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  2. Protein Tyrosine Kinase/RTK
  3. Tie VEGFR
  4. NVP-BAW2881

NVP-BAW2881 (BAW2881) 是有效，選擇性的 VEGFR2 抑制劑，IC50 為值9 nM。

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NVP-BAW2881 Chemical Structure

NVP-BAW2881 Chemical Structure

CAS No. : 861875-60-7

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥747
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2 mg ￥500
In-stock
5 mg ￥800
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10 mg ￥1400
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25 mg ￥2700
In-stock
50 mg ￥4400
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100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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  • 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

NVP-BAW2881 (BAW2881) is a potent and selective VEGFR2 inhibitor with an IC50 of 4 nM.

IC50 & Target[1]

VEGFR1

820 nM (IC50)

VEGFR2

9 nM (IC50)

VEGFR3

420 nM (IC50)

Tie2

650 nM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
> 10 μM
Compound: BAW2881
Antiproliferative activity against mouse BaF3 cells expressing ERBB2 V659E mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing ERBB2 V659E mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: BAW2881
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: BAW2881
Antiproliferative activity against mouse BaF3 cells expressing Tel-IGF-1R assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Tel-IGF-1R assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: BAW2881
Antiproliferative activity against mouse BaF3 cells expressing KIT D816V mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing KIT D816V mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: BAW2881
Antiproliferative activity against mouse BaF3 cells expressing Trp-MET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Trp-MET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: BAW2881
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
> 10 μM
Compound: BAW2881
Antiproliferative activity against mouse BaF3 cells expressing NPM-ALK assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing NPM-ALK assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
0.004 μM
Compound: BAW2881
Antiproliferative activity against mouse BaF3 cells expressing Tel-KDR-myc1.3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Tel-KDR-myc1.3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
0.009 μM
Compound: BAW2881
Antiproliferative activity against mouse BaF3 cells expressing Tel-PDGFRbeta assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Tel-PDGFRbeta assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
0.152 μM
Compound: BAW2881
Antiproliferative activity against mouse BaF3 cells expressing PTC3-RET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing PTC3-RET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
4.748 μM
Compound: BAW2881
Antiproliferative activity against mouse BaF3 cells expressing Bcr-ABL assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Bcr-ABL assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
BaF3 IC50
8.271 μM
Compound: BAW2881
Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
[PMID: 26629594]
HUVEC IC50
> 3 μM
Compound: BAW2881
Antiproliferative activity against bFGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
Antiproliferative activity against bFGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
[PMID: 26629594]
HUVEC IC50
0.21 nM
Compound: BAW2881
Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
[PMID: 26629594]
體外研究
(In Vitro)

BAW2881 在CHO細(xì)胞中抑制VEGF驅(qū)動(dòng)的細(xì)胞受體自身磷酸化，其IC50值為4 nM。BAW2881對(duì)有限數(shù)量的激酶具有抑制作用，包括c-RAF、B-RAF、RET、ABL和TIE-2，這些激酶的IC50均在亞微摩爾級(jí)別[1]。NVP-BAW2881對(duì)VEGFR表現(xiàn)出高度選擇性，盡管它也對(duì)Tie2（IC50=650 nM）和RET（IC50=410 nM）顯示出活性。對(duì)于廣泛的一系列其他激酶，NVP-BAW2881的IC50值均大于10 μM。NVP-BAW2881能夠抑制VEGF-A誘導(dǎo)的人臍靜脈內(nèi)皮細(xì)胞（HUVECs）及轉(zhuǎn)染了VEGFR-2的中國(guó)倉(cāng)鼠卵巢細(xì)胞中VEGFR-2的磷酸化，相應(yīng)的IC50值分別為2.9 nM和4.2 nM[2]。

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

在牛皮癬的轉(zhuǎn)基因小鼠模型中，NVP-BAW2881 減少了血液和淋巴管的數(shù)量以及皮膚中浸潤(rùn)的白細(xì)胞，并使表皮結(jié)構(gòu)正?；?。NVP-BAW2881 在急性炎癥模型中也表現(xiàn)出很強(qiáng)的抗炎作用；用局部 NVP-BAW2881 預(yù)處理可顯著抑制 VEGF-A 誘導(dǎo)的豬和小鼠皮膚血管通透性[2]。

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

424.38

Formula

C22H15F3N4O2
CAS 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 33 mg/mL (77.76 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.3564 mL 11.7819 mL 23.5638 mL
5 mM 0.4713 mL 2.3564 mL 4.7128 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(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(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.89 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.89 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料
參考文獻(xiàn)
Cell Assay
[2]

HUVECs or LECs (1200) are seeded into fibronectin-coated 96-well plates. After 24 hours, the cells are transferred into LEC medium containing 2% fetal bovine serum and incubated for an additional 24 hours. Cells (eight wells/condition) are incubated with medium alone (control), 20 ng/mL VEGF-A, or a combination of 20 ng/mL VEGF-A and 1 nM to 1 μM NVP-BAW2881. Proliferation is also assayed in LECs incubated with 500 ng/mL VEGF-C. The DMSO is adjusted to 0.1% in all wells. After 72 hours, cells are incubated with 5-methylumbelliferylheptanoate for subsequent fluorescent quantification of viable cells, using a electron microscope[2].

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

Mice: A contact hypersensitivity response is induced in the ear skin of 8-week-old female K14/VEGF-A TG mice. Five days after sensitization (day 0), the right ear is challenged by topical application of 10 μL oxazolone (1%) on each side. Starting on day 7, once-daily oral doses of 25 mg/kg NVP-BAW2881 or twice-daily topical doses of 0.5% NVP-BAW2881 are administered for 14 days. Control groups are given vehicles alone. The ear thickness is measured every other day using calipers. On day 21, mice are sacrificed and the weight of each ear and of its draining retro-auricular lymph node (LN) is determined[2].

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

完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(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 2.3564 mL 11.7819 mL 23.5638 mL 58.9095 mL
5 mM 0.4713 mL 2.3564 mL 4.7128 mL 11.7819 mL
10 mM 0.2356 mL 1.1782 mL 2.3564 mL 5.8909 mL
15 mM 0.1571 mL 0.7855 mL 1.5709 mL 3.9273 mL
20 mM 0.1178 mL 0.5891 mL 1.1782 mL 2.9455 mL
25 mM 0.0943 mL 0.4713 mL 0.9426 mL 2.3564 mL
30 mM 0.0785 mL 0.3927 mL 0.7855 mL 1.9636 mL
40 mM 0.0589 mL 0.2945 mL 0.5891 mL 1.4727 mL
50 mM 0.0471 mL 0.2356 mL 0.4713 mL 1.1782 mL
60 mM 0.0393 mL 0.1964 mL 0.3927 mL 0.9818 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.

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產(chǎn)品名稱：
NVP-BAW2881
目錄號(hào)：
HY-100394
需求量：