AAL993

目录号: HY-19986 纯度: 99.50%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

AAL993 是一种有效的、选择性的、具有口服活性的 VEGFR 抑制剂，对 VEGFR1、VEGFR2 和 VEGFR3 的 IC₅₀ 分别为 130 nM、23 nM 和 18 nM。AAL993 对其他酪氨酸激酶的抑制作用较弱。AAL993 具有有效的抗血管生成和抗肿瘤特性。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

AAL993 Chemical Structure

CAS No. : 269390-77-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1210	In-stock
1 mg	￥440	In-stock
5 mg	￥1100	In-stock
10 mg	￥1850	In-stock
25 mg	￥3500	In-stock
50 mg	￥5500	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

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查看所有亚型

VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

生物活性
纯度 & 产品资料
参考文献

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)

细胞效力
(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]

体外研究
(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.

体内研究
(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 号

269390-77-4

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 125 mg/mL (336.60 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	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
10 mM	0.2693 mL	1.3464 mL	2.6928 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.60 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.60 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

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

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.50%

选择批次：

Data Sheet (625 KB) SDS (251 KB)

COA (266 KB) HNMR (248 KB) LCMS (258 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Paul W Manley , et al. Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. J Med Chem. 2002 Dec 19;45(26):5687-93. [Content Brief]

[2]. Hyun Seung Ban, et al. Suppression of hypoxia-induced HIF-1alpha accumulation by VEGFR inhibitors: Different profiles of AAL993 versus SU5416 and KRN633. Cancer Lett. 2010 Oct 1;296(1):17-26. [Content Brief]

AAL993 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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.

Keywords:

AAL993269390-77-4AAL 993AAL-993VEGFRVascular endothelial growth factor receptorVEGFR inhibitororally activeVEGFR1VEGFR2VEGFR3antiangiogenicantitumor propertiesInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

AAL993

Customer Review