Anlotinib (AL3818) dihydrochloride

For research use only. Not for use in humans.

目录号:S8726

Anlotinib (AL3818) dihydrochloride Chemical Structure

CAS No. 1360460-82-7

Anlotinib (AL3818) 是一种高度有效的VEGFR2选择性抑制剂,IC50小于1 nM。它在临床试验中具有广谱性抗肿瘤潜力。稀释请用生理盐水,请勿用PBS稀释,可能产生沉淀。

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RMB 3850.17 现货
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客户使用Selleck生产的Anlotinib (AL3818) dihydrochloride发表文献14篇:

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

产品描述 Anlotinib (AL3818) 是一种高度有效的VEGFR2选择性抑制剂,IC50小于1 nM。它在临床试验中具有广谱性抗肿瘤潜力。稀释请用生理盐水,请勿用PBS稀释,可能产生沉淀。
靶点
VEGFR2 [1]
(Cell-free assay)
VEGFR3 [1]
(Cell-free assay)
c-Kit [1]
(Cell-free assay)
c-Kit [1]
(Cell-free assay)
c-Kit [1]
(Cell-free assay)
0.2 nM 0.7 nM 14.8 nM 14.8 nM 14.8 nM
体外研究

Anlotinib可占据VEGFR酪氨酸激酶的ATP结合区域,相对于其他酪氨酸激酶,对VEGFR2的选择性和抑制活性较高(IC50<1 nM)。Anlotinib可抑制VEGFR2和VEGFR3,IC50分别为0.2 nM和0.7 nM。Anlotinib对VEGFR1的抑制活性较低,IC50为26.9 nM。anlotinib抑制PDGFR相关激酶c-Kit和PDGFRβ的IC50分别为14.8和115 nM。它对其他激酶,如c-Met, c-Src, EGFR和HER2具有较小的活性。Anlotinib以皮摩尔级别的浓度在HUVEC细胞中抑制VEGF诱导的信号通路和细胞增殖。然而,在体外肿瘤细胞中则需要微摩尔级别浓度的anlotinib来直接抑制其增殖。Anlotinib可显著地抑制HUVEC的迁移和小管生成,在体外还能抑制大鼠主动脉移植体的血管生长[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U-87MG MYnGeY5kfGmxbjDhd5NigQ>? NYnmWplKOC5yMTygNE4yNCBzLDCxNEBidmRiMUCwJO69VQ>? MV2xMlUhcA>? M2LBeYlvcGmkaYTl[EBRTEeILVLCMZN1cW23bHH0[YQheGixc4Doc5J6dGG2aX;uJI9nKFCGR1\S{tItKEGNVDDhcoQhTVKNIHnuJHUuQDePRzDj[Yxtew>? NEi3[XY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS0Olg2Oyd-Mkm0OFY5PTN:L3G+
Mo7e NVTpN|l4TnWwY4Tpc44h[XO|YYm= MmfNNE4xOSxiMD6xMEAyNCBzMDDhcoQhOTByIN88US=> NXHpPW0yOS53IHi= NV;nNFBiSW6ub4TpcoljKGmwaHnibZRm\CCVQ1dihLAy6oDSc4TpcZVt[XSnZDDwbI9{eGixconsZZRqd25ib3[gZ-KBmEurdDygRWtVKGGwZDDFVmshcW5iTX:3[UBk\Wyucx?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR2Nki1N{c,Ojl2NE[4OVM9N2F-
HUVEC M{LuSmZ2dmO2aX;uJIF{e2G7 MVmwMlAyNCByLkGsJFEtKDFyIHHu[EAyODBizszN MkXUNU42KGh? MkXNZY5td3SrbnniJIlvcGmkaYTl[EBXTUeI4pEQd5RqdXWuYYTl[EBqdnS{YXPlcIx2dGG{IIDoc5NxcG:{eXzheIlwdiCxZjDWSWdHWjJiaX6gZUBkd26lZX70doF1cW:w4pEQ[IVx\W6mZX70JJdigSCrbjDIWXZGSyC5aYToJIEhe3WkbnHuc41wdGG{IFnDOVAhfmGudXW= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR2Nki1N{c,Ojl2NE[4OVM9N2F-
A549 Mmf6R4VtdCC4aXHibYxqfHliYYPzZZk> MUCyOEwhPDhiYX7kJFcz6oDLaB?= MXLJR|UxRTZ2LkiyJO69Ve,:iIS9NlQhcO,:iUugTWM2OD1|MD6zOEDPxE4xvJj0QVQ5KGkxvJm7JGlEPTB;MUeuNlkh|ryP78{IeF04OiCq78{J MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODd3NUK0Nkc,OzB5NUWyOFI9N2F-
NCI-H1975 MUPD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NYDoW3BxQOLCid88[{9udA>? NXnwR|B{OjUkgJno MlXzR4VtdCC4aXHibYxqfHlid3HzJIRm[3KnYYPl[EBz\W2jcnvhZox6 NXXLZnVrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C4O|E2OjZpPkOwPFcyPTJ4PD;hQi=>
Calu-1 M3Hjd2NmdGxidnnhZoltcXS7IHHzd4F6 MkHzNlQtKDR6IHHu[EA4OuLCiXi= M1HPdGlEPTB;NkGuNlMh|ryP78{IeF0zPCCq78{JP{BKSzVyPUO2Mlgh|ryP78{IeF01QCCq78{JP{BKSzVyPUK4MlY1KM7:Tf-8jJQ:PzJiaP-8jS=> M1vaVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyN{W1NlQzLz5|MEe1OVI1OjxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
TP53 / Cleaved-caspase 3 / Cleaved PARP ; 

