BMS-777607

製品コードS1561

BMS-777607化学構造

分子量(MW):512.89

BMS-777607は一種のMet関連の阻害剤で、無細胞実験でc-Met、Axl、RonとTyro3に作用する時のIC50値が3.9 nM、1.1 nM、1.8 nMと4.3 nMにそれぞれ分かれることです。BMS-777607は、Met関連ターゲットに作用する選択性はLck、VEGFR-2とTrkA/Bに作用する選択性より40倍が高くなって、他の受容体と非受容体のキナーゼに作用する選択性より500倍が高くなります。臨床 1/2期。

サイズ 価格(税別)  
JPY 41500.00
JPY 19920.00
JPY 34860.00
JPY 111220.00

カスタマーフィードバック(6)

  • Numbers of clonogenic cells from L3.6pl cells and CSCs+24/44/ESAin duplicate were counted. Clonogenic growth from the cell control was set as 100%.

    Mol Cancer Ther 2014 13(1), 37-48. BMS-777607 purchased from Selleck.

    The inhibitory effect of BMS-777607 on survival and proliferation of L3.6pl and CSCs+24/44/ESA was determined by the clonogenic assay. Briefly, L3.6pl cells (6,000 cells/well) in minimum essential media (MEM) with 5% FBS were cultured in duplicate in a 24-well plate and then treated with different amounts of BMS-777607 for 12 days. CSCs+24/44/ESA in stem cell culture media were incubated for 18 days in the ultra-low attachment culture plate coated with a thin layer of 0.2% of agarose to facilitate cell anchored growth. Clonogenic cells were stained with Hema-3 staining solution (Fisher Scientific), photographed using an Olympus BK71 microscope equipped with CCD camera, and counted. The number of clonogenic growth from individual groups is presented.

    Mol Cancer Ther 2014 13(1), 37-48. BMS-777607 purchased from Selleck.

  • Mol Oncol 2013 10.1016/j.molonc.2013.12.014. BMS-777607 purchased from Selleck.

    BMS-777607 increases p21/WAF1 and survivin expression but down-regulates Rb expression. T-47D and ZR-75-1 cells (2×106 cells in 60 mm diameter culture dish) were treated with 5 mM BMS-777607 for different time intervals. Cellular proteins (50 mg per sample) from cell lysates were subjected to Western blot analysis using individual antibodies specific to p53, p21/WAF1, survivin, regular and phospho-Rb. B-actin was used as the loading control.

    Mol Oncol 2013 8, 469-82. BMS-777607 purchased from Selleck.

  • Effect of BMS-777607 on growth and survival of breast cancer cells. A, the effect of BMS-777607 on survival and proliferation of MCF-7, ZR-75-1, and T-47D cells was determined by clonogenic assay. Briefly, cells (8,000 cells per well) in RPMI-1640 with 5% FBS were cultured in duplicate in a 24-well plate and then treated with different amounts of BMS-777607 for 10 days. Clonogenic cells were stained with Hema-3 staining solution (Fisher Scientific) and photographed using an Olympus BK71 microscope equipped with CCD camera. B, numbers of clonogenic cells in duplicate from 3 cell lines were counted.

    Acta Pharmacol Sin 2013 34, 1545-53. BMS-777607 purchased from Selleck.

    Effect of MEK inhibitor BMS-777607 in A549 cells. A549 cells were incubated with increasing concentrations of BMS-777607 for 2 h. The cell lysates were harvested and phosphorylation of indicated proteins was determined by Western blotting.

