CP-724714

製品コードS1167

CP-724714化学構造

分子量(MW):469.53

CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2.

サイズ 価格(税別)  
JPY 38180.00
JPY 19920.00
JPY 36520.00
JPY 78020.00
JPY 127820.00

カスタマーフィードバック(6)

  • For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of CP-724714 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.

    2012 Dr. Yong-Weon Yi from Georgetown University Medical Center. CP-724714 purchased from Selleck.

    Cancer Res 2014 74(1), 341-52. CP-724714 purchased from Selleck.

  • Cancer Res 2013 74(1), 341-52. CP-724714 purchased from Selleck.

    VX-702, a p38 inhibitor, sensitizes HT29, HCT116 and DLD-1 colorectal cell lines to drugs in the presence of conditioned media from CAFs. Different concentrations of inhibitor were used in a range of 25-400 ng/ml. Relative values of the survival fraction are calculated from each VX-702 concentration relative to the corresponding VX-702 concentration without oxaliplatin or 5FU. Asterisks denote statistically significant differences between VX-702-treated groups and oxaliplatin or 5FU as single agents.

    Oncotarget, 2016, 7(37):59766-59780. CP-724714 purchased from Selleck.

  • After starved in primary serum, rat Schwann cells was stimulated for 15 minutes with a soluble form of neuregulin 1 type III to activate ErbB2. Activity of ErbB2 was determined by phosphorylation on Tyr1248. CP-724714 was applied at different concentrations, but achieved strong RTK inhibition already at very low concentrations.

    2012 Reto Baumann from ETH Zurich. CP-724714 purchased from Selleck.

    CP-724714 purchased from Selleck.

製品安全説明書

HER2阻害剤の選択性比較

生物活性

製品説明 CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, >640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc in cell-free assays. Phase 2.
ターゲット
HER2/ErbB2 [1]
(Cell-free assay)
10 nM
体外試験

CP-724,714 is marked selectively against EGFR with IC50 of 6.4 μM. CP-724,714 is >1,000-fold less potent for IR, IGF-1R, PDGFRβ, VGFR2, abl. Src, c-Met c-jun NH2-terminal kinase (JNK)-2, JNK-3, ZAP-70, cyclin-dependent kinase (CDK)-2, and CDK-5. CP-724,714 potently reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain with IC50 of 32 nM, but is markedly less potent against EGFR in transfected NIH3T3 cells. CP-724,714 sensitively inhibits the proliferation of erbB2-amplified cells including BT-474 and SKBR3, with IC50 of 0.25 and 0.95 μM. CP-724,714 induces the accumulation of cells in G1 phase and a marked reduction in S-phase in BT-474 cells at 1 μM. [1] CP-724,714 likely exerts its hepatotoxicity via both hepatocellular injury and hepatobiliary cholestatic mechanisms. CP-724,714 displays inhibition of cholyl-lysyl fluorescein and taurocholate (TC) efflux into canaliculi in cryopreserved and fresh cultured human hepatocytes, respectively. CP-724,714 inhibits TC transport in membrane vesicles expressing human bile salt export pump with IC50 of 16 μM and inhibits the major efflux transporter in bile canaliculi, MDR1, with IC50 of ~28 μM. [2]

体内試験 CP-724,714 (25 mg/kg) is rapidly absorbed after p.o. administration and causes reduction of tumor erbB2 receptor phosphorylation after dosing in FRE-erbB2 or BT-474 xenografts. CP-724,714 induces apoptosis in FRE-erbB2 xenograft–bearing (s.c.) mice and shows 50% tumor growth inhibition at 50 mg/kg, without weight loss or mortality. CP-724,714 also has great antitumor activity in MDA-MB-453, MDA-MB-231, LoVo (colon), and Colo-205 (colon) xenografts. Furthermore, CP-724,714 (30 or 100 mg/kg) reduces the extracellular signal–regulated kinase and Akt phosphorylation in BT-474 xenografts. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

Kinase assays:

Recombinant erbB2 (amino acid residues 675-1255) and EGFR (amino acid residues 668-1211) intracellular domains are expressed in baculovirus-infected Sf9 cells as glutathione S-transferase fusion proteins. The proteins are purified by affinity chromatography on glutathione Sepharose beads for use in the assay. Nunc MaxiSorp 96-well plates are coated by incubation overnight at 37 °C with 100 μL/well of 0.25 mg/mL poly(Glu:Tyr, 4:1), PGT in PBS. Excess PGT is removed by aspiration and the plate is washed 3 times with wash buffer (0.1% Tween 20 in PBS). The kinase reaction is performed in 50 μL of 50 mm HEPES (pH 7.4) containing 125 mm sodium chloride, 10 mm magnesium chloride, 0.1 mm sodium orthovanadate, 1 mm ATP, and ∼15 ng of recombinant protein. Inhibitors in DMSO are added; the final DMSO concentration is 2.5%. Phosphorylation is initiated by addition of ATP and proceeded for 6 min at room temperature, with constant shaking. The kinase reaction is terminated by aspiration of the reaction mixture and washing four times with wash buffer. Phosphorylated PGT is measured after a 25-min incubation with 50 μL/well HRP conjugated-PY54 antiphosphotyrosine antibody, diluted to 0.2 μg/mL in blocking buffer (3% BSA, 0.05% Tween 20 in PBS). Antibody is removed by aspiration and the plate is washed four times with wash buffer. The colorimetric signal is developed by addition of 50 μL/well Tetramethylbenzidine Microwell Peroxidase Substrate and stopped by the addition of 50 μL/well 0.09 m sulfuric acid. The phosphotyrosine product formed is estimated by measurement of absorbance at 450 nm. The signal for controls is typically A0.6–1.2, with essentially no background in wells without ATP, kinase protein, or PGT, and is proportional to the time of incubation for 6 min.
細胞試験: [1]
+ 展開
  • 細胞株: ZR-75-30, HCC-1419, MDA-MB-175, BT-474, SKBR3, MDA-MB-361, UACC-812, T-47D, MDA-MB-453, MDA-MB-468, CAMA-1, MDA-MB-157, MCF-7, MDA-MB-435, ZR-75-1, BT-20, and MDA-MB-231.
  • 濃度: 0.1 nM - 10 μM.
  • 反応時間: 6 to 7 days.
  • 実験の流れ: Cells are seeded in duplicate at 5~10 × 103 per well in 24-well plates. The day after plating, CP-724,714 is added by titrating over six or more dilutions from 0.1 nM to 10 μM. Control wells without CP-724,714 are seeded as well. Cells are grown for 6 to 7 days, at which time surviving cells are counted. After trypsinization, cells are placed in isotone solution and counted immediately using a Coulter Z2 particle counter. Growth inhibition is calculated [(1− experimental value / control value) × 100] for each concentration. Dose-response curves are repeated at least twice and averaged. IC50 values are calculated using Calcusyn Software.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: FRE-erbB2 BT-474, MDA-MB-453, MDA-MB-231, LoVo (colon), and Colo-205 (colon) xenografts are established in athymic female mice (CD-1 nu/nu).
  • 製剤: 0.5% methylcellulose.
  • 投薬量: ~100 mg/kg.
  • 投与方法: Administered via p.o.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 94 mg/mL (200.2 mM)
Ethanol 94 mg/mL (200.2 mM)
Water 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):
0.5% methylcellulose
混合させたのち直ちに使用することを推奨します。
30 mg/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 469.53
化学式

C27H27N5O3

CAS No. 537705-08-1
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 (g) = 濃度 (mol/L) x 体積 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT00102895 Terminated Breast Neoplasms|Neoplasm Metastasis Pfizer April 2005 Phase 2
NCT00102895 Terminated Breast Neoplasms|Neoplasm Metastasis Pfizer April 2005 Phase 2
NCT00055926 Completed Breast Cancer Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) January 2003 Phase 1
NCT00055926 Completed Breast Cancer Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) January 2003 Phase 1

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

HER2シグナル伝達経路

HER2 Inhibitors with Unique Features

相関HER2製品

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