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  2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. AAL993

AAL993 是一種有效的、選擇性的、具有口服活性的 VEGFR 抑制劑，對(duì) VEGFR1、VEGFR2 和 VEGFR3 的 IC50 分別為 130 nM、23 nM 和 18 nM。AAL993 對(duì)其他酪氨酸激酶的抑制作用較弱。AAL993 具有有效的抗血管生成和抗腫瘤特性。

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)

AAL993 Chemical Structure

AAL993 Chemical Structure

CAS No. : 269390-77-4

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1210
In-stock
1 mg ￥440
In-stock
5 mg ￥1100
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10 mg ￥1850
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25 mg ￥3500
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50 mg ￥5500
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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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查看 VEGFR 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

IC50s of 130 nM, 23 nM, and 18 nM for VEGFR1, VEGFR2, and VEGFR3, respectively. AAL993 shows less potently inhibits other tyrosine kinases. AAL993 possesses potent antiangiogenic and antitumor properties[1].

IC50 & Target[1]

VEGFR1

130 nM (IC50)

VEGFR2

23 nM (IC50)

VEGFR3

18 nM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
BaF3 IC50
> 10 μM
Compound: AAL993
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
> 5.5 μM
Compound: AAL993
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
> 5.5 μM
Compound: AAL993
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]
BaF3 IC50
> 5.5 μM
Compound: AAL993
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
> 5.5 μM
Compound: AAL993
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
> 5.5 μM
Compound: AAL993
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
> 5.5 μM
Compound: AAL993
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
0.013 μM
Compound: AAL993
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
0.019 μM
Compound: AAL993
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
2.9 μM
Compound: AAL993
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
5.6 μM
Compound: AAL993
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
8.4 μM
Compound: AAL993
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]
CHO IC50
0.0012 μM
Compound: C
Inhibition of VEGF-induced VEGFR2 phosphorylation expressed in CHO cells in presence of 8 uM ATP by ELISA
Inhibition of VEGF-induced VEGFR2 phosphorylation expressed in CHO cells in presence of 8 uM ATP by ELISA
[PMID: 19124243]
HEK293 IC50
0.09 μM
Compound: C
Inhibition of VEGFR2 expressed in HEK293 cells assessed as inhibition of receptor phosphorylation by ELISA
Inhibition of VEGFR2 expressed in HEK293 cells assessed as inhibition of receptor phosphorylation by ELISA
[PMID: 19124243]
HEK293 IC50
0.09 μM
Compound: C
Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA
Inhibition of VEGFR2 phosphorylation in HEK293 cells by cell-based ELISA
[PMID: 16460936]
HUVEC IC50
> 3 μM
Compound: AAL993
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
1 nM
Compound: AAL993
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)

AAL993 suppresses HIF-1α expression through ERK inhibition without affecting Akt phosphorylation[2].

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

AAL993 (compound 5) potently inhibits VEGF-induced angiogenesis in an implant model, with an ED50 value of 7 mg/kg[1].
In B16 melanoma xenograft model, AAL993 (24-100 mg/kg; p.o.; daily; for 14days) inhibits both the growth of the primary tumor as well as the formation of spontaneous peripheral metastases[1].

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

371.36

Formula

C20H16F3N3O
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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 125 mg/mL (336.60 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.6928 mL 13.4640 mL 26.9281 mL
5 mM 0.5386 mL 2.6928 mL 5.3856 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, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?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(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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/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: ≥ 2.08 mg/mL (5.60 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.60 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 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 20.8 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 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
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）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的儲(chǔ)備液濃度超過該產(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)

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, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?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 2.6928 mL 13.4640 mL 26.9280 mL 67.3201 mL
5 mM 0.5386 mL 2.6928 mL 5.3856 mL 13.4640 mL
10 mM 0.2693 mL 1.3464 mL 2.6928 mL 6.7320 mL
15 mM 0.1795 mL 0.8976 mL 1.7952 mL 4.4880 mL
20 mM 0.1346 mL 0.6732 mL 1.3464 mL 3.3660 mL
25 mM 0.1077 mL 0.5386 mL 1.0771 mL 2.6928 mL
30 mM 0.0898 mL 0.4488 mL 0.8976 mL 2.2440 mL
40 mM 0.0673 mL 0.3366 mL 0.6732 mL 1.6830 mL
50 mM 0.0539 mL 0.2693 mL 0.5386 mL 1.3464 mL
60 mM 0.0449 mL 0.2244 mL 0.4488 mL 1.1220 mL
80 mM 0.0337 mL 0.1683 mL 0.3366 mL 0.8415 mL
100 mM 0.0269 mL 0.1346 mL 0.2693 mL 0.6732 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：
AAL993
目錄號(hào)：
HY-19986
需求量：