    2014 Dr.Wang from Southern Medical Hospital. BMS-777607 purchased from Selleck.

製品安全説明書

c-Met阻害剤の選択性比較

生物活性

製品説明 BMS-777607は一種のMet関連の阻害剤で、無細胞実験でc-Met、Axl、RonとTyro3に作用する時のIC50値が3.9 nM、1.1 nM、1.8 nMと4.3 nMにそれぞれ分かれることです。BMS-777607は、Met関連ターゲットに作用する選択性はLck、VEGFR-2とTrkA/Bに作用する選択性より40倍が高くなって、他の受容体と非受容体のキナーゼに作用する選択性より500倍が高くなります。臨床 1/2期。
特性 A potent inhibitor of the Met family, and >40-fold selectivity vs. Lck, VEGFR2, and TrkA/B and >500-fold selective vs. other receptor and non-receptor kinases.
ターゲット
Axl [1]
(Cell-free assay)
RON [1]
(Cell-free assay)
Met [1]
(Cell-free assay)
Tyro3 [1]
(Cell-free assay)
Mer [1]
(Cell-free assay)
1.1 nM 1.8 nM 3.9 nM 4.3 nM 14 nM
体外試験

BMS-777607 is a selective ATP-competitive Met kinase inhibitor which potently blocks the autophosphorylation of c-Met with IC50 of 20 nM in GTL-16 cell lysates, and demonstrates selective inhibition of proliferation in Met-driven tumor cell lines, such as GTL-16 cell line, H1993 and U87. [1] BMS-777607 inhibits hepatocyte growth factor (HGF)-triggered c-Met autophosphorylation with IC50 of <1 nM in PC-3 and DU145 prostate cancer cells. BMS 777607 has little effect on tumor cell growth, but exhibits inhibitory effect on HGF-induced cell scattering in PC-3 and DU145 cells, with almost complete inhibition at 0.5 μM. BMS 777607 also suppresses stimulated cell migration and invasion in a dose-dependent fashion (IC50 < 0.1 μM) in both cell lines. [2] Application of BMS 777607 (~10 μM) to the highly metastatic murine KHT cells for 2 hours potently eliminates basal levels of autophosphorylated c-Met with IC50 of 10 nM without affecting the total c-Met, leading to dose-dependent inhibition of phosphorylation of downstream signaling molecules including ERK, Akt, p70S6K and S6. Treatment with BMS-777607 (~1 μM) for 24 hours potently inhibits the KHT cell scatter, motility and invasion at doses in the nanomolar range which consists with MET gene knockdown, and modestly affects cell proliferation and colony formation. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
