Cabozantinib (XL184, BMS-907351)

製品コードS1119

Cabozantinib (XL184, BMS-907351)化学構造

分子量(MW):501.51

Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively.

サイズ 価格(税別) 在庫  
In DMSO JPY 38500 あり
JPY 20200 あり
JPY 30200 あり
JPY 80000 あり
JPY 167500 あり
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バルク問合せ

文献中Selleckの製品使用例(46)

製品安全説明書

VEGFR阻害剤の選択性比較

生物活性

製品説明 Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively.
ターゲット
VEGFR2/KDR [1]
(Cell-free assay)
c-Met [1]
(Cell-free assay)
0.035 nM 1.3 nM
体外試験

XL184 has weak inhibitory activity against RON and PDGFRβ with IC50 of 124 nM and 234 nM, respectivey, and has low activity against FGFR1 with IC50 of 5.294 μM. [1] XL184 at low concentration (0.1-0.5 μM) is sufficient to induce marked inhibition of constitutive and inducible Met phosphorylation and its resultant downstream signaling in MPNST cells, and inhibit HGF-induced MPNST cell migration and invasion. XL184 also induces marked inhibition of Met and VEGFR2 phosphorylation in cytokine-stimulated human umbilical vein endothelial cells (HUVECs). Although XL-184 has no significant effect on MPNST cell growth at 0.1 μM, XL184 at 5-10 μM significantly inhibits the MPNST cell growth. [2]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
E98NT  MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1qxdVAvODFvMUCg{txO M17VVmROW09? M3nIbWlEPTB;OEmgcm0> NXfWSZlGOjN2OESwNFY>
SNU-5  NVPINVBxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jB[GlEPTB;IEG5JI5O NXLnWWlCOjF7Mk[xPVE>
Hs746T  MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHUTWM2OD17Lkmgcm0> MnP2NlE6OjZzOUG=
SNU-1  M{LxcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1Hp[mlEPTB;NUKyN{BvVQ>? NEj6T|czOTl{NkG5NS=>
SNU-16 NGXPeZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGC1dI1KSzVyPUGxOFkhdk1? M4\IdlIyQTJ4MUmx
MDA-MB-231 MnvlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRSB4NEKxJI5O MmTQNlE6OjZzOUG=
U87MG M3TLZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInnT|JKSzVyPUG4OVEhdk1? M17sRVIyQTJ4MUmx
H441  MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTJzN{CwJI5O NYfL[GVIOjF7Mk[xPVE>
H69 M2ntZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fvcWlEPTB;MkCyNFAhdk1? MVyyNVkzPjF7MR?=
PC3 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTFyOECwJI5O MU[yNVkzPjF7MR?=
MTC-TT NUjQOoNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInFb|NKSzVyPUCuNFQhMyByLkCzJO69VQ>? M1juVFIyPDdyOUm1
MZ-CRC NYXoeo5rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRiB3IN88US=> NGTZV|MzOTR5MEm5OS=>
TPC-1 M3L0bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rWWmlEPTB;MD6wOkAsKDBwMEKg{txO M2foOlIyPDdyOUm1

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アッセイ
Methods Test Index PMID
Western blot
p-MET(Y1234/1235) / MET / p-EGFR(Y1068) / EGFR / p-Gab1(Y627) / Gab1 / p-AKT(S473) / p-ERK / p-EIF4E; 

PubMed: 29188469     


MET kinase inhibitors but not emibetuzumab inhibited MET signaling pathway in Hs746t cells in vitro by western blot analysis. Hs746t cells were treated for 24 h with 133 nM (20 μg/ml) or 667 nM (100 μg/ml) emibetuzumab or MET kinase inhibitors (merestinib, PF04217903, crizotinib, cabozantinib) at 15.6, 62.5, 250 or 1000 nM.

p-MET / p-ERK / p-AKT; 

PubMed: 29520051     


Western blot analysis of cellular pathways modifications after CBZ 5 μM treatment in HOS, MG-63, Saos-2 and U-2 OS cells; (A) CBZ 5 μM inhibits c-MET phosphorilation after 1 hour of treatment; downstream ERK activation kinetic adopts a sigmoidal shape in all OS cell lines, whereas AKT activation is strongly inhibited in HOS, Saos-2 and U-2OS, but not in MG-63 cells.

