製品番号: HY-110272

Vatalanib succinate

(別名: PTK787 succinate; ZK-222584 succinate; CGP-79787 succinate)

15 Cited Publications

カスタマーレビュー

Based on 15 publication(s) in Google Scholar

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.

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CAS 番号: 212142-18-2
分子式: C₂₄H₂₁ClN₄O₄
分子量:464.90

保管条件:

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

Data Sheet (274 KB)

Vatalanib succinate 構造式

CAS 番号: 212142-18-2

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (15)
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

KDR

37 nM (IC₅₀)

Flt-1

77 nM (IC₅₀)

Flt-4

730 nM (IC₅₀)

VEGFR アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
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 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 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 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 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	>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 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 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 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	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	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
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
CHO	ED₅₀	34 nM Compound: CGP-79787D	Inhibition of VEGF-stimulated autophosphorylation of VEGF-receptor 2 (KDR) expressed in CHO cells Inhibition of VEGF-stimulated autophosphorylation of VEGF-receptor 2 (KDR) expressed in CHO cells	[PMID: 10882357]
CHO	IC₅₀	16 nM Compound: 2 (PTK787)	Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells	[PMID: 12477352]
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	6 nM Compound: 2, PTK787	Antiproliferative activity against VEGF-induced HUVEC cells Antiproliferative activity against VEGF-induced HUVEC cells	[PMID: 18420406]
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]

体外実験

Vatalanib (PTK787) inhibits VEGF-induced autophosphorylation of kinase insert domain-containing receptor (KDR), endothelial cell proliferation, migration, and survival in the nanomolar range in cell-based assays. In concentrations up to 1 µM, Vatalanib (PTK787) does not have any cytotoxic or antiproliferative effect on cells that do not express VEGF receptors^[1].

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

体内実験

After oral dosing (50 mg/kg) to mice, plasma concentrations of Vatalanib (PTK787) remain above 1 μM for more than 8 h. Vatalanib (PTK787) induces dose-dependent inhibition of VEGF and PDGF-induced angiogenesis in a growth factor implant model, as well as a tumor cell-driven angiogenesis model after once-daily oral dosing (25-100 mg/kg)^[1].

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

化学情報

CAS 番号 212142-18-2
分子量 464.90
分子式 C₂₄H₂₁ClN₄O₄
SMILES

ClC(C=C1)=CC=C1NC2=C3C(C=CC=C3)=C(CC4=CC=NC=C4)N=N2.OC(CCC(O)=O)=O
別名

PTK787 succinate; ZK-222584 succinate; CGP-79787 succinate
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

Publications (15)

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Bioact Mater

Turning gray selenium into a nanoaccelerator of tissue regeneration by PEG modification. [Abstract]

2022 Jan 2:15:131-144. PMID: 35386336
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Pharm Anal

Distinct molecular targets of ProEGCG from EGCG and superior inhibition of angiogenesis signaling pathways for treatment of endometriosis. [Abstract]

2024 Jan;14(1):100-114. PMID: 38352946
Br J Pharmacol

Tanshinol borneol ester, a novel synthetic small molecule angiogenesis stimulator inspired by botanical formulations for angina pectoris. [Abstract]

2019 Sep;176(17):3143-3160. PMID: 31116880
JCI Insight

Blocking the angiopoietin-2-dependent integrin β-1 signaling axis abrogates small cell lung cancer invasion and metastasis. [Abstract]

2024 May 22;9(10):e166402. PMID: 38775153
Int J Mol Sci

Targeting Myeloid Cells in Head and Neck Squamous Cell Carcinoma: A Kinase Inhibitor Library Screening Approach. [Abstract]

2024 Nov 15;25(22):12277. PMID: 39596341
Oncol Rep

Local recurrence of small cell lung cancer following radiofrequency ablation is induced by HIF-1α expression in the transition zone. [Abstract]

2016 Mar;35(3):1297-308. PMID: 26750332
J Microbiol Biotechnol

Soluble Expression and Purification of the Catalytic Domain of Human Vascular Endothelial Growth Factor Receptor 2 in Escherichia coli. [Abstract]

2015 Aug;25(8):1227-33. PMID: 25907066
Drug Metab Pharmacokinet

Precise prediction of activators for the human constitutive androstane receptor using structure-based three-dimensional quantitative structure-activity relationship methods. [Abstract]

2017 Jun;32(3):179-188. PMID: 28412023
Mutat Res

Deciphering the molecular mechanism of YY1/HIF1A modulating ovarian cancer angiogenesis based on single-cell transcriptomics technology. [Abstract]

2025 Sep 24:831:111916. PMID: 41072350
Ulm University

2023 Mar 21.
Oxid Med Cell Longev

Tetramethylpyrazine Protects Endothelial Injury and Antithrombosis via Antioxidant and Antiapoptosis in HUVECs and Zebrafish. [Abstract]

2022 Jul 18:2022:2232365. PMID: 35898617
Evid Based Complement Alternat Med

Inhibitory Effects of Euphorbia ebracteolata Hayata Extract ECB on Melanoma-Induced Hyperplasia of Blood Vessels in Zebrafish Embryos. [Abstract]

2021 Apr 26:2021:5543259. PMID: 33995546
Patent

US20170349880A1.
Kitasato University

2017.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (274 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. J M Wood, et al. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 2000 Apr 15;60(8):2178-89. [Content Brief]

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Vatalanib succinate

15 Cited Publications

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Vatalanib succinate

High-Throughput Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 Vatalanib succinate

VEGFR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (15)

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

Vatalanib succinate

High-Throughput Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 Vatalanib succinate

VEGFR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (15)

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

Vatalanib succinate 関連分類

HY-110272 関連分類