GTL-16 M3P5NWtqdmG|ZTDhd5NigQ>? MXrEUXNQ NG\o[m5qdmirYnn0d{BO\XRia3nuZZNmKHerdHigTWM2OCCxZjCxNFAhdk1? MVuxPVI3ODdzMR?=
H1993 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MXv+NVAh|ryP NFP4bVNFVVOR MlHiTWM2OD1zNUCgcm0> M3PnT|E6OjZyN{Gx
U87 NGrRcHVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXTuRmVwhjFyIN88US=> M4fXfWROW09? NGnCPWhKSzVyPUG2NEBvVQ>? M3rQU|E6OjZyN{Gx
PC-3 MYHGeY5kfGmxbjDhd5NigQ>? MlTMNE4yKM7:TR?= M2nYdGROW09? MUXlfIhq[mm2czDpcohq[mm2b4L5JIVn\mWldDDvckBJT0ZvaX7keYNm\CClZXzsJJNk[XS2ZYLpcoc> NF[zZ3UzODVzNUm0Ny=>
DU145 MWnGeY5kfGmxbjDhd5NigQ>? Mo\UNE4yKM7:TR?= NF\t[plFVVOR MljO[ZhpcWKrdIOgbY5pcWKrdH;yfUBm\m[nY4Sgc44hUEeILXnu[JVk\WRiY3XscEB{[2G2dHXybY5o MYGyNFUyPTl2Mx?=
PC-3 MkjOSpVv[3Srb36gZZN{[Xl? MkHmNE4xOSEQvF2= M2TJbmROW09? M3vMPZN2eHC{ZYPz[ZMhUEeILXnu[JVk\WRiY3XscEBucWe{YYTpc44> M2\rPFIxPTF3OUSz
DU145 M{[ydWZ2dmO2aX;uJIF{e2G7 NIPWOWwxNjBzIN88US=> M4nqfWROW09? MljCd5VxeHKnc4Pld{BJT0ZvaX7keYNm\CClZXzsJI1q\3KjdHnvci=> NYDhWZVbOjB3MUW5OFM>
PC-3 MVTGeY5kfGmxbjDhd5NigQ>? M33lO|AvOSEQvF2= NV7MN3hxTE2VTx?= M1OzOIlueGGrcoOgTGdHNW2nZHnheIVlKGOnbHygbY53[XOrb36= MlHPNlA2OTV7NEO=
DU145 MUjGeY5kfGmxbjDhd5NigQ>? Mm[1NE4yKM7:TR?= M1Xqc2ROW09? NVLYO|dvcW2yYXnyd{BJT0ZvbXXkbYF1\WRiY3XscEBqdn[jc3nvci=> MXiyNFUyPTl2Mx?=
PC-3 M{LYRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYL+NVAh|ryP NInMPW5FVVOR NWTVdXc4emWmdXPld{Bk\WyuIIDyc4xq\mW{YYTpc44> MmW1NlA2OTV7NEO=
KHT NIniNmNMcW6jc3WgZZN{[Xl? NWLIenVXTE2VTx?= M3W4UoJtd2OtczD0bIUh[y2PZYSgd4lodmGuaX7nJJBifGi5YYmge4l1cCCLQ{WwJI9nKDFyIH7N NXnvOpVKOjJ{OE[1NlM>
KHT NX21T3lyTnWwY4Tpc44h[XO|YYm= NVfKXWFWhjFizszN NHLBd4hFVVOR MVzwdoV3\W62czDzdI9vfGGwZX;1d{BMUFRiY3XscEB{[2G2dHXybY5oKHerdHigTWM2OCCxZjCwMlEuOC53IN88US=> NG\j[3gzOjJ6NkWyNy=>
KHT NVrIWllITnWwY4Tpc44h[XO|YYm= MoroglAvPSEQvF2= M1vpbmROW09? MUjpcohq[mm2czDj[YxtKG2rZ4LheIlwdg>? NYfhZW1HOjJ{OE[1NlM>
KHT NXLwN|ZVTnWwY4Tpc44h[XO|YYm= NEj6XZh,OC53IN88US=> M330OWROW09? MmrXbY5pcWKrdIOgZ4VtdCCrbo\hd4lwdg>? NHPhPYgzOjJ6NkWyNy=>
KHT MV;Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYTqSJpThjFyIN88US=> MWjEUXNQ M33ObIlvcGmkaYTzJGtJXCClZXzsJJBzd2yrZnXyZZRqd25? NGL2ZnozOjJ6NkWyNy=>