29188469 29520051
Immunofluorescence
α-tubulin; 

PubMed: 29520051     


Immunostaining of mitotic spindle in control and CBZ 5 μM treated HOS cells using a monoclonal antibody against α-tubulin (in green); white arrows indicate the mitotic spindle poles; control cells show normal bipolar spindles during metaphase formation, whereas treated cells show tripolar spindles during prometaphase (II), metaphase (III) and anaphase (IV); bar scale = 10 μm.

29520051
Growth inhibition assay
Cell viability; 

PubMed: 23661005     


Cells were left untreated or were treated with 5, 7.5 or 10 μM cabozantinib (XL184). Seventy-two hours later viability was detected by MTT-assay and apoptosis by staining with annexinV-FITC followed by FACS-analysis.

23661005
体内試験 XL184 treatment at 30 mg/kg in RIP-Tag2 mice with spontaneous pancreatic islet tumors disrupts 83% of the tumor vasculature, reduces pericytes and empty basement membrane sleeves, causes widespread intratumoral hypoxia and extensive tumor cell apoptosis, and slows regrowth of the tumor vasculature after drug withdrawal, more significantly compared with XL999 that blocks VEGFR but not c-Met, leading to only 43% reduction in vascularity, suggesting that concurrent inhibition of VEGFR and other functionally relevant receptor tyrosine kinases (RTK) amplifies angiogenesis inhibition. XL184 also decreases invasiveness of primary tumors and reduces metastasis. [1] XL184 at 30 mg/kg/day significantly abrogates human MPNST xenografts growth and metastasis in SCID mice. [2] Administration of XL184 induces dose-dependent inhibition of tumor growth in breast, lung, and glioma tumor models, in association with decreased tumor and endothelial cell proliferation as well as increased apoptosis. A single oral dose of XL184 is sufficient to induce sustained tumor growth inhibition in MDA-MB-231 tumor-bearing mice and C6 tumor-bearing rats at 100 mg/kg and 10 mg/kg, respectively. [3]

お薦めの試験操作(参考用のみ)

細胞試験:

[2]

- 合併
  • 細胞株: ST88-14, STS26T, and MPNST724
  • 濃度: Dissolved in DMSO, final concentrations ~10 μM
  • 反応時間: 48 hours
  • 実験の流れ:

    Cells are exposed to various concentrations of XL184 for 48 hours. Cell growth is determined by MTS assays using CellTiter96 Aqueous Non-Radioactive Cell Proliferation Assay kit. Absorbance is measured at a wavelength of 490 nm, and the absorbance values of treated cells are presented as a percentage of the absorbance of untreated cells.


    (参考用のみ)
動物試験:

[1]

- 合併
  • 動物モデル: RIP-Tag2 transgenic mice in a C57BL/6 background with spontaneous pancreatic islet tumors
  • 製剤: Suspended at a concentration of 5 mg/mL in sterile saline or water
  • 投薬量: ~60 mg/kg
  • 投与方法: Oral gavage
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (199.39 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 501.51
化学式

C28H24FN3O5

CAS No. 849217-68-1
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck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

希釈の計算式

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

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

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

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04091750 Not yet recruiting Drug: Nivolumab|Drug: Ipilimumab|Drug: Cabozantinib Melanoma Georgetown University|MedStar Franklin Square Medical Center|Hackensack Meridian Health|Exelixis October 2019 Phase 2
NCT04066595 Not yet recruiting Drug: Cabozantinib Urothelial Carcinoma Johannes Gutenberg University Mainz|Interdisciplinary Center Clinical Trials (IZKS) University Medical Center Mainz September 30 2019 Phase 2
NCT03964337 Not yet recruiting Drug: Cabozantinib|Procedure: Radical Prostatectomy Prostate Cancer|Prostate Cancer Adenocarcinoma|Non-Metastatic Duke University|Exelixis September 2019 Phase 2
NCT03963206 Recruiting Drug: Cabozantinib group|Other: ECG Hepatocellular Carcinoma Hospices Civils de Lyon September 9 2019 Phase 4
NCT03696407 Completed -- Advanced Renal Cell Carcinoma Ipsen December 20 2018 --

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID