Vatalanib (PTK787) 2HCl

製品コードS1101 別名:ZK 222584 (cpg-79787) 2HCl

Vatalanib (PTK787) 2HCl化学構造


Vatalanib (PTK787) 2HClは一種のVEGFR2/KDR阻害剤で、無細胞試験でIC50値が37 nMです。Vatalanib (PTK787) 2HClはVEGFR1/Flt-1に作用する効果が少し弱いですが、VEGFR2/KDRに作用する効果はVEGFR3/Flt-4に作用する効果より18倍が高くなります。臨床3期。

サイズ 価格(税別)  
JPY 10624.00
JPY 11620.00
JPY 34860.00
JPY 61420.00


  • Combinational treatment of kinase inhibitors induces the similar phenotype produced by PP1. All images are lateral view with dorsal to the top and anterior to the left. The combinational treatment of Dasatinib (D) or U0126 (U) with Sunitinib (SU),PTK787 (PTK), or ZM323881 (Z) resulted in the shrinkage of dorsal aorta.

    Cell Res 2011 21, 1080-1087. Vatalanib (PTK787) 2HCl purchased from Selleck.

    Mechanisms of VEGF-activated Ca2 entry. All data were from HUVECs. a, Mean 100 ng/mL VEGF-evoked Ca2 entry in the presence of 100 nmol/L sorafenib (n/N3/40), 10 nmol/L vatalanib (n/N=3/24), or 10 mol/L U73122 (n/N=3/24) normalized to their matched controls. b and c, eYFP-STIM1 (green) before (control) (b) and after exposure to 100 ng/mL VEGF (c). d, Summary data for 100 ng/mL VEGF-evoked transient and sustained Ca2 signals after transfection with or (n/N3/64). e, Example merged image of a cell labeled with anti-VEGFR2 antibody (green), anti-Orai1 antibody (red), and the nuclear counter stain, DAPI (blue).

    Circ Res 2011 108, 1190-1198. Vatalanib (PTK787) 2HCl purchased from Selleck.

  • (Aa-Ja) A single row of BTs on the intact fin and stump after 6-14 dot with PTK787 and 4-12 dot with T. Small BTs appear in the fin regenerate after 8 dot with PTK787 and 6 dot with T (Da,Ea). A small BT cluster appears on the regenerate after 14 dot with PTK787 and 12 dot with T (Ga,Ha). (Ab-Jb) After 4 dot with T, BTs develop on the regenerate, stump and intact fin and continue to grow from 6-12 dot. (Jb) After 12 dot, the blood vessel network of T-treated females is similar to that of males. (Ac-Jc) PTK787-treated females do not possess BTs. (Aa-Ja,Ac-Jc) Neo-angiogenesis and regenerative outgrowth are inhibited in all PTK787-treated females. (Ad-Jd) System water controls regenerate normally and do not grow BTs. B.F., brightfield. Fli, fli1a:EGFP (green). KR21 (red) outlines the BTs. White vertical lines indicate the amputation plane. Scale bar: 100 um.

    Development 2013 140, 4323-34. Vatalanib (PTK787) 2HCl purchased from Selleck.




製品説明 Vatalanib (PTK787) 2HClは一種のVEGFR2/KDR阻害剤で、無細胞試験でIC50値が37 nMです。Vatalanib (PTK787) 2HClはVEGFR1/Flt-1に作用する効果が少し弱いですが、VEGFR2/KDRに作用する効果はVEGFR3/Flt-4に作用する効果より18倍が高くなります。臨床3期。
(Cell-free assay)
(Cell-free assay)
VEGFR2/Flk1 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
(Cell-free assay)
37 nM 77 nM 270 nM 580 nM 660 nM

Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC50 of 270 nM, 730 nM and 580 nM, respectively. Furthermore, 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]

体内試験 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]


+ 展開

VEGF Receptor Tyrosine Kinase Assays :

