驗： 

DMSO 中的溶解度 : 62.5 mg/mL (180.21 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.8834 mL 14.4171 mL 28.8342 mL
5 mM 0.5767 mL 2.8834 mL 5.7668 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.93%

參考文獻
Kinase Assay
[1]

Each GST-fused kinase is incubated under optimized buffer conditions. ATP in a total volume of 30 μL in the presence or absence of a test substance (Vatalanib) for 10 min at ambient temperature. The reaction is stopped by adding 10 μL of 250 mM EDTA[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Subconfluent HUVECs are seeded into 96-well plates coated with 1.5% gelatin. After 24 h, growth medium is replaced by basal medium containing 1.5% FCS and a constant concentration of VEGF (50 ng/mL), bFGF (0.5 ng/mL), or FCS (5%), in the presence or absence of Vatalanib. As a control, wells without growth factor are also included. After 24 h of incubation, BrdUrd labeling solution is added, and cells incubated an additional 24 h before fixation, blocking, and addition of peroxidase-labeled anti-BrdUrd antibody. Bound antibody is then detected using 3,3' 5,5'-tetramethylbenzidine substrate[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

A porous Teflon chamber (volume, 0.5 mL) is filled with 0.8% w/v agar containing heparin (20 units/mL) with or without growth factor (3 μg/mL human VEGF, 2 μg/mL human PDGF) is implanted s.c. on the dorsal flank of C57/C6 mice. The mice are treated with Vatalanib (12.5, 25 or 50 mg/kg dihydrochloride p.o. once daily) or vehicle (water) starting 1 day before implantation of the chamber and continuing for 5 days after. At the end of treatment, the mice are killed, and the chambers are removed. The vascularized tissue growing around the chamber is carefully removed and weighed, and the blood content is assessed by measuring the hemoglobin content of the tissue[1].

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

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8834 mL 14.4171 mL 28.8342 mL 72.0856 mL
5 mM 0.5767 mL 2.8834 mL 5.7668 mL 14.4171 mL
10 mM 0.2883 mL 1.4417 mL 2.8834 mL 7.2086 mL
15 mM 0.1922 mL 0.9611 mL 1.9223 mL 4.8057 mL
20 mM 0.1442 mL 0.7209 mL 1.4417 mL 3.6043 mL
25 mM 0.1153 mL 0.5767 mL 1.1534 mL 2.8834 mL
30 mM 0.0961 mL 0.4806 mL 0.9611 mL 2.4029 mL
40 mM 0.0721 mL 0.3604 mL 0.7209 mL 1.8021 mL
50 mM 0.0577 mL 0.2883 mL 0.5767 mL 1.4417 mL
60 mM 0.0481 mL 0.2403 mL 0.4806 mL 1.2014 mL
80 mM 0.0360 mL 0.1802 mL 0.3604 mL 0.9011 mL
100 mM 0.0288 mL 0.1442 mL 0.2883 mL 0.7209 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.

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