T-47D MlPsS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWjhdGJ{hjVizszN NHPvO|NFVVOR M4fYdYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> M13wNlI{PDZ6NUK5
ZR-75-1 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWmxNGpzhjVizszN NH\YfGNFVVOR M3W1WolvcGmkaYTzJINmdGxicILvcIln\XKjdHnvci=> NFvZWmQzOzR4OEWyPS=>
T-47D NVjYUXJbTnWwY4Tpc44h[XO|YYm= M3jnblExKM7:TR?= MYfEUXNQ NX64N3JsUW6mdXPld{Bxd2y7cHzvbYR6KGK7IEi2JEU> M2nTU|I{PDZ6NUK5
ZR-75-1 NH;WVYlHfW6ldHnvckBie3OjeR?= M2T3elExKM7:TR?= NFrxc21FVVOR MUPJcoR2[2W|IIDvcJlxdG:rZImgZpkhQDhn NYizdWdTOjN2Nki1Nlk>
T-47D MmnSSpVv[3Srb36gZZN{[Xl? M1KySFExKM7:TR?= NE\yUZJFVVOR M{fSRolvcGmkaYTzJGFWWktvQjDmeY5kfGmxbjDhcoQhcW6mdXPld{BqfHNicILveIVqdiCmZXfyZYRifGmxbh?= NULReIp7OjN2Nki1Nlk>
CHRF NWLrU|ZwTnWwY4Tpc44h[XO|YYm= MVOxNEDPxE1? NUi0WJVmTE2VTx?= MmmybY5pcWKrdIOgZ4VtdCCmaY\pd4lwdg>? M3LFR|I2OzB2OUCw
HPDE MX3GeY5kfGmxbjDhd5NigQ>? NF[5[lMyOCEQvF2= Ml\ZSG1UVw>? MlntZoxw[2u|IHPvcpN1cXS3dHn2[UBi[3SrdnH0bY9vKGGwZDDk[YNz\WG|ZXSgRWtVKHOrZ37hcIlv\w>? MWSyOlQ4PzNzNB?=
U118MG NGf5b3JMcW6jc3WgZZN{[Xl? MWP+N{DPxE1? M1i4e2ROW09? MlTSZoxw[2u|IFHYUEBxcG:|cHjvdplt[XSrb36= MoPTNlY5PDh3MkS=
SF126 MXvLbY5ie2ViYYPzZZk> MX\+N{DPxE1? M13jfWROW09? M4Dyb4Jtd2OtczDBXGwheGixc4Doc5J6dGG2aX;u M13DcFI3QDR6NUK0
U118MG MmnNR5l1d3irY3n0fUBie3OjeR?= MYixNk42KM7:TR?= MVTEUXNQ Ml:y[IVkemWjc3XzJIdtcW:vYTDj[YxtKH[rYXLpcIl1gQ>? MY[yOlg1QDV{NB?=
SF126 NGnEXoJEgXSxeHnjbZR6KGG|c3H5 NVvJUpU5OTJwNTFOwG0> NV7VS4ZzTE2VTx?= M1jXeIRm[3KnYYPld{BodGmxbXGgZ4VtdCC4aXHibYxqfHl? M2DRd|I3QDR6NUK0
U118MG MlzYRZBweHSxc3nzJIF{e2G7 NIPQTpIyOi53IN88US=> MYTEUXNQ NEXVS5VqdmS3Y3XzJIdtcW:vYTDj[YxtKGGyb4D0c5Nqew>? M1\4fVI3QDR6NUK0
SF126 NEL0T5hCeG:ydH;zbZMh[XO|YYm= MWmxNk42KM7:TR?= NInpVodFVVOR NUfhc5FYcW6mdXPld{BodGmxbXGgZ4VtdCCjcH;weI9{cXN? NFfERW0zPjh2OEWyOC=>
U118MG MoHUSpVv[3Srb36gZZN{[Xl? M4f4flEzNjVizszN MojISG1UVw>? M3nkOIJtd2OtczDncIlwdWFiY3XscEBucWe{YYTpc44h[W6mIHnueoF{cX[nIHfyc5d1cCCyYYT0[ZJv M1;kdFI3QDR6NUK0
SF126 NV;JOZRlTnWwY4Tpc44h[XO|YYm= M1TCW|EzNjVizszN M4HkdmROW09? NVHSd2Z6[myxY3vzJIdtcW:vYTDj[YxtKG2rZ4LheIlwdiCjbnSgbY53[XOrdnWg[5Jwf3SqIIDheJRmem5? MX[yOlg1QDV{NB?=

多くの細胞株試験データを見る場合、クリックしてください

体内試験 Oral administration of BMS 777607 (6.25-50 mg/kg) significantly reduces tumor volumes of the GTL-16 human tumor xenografts in athymic mice with no observed toxicity. [1] Administration of BMS 777607 (25 mg/kg/day) decreases the number of KHT lung tumor nodules (28.3%), improves the morphological hemorrhage, and significantly impairs the metastatic phenotype in the 6-8 week-old female C3H/HeJ mice injected with rodent fibrosarcoma KHT cells without apparent systemic toxicity compared to the control treatment. A low dose of BMS 777607 (10 mg/kg) also offers a mild but not significant inhibition of lung nodule formation compared to the vehicle control. [3]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[4]
+ 展開

Met Kinase Assay:

The kinase reaction consists of baculovirus expressed GST-Met, 3 μg of poly(Glu/Tyr), 0.12 μCi 33P γ-ATP, 1 μM ATP in 30 μL of kinase buffer (20 mM Tris-Cl, 5 mM MnCl2, 0.1 mg/mL BSA, 0.5 mM DTT). Reactions are incubated for 1 hour at 30 °C and stopped by the addition of cold trichloroacetic acid (TCA) to a final concentration of 8%. TCA precipitates are collected onto GF/C unifilter plates using a Filtermate universal harvester, and the filters are quantitated using a TopCount 96-well liquid scintillation counter. Dose response curves are generated to determine the concentration required to inhibit 50% of substrate phosphorylation (IC50). BMS 777607 is dissolved at 10 mM in dimethylsulfoxide (DMSO) and evaluated at 10 concentrations, in duplicate.
細胞試験: [3]
+ 展開
  • 細胞株: Rodent fibrosarcoma KHT cells
  • 濃度: Dissolved in DMSO as a stock solution (10 mM), final concentration ~10 μM.
  • 反応時間: 2, 24 and 96 hours
  • 実験の流れ: KHT cells are exposed to serial dilution of BMS 777607 for 96 hours, then the MTT assay and trypan blue exclusion are used for the determination of cell proliferation and cell death, respectively. KHT cell colonies are incubated with BMS 777607 for 24 hours and then stained with crystal violet (0.1%) and photographed for the assessment of cell scattering. 2 mm scratch on the confluent KHT cell monolayer is made using a sterilized 1 ml pipette tip followed by treated with BMS-777607 for 24 hours, then the number of cells that have migrated into the denuded area is counted on 4 random fields for the evaluation of cell migration. For the examination of cell invasion, the commercial transwell inserts (8 μm pore membrane) pre-loaded with Matrigel are incubated with serum-free medium in the presence or absence of BMS 777607 at 37 °C for 2 hours to allow rehydration of Matrigel. Then cells suspended in serum-free medium are loaded onto the top chamber (5 × 103/insert) and complete medium (containing 10% FBS) is used in the lower chamber as a chemoattractant. After incubation for 24 hours, the Matrigel is removed and the inserts are stained with crystal violet. Invaded cells on the underside of the filter are photographed and counted.
    (参考用のみ)
動物試験:[3]
+ 展開
  • 動物モデル: Rodent fibrosarcoma KHT cells are established in female C3H/HeJ mice.
  • 製剤: Dissolved in DMSO as a stock solution (10 mM).
  • 投薬量: 10-25 mg/kg.
  • 投与方法: Oral gavage once daily.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 47 mg/mL (91.63 mM)
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
4% DMSO+45% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 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。

化学情報

分子量 512.89
化学式

C25H19ClF2N4O4

CAS No. 1025720-94-8
保管
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

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

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01721148 Completed Malignant Solid Tumour Aslan Pharmaceuticals October 2012 Phase 1
NCT00605618 Completed Advanced Solid Tumors Bristol-Myers Squibb March 2008 Phase 1|Phase 2

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題1:

    What formulation can we use to dissolve S1561 for mice in vivo study?

  • 回答:

    S1561 BMS-777607 in 1% DMSO+30% polyethylene glycol+1% Tween 80 at 30 mg/ml is a suspension. It is fine for oral gavage. If you are going to use it for injection, please try the following vehicle: 4% DMSO+30% PEG 300+ddH2O. BMS-777607 can be dissolved in it at 5 mg/ml as a clear solution.

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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