The in vitro kinase assays are performed in 96-well plates as a filter binding assay, using the recombinant GST-fused kinase domains expressed in baculovirus and purified over glutathione-Sepharose. γ-[33P]ATP is used as the phosphate donor, and poly-(Glu:Tyr 4:1) peptide is used as the acceptor. Recombinant GST-fusion proteins are diluted in 20 mM Tris·HCl (pH 7.5) containing 1–3 mM MnCl2, 3–10 mM MgCl2, 0.25 mg/mL polyethylene glycol 20000, and 1 mM DTT, according to their specific activity. Each GST-fused kinase is incubated under optimized buffer conditions [20 mM Tris-HCl buffer (pH 7.5), 1–3 mM MnCl2, 3–10 mM MgCl2, 3–8 μg/mL poly-(Glu:Tyr 4:1), 0.25 mg/mL polyethylene glycol 20000, 8 μM ATP, 10 μM sodium vanadate, 1 mM DTT, and 0.2 μCi[γ-33P]ATP in a total volume of 30 μL in the presence or absence of a test substance for 10 minutes at ambient temperature. The reaction is stopped by adding 10 μL of 250 mM EDTA. Using a 96-well filter system, half the volume (20 μL) is transferred onto a Immobilon-polyvinylidene difluoride membrane. The membrane is then washed extensively in 0.5% H3PO4 and then soaked in ethanol. After drying, Microscint cocktail is added, and scintillation counting is performed. IC50s for PTK787/ZK 222584 or SU5416 in these as well as all assays described below are calculated by linear regression analysis of the percentage inhibition.
細胞試験: [1]
+ 展開
  • 細胞株: HUVECs
  • 濃度: 0-10 μM
  • 反応時間: 48 hours
  • 実験の流れ: As a test of the ability of PTK787/ZK 222584 to inhibit a functional response to VEGF, an endothelial cell proliferation assay, based on BrdUrd incorporation is used. Subconfluent HUVECs are seeded into 96-well plates coated with 1.5% gelatin and then incubated at 37 °C and 5% CO2 in growth medium. After 24 hours, 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 PTK787/ZK 222584. As a control, wells without growth factor are also included. After 24 hours of incubation, BrdUrd labeling solution is added, and cells incubated an additional 24 hours before fixation, blocking, and addition of peroxidase-labeled anti-BrdUrd antibody. Bound antibody is then detected using 3,3′5,5′-tetramethylbenzidine substrate, which results in a colored reaction product that is quantified spectrophotometrically at 450 nm.
+ 展開
  • 動物モデル: A431 epithelial carcinoma, Ls174T colon carcinoma, HT-29 colon carcinoma, PC-3 prostate carcinoma, DU145 prostate carcinoma, and CWR-22 prostate carcinoma cells are injected s.c. into the nude mice.
  • 製剤: Vatalanib is dissolved in distilled water containing 5% DMSO and 1% Tween 80.
  • 投薬量: 25-100 mg/kg
  • 投与方法: Administered via p.o.

溶解度 (25°C)

体外 DMSO 85 mg/mL (202.51 mM)
Water 10 mg/mL (23.82 mM)
Ethanol 6 mg/mL (14.29 mM)

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。


分子量 419.73


CAS No. 212141-51-0
別名 ZK 222584 (cpg-79787) 2HCl





マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)


  • マス




貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1



  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


マス 濃度 ボリューム 分子量


NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00390000 Active, not recruiting Unspecified Adult Solid Tumor, Protocol Specific Mayo Clinic|National Cancer Institute (NCI) January 2007 Phase 1
NCT00627198 Completed Neuroendocrine Tumors University of Iowa|Novartis Pharmaceuticals December 2006 Phase 2
NCT00615160 Suspended Melanoma University of Schleswig-Holstein December 2006 Phase 1|Phase 2
NCT00385853 Completed Glioblastoma Massachusetts General Hospital|Dana-Farber Cancer Institute|Novartis September 2006 Phase 1
NCT00348790 Completed Brain and Central Nervous System Tumors|Sarcoma Northwestern University|Novartis May 2006 Phase 2
NCT00358163 Unknown status Metastatic Non-hematologic Malignancies Massachusetts General Hospital|Novartis Pharmaceuticals|Beth Israel Deaconess Medical Center|Brigham and Womens Hospital|Dana-Farber Cancer Institute April 2006 Phase 1



Handling Instructions


  • * 必須

Related Antibodies


VEGFR Inhibitors with Unique Features


Tags: Vatalanib (PTK787) 2HClを買う | Vatalanib (PTK787) 2HCl ic50 | Vatalanib (PTK787) 2HCl供給者 | Vatalanib (PTK787) 2HClを購入する | Vatalanib (PTK787) 2HCl費用 | Vatalanib (PTK787) 2HCl生産者 | オーダーVatalanib (PTK787) 2HCl | Vatalanib (PTK787) 2HCl化学構造 | Vatalanib (PTK787) 2HCl分子量 | Vatalanib (PTK787) 2HCl代理店
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID