成人免费xx,国产又黄又湿又刺激不卡网站,成人性视频app菠萝网站,色天天天天

  2. Protein Tyrosine Kinase/RTK
  3. VEGFR c-Met/HGFR
  4. Pamufetinib

Pamufetinib (TAS-115) 是一種有效的 VEGFR 和 c-Met/HGFR 抑制劑，能夠抑制 rVEGFR2 和 rMET 的活性，IC50 值分別為 30 和 32 nM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

我們將采用定制合成服務(wù)的方式為您快速提供所需產(chǎn)品和技術(shù)服務(wù)

Pamufetinib Chemical Structure

Pamufetinib Chemical Structure

CAS No. : 1190836-34-0

1.  客戶無需承擔(dān)相應(yīng)的運(yùn)輸費(fèi)用。

2.  同一機(jī)構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機(jī)構(gòu)（單位）一年內(nèi)

     可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價(jià)格 是否有貨 數(shù)量
5 mg ￥1440
In-stock
10 mg ￥2080
In-stock
25 mg ￥3600
In-stock
50 mg ￥5400
In-stock
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Other Forms of Pamufetinib:

查看 VEGFR 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Pamufetinib (TAS-115) is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.

IC50 & Target[1]

VEGFR2

30 nM (IC50)

c-Met

32 nM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
HUVEC GI50
> 10 μM
Compound: TAS-115
Cytotoxicity against HUVEC assessed as inhibition of VEGF-independent growth after 72 hrs by CellTiter-Glo method
Cytotoxicity against HUVEC assessed as inhibition of VEGF-independent growth after 72 hrs by CellTiter-Glo method
[PMID: 26717201]
體外研究
(In Vitro)

Pamufetinib is ATP antagonism with inhibition constant (Ki) values against rVEGFR2 and rMET of 12 and 39 nM, respectively. Pamufetinib inhibits the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors. Pamufetinib induces less damage in various normal cells than do other VEGFR inhibitors[1]. Pamufetinib does not affect the growth of PC-9 or HCC827 cells at concentrations less than 10 μM; however, the combined use of Pamufetinib with erlotinib reverses HGF-induced resistance in the cell lines in a concentration-dependent manner. Pamufetinib inhibits VEGF production by cancer cells and endothelial proliferation[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Pamufetinib (50 mg/kg/d) completely prevents tumor growth during the treatment period. Pamufetinib (200 mg/kg/d) induces a 48% regression from the initial tumor volume in MET-amplified human cancer transplanted models. The estimated 50% effective dose (ED50) of Pamufetinib in this model is 8 mg/kg/d. Pamufetinib significantly prolongs survival of these mice when administered at doses of 50 or 200 mg/kg/d[1]. Pamufetinib inhibits angiogenesis in PC-9/HGF tumors in vivo. Moreover, the doublet erlotinib and Pamufetinib successfully inhibit PC-9/HGF tumor growth and delay tumor regrowth associated with sustained tumor vasculature inhibition even after cessation of the treatment[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

518.56

Formula

C27H23FN4O4S
CAS 號
性狀

固體

顏色

Off-white to light yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 25 mg/mL (48.21 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.9284 mL 9.6421 mL 19.2842 mL
5 mM 0.3857 mL 1.9284 mL 3.8568 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻(xiàn)
Kinase Assay
[1]

Enzyme inhibition studies are performed using a mobility shift assay. Briefly, 0.3 μg/mL of recombinant MET (rMET, N-terminal glutathione S-transferase (GST) Tag) and 1.5 μM of FL-Peptide 2 or 2 μg/mL of recombinant VEGFR2 (rVEGFR2, amino acid 790-end, N-terminal 6His Tagged) and 1.5 μM of FL-Peptide 22 are added to a 25 μL mixture containing 1/2 the Michaelis constant (Km) level of ATP, 100 mM of HEPES (pH 7.2), 0.003% (w/v) Brij35, 0.04% (v/v) Tween 20, 10 mM of MgCl2, 1 mM of dithiothreitol, a Complete Mini EDTA-free Protease Inhibitor Cocktail Tablet, and a PhosSTOP Phosphatase Inhibitor Cocktail Tablet, with the addition of 0.05% (w/v) CHAPSO only in the case of rVEGFR2. The reaction mixture is incubated for 90 minutes at 28°C and is stopped by the addition of 15 mM of EDTA. Phosphorylated peptide is calculated using a LabChip EZ Reader, Version 2.1.82.0 (UCC Version: 1.96, CCD Version: 102). On the basis of the amount of phosphorylated peptide formed in the control well and the drug-treated well, the 50% inhibitory concentration (IC50) is calculated using a logistic regression analysis. A total of 192 kinase panel assays is performed using the ProfilerPro Kit 1-8 and is analyzed using a mobility shift assay.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

Cell growth is measured using the MTT dye reduction method. Tumor cells are plated into 96-well plates at a density of 2×103 cells/100 mL RPMI-1640 medium with 10% FBS per well. After 24-hour incubation, various reagents are added to each well, and the cells incubated for a further 72 hours, followed by the addition of 50 μL of MTT solution (2 mg/mL) to each well and incubation for 2 hours. The media containing MTT solution is removed, and the dark blue crystals are dissolved by adding 100 mL of dimethyl sulfoxide. The absorbance of each well is measured with a microplate reader at test and reference wavelengths of 550 and 630 nm, respectively. The percentage of growth is shown relative to untreated controls. Each reagent concentration is tested at least in triplicate during each experiment, and each experiment is conducted at least three times.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

A SC-9 fragment is implanted subcutaneously into the right abdomen of each mouse via a trocar. Suspensions of MKN45 cells are prepared and are implanted subcutaneously into the right abdomen of each nude mouse. The tumor volume (TV, mm3) is calculated. The TAS-115 dose levels are set at 12.5, 50, and 200 mg/kg/d. The dose level for sunitinib is set at 40 mg/kg/d; this dose is equivalent to the maximum tolerated dose (MTD). Oral drug treatment is continued for 14 or 42 consecutive days for the chronic dosing in the SC-9 xenograft model. During the treatment period, TV and body weight are measured twice per week.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9284 mL 9.6421 mL 19.2842 mL 48.2104 mL
5 mM 0.3857 mL 1.9284 mL 3.8568 mL 9.6421 mL
10 mM 0.1928 mL 0.9642 mL 1.9284 mL 4.8210 mL
15 mM 0.1286 mL 0.6428 mL 1.2856 mL 3.2140 mL
20 mM 0.0964 mL 0.4821 mL 0.9642 mL 2.4105 mL
25 mM 0.0771 mL 0.3857 mL 0.7714 mL 1.9284 mL
30 mM 0.0643 mL 0.3214 mL 0.6428 mL 1.6070 mL
40 mM 0.0482 mL 0.2411 mL 0.4821 mL 1.2053 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

您最近查看的產(chǎn)品:

Your information is safe with us. * Required Fields.

   產(chǎn)品名稱：

  

* 需求量：

* 客戶姓名：

 

* Email：

* 電話：

 

* 公司或機(jī)構(gòu)名稱：

   留言給我們：

Bulk Inquiry

Inquiry Information

產(chǎn)品名稱：
Pamufetinib
目錄號：
HY-12423
需求量：