PubMed: 30139768     


BCPAP (C) and 8505C (F) cells were treated with anlotinib (0, 1, 5, 10 and 15 µM) for 36 h. Cell lysates were prepared and subjected to Western blot to detect the expression of TP53, cleaved caspase 3 (CL-caspase 3) and cleaved PARP (CL-PARP).

Beclin-1 / LC3-I / LC3-II ; 

PubMed: 30755242     


Calu-1 and A549 cells were treated with anlotinib 0–20 μM for 24 h or anlotinib 20 μM for 0–24 h, and the expression levels of beclin-1 and LC3-I/II were detected by western blotting.

Akt / p-Akt / mTOR / p-mTOR ; 

PubMed: 30755242     


Expression of Akt, pAkt, mTOR, p-mTOR, and beclin-1 in lung cancer cells after treatment with concentration gradient anlotinib for 24 h was detected by immunoblotting. 

30139768 30755242
Immunofluorescence
LC3-II ; 

PubMed: 30755242     


Calu-1 and A549 cells on the coverslips were treated with anlotinib or RAPA for 48 h. The punctate patterns of LC3-II were observed by confocal microscopy. 

30755242
Growth inhibition assay
Cell viability; 

PubMed: 30755242     


a, Dose-response curves of Calu-1 and A549 cells to anlotinib treatment. Cells were cultured by anlotinib at various concentrations for 24, 48 and 72 h and cell viability was detected by CCK-8 assay. b, Representative images of clone formation assay.

30755242
体内研究 在体内肿瘤组织中,Anlotinib可降低血管密度。在某些动物模型中,与sunitinib相比,每天口服一定剂量anlotinib具有更广泛和有效的抗肿瘤活性,在裸鼠中能引起肿瘤消退。在小鼠中,Anlotinib耐受良好,显著抑制其肿瘤生长的有效剂量(1.5-6 mg/kg)比其他TKI低[1]。在体内,anlotinib对多种人源异种移植瘤如SW-620、SK-OV-3、SMMC-7721、Caki-1、U87MG、Calu-3等具有广泛的活性。在Sprague-Dawley大鼠和beagle dogs体内,口服anlotinib能快速地从胃肠道吸收。在大鼠中,其口服生物利用度约为23-45%,而在犬类中为47%-74%。Anlotinib在犬类和大鼠中,分布体积大。在大鼠中,在一些主要的组织器官如肺、肾、肝和心脏中具有较血浆中更高的暴露量,而在大脑中的暴露量与血浆中水平相当。在携瘤小鼠中,肿瘤组织中的anlotinib的浓度比血浆中的高2.4-2.6倍。在人类,anlotinib具有较长的半衰期(t1/2=96 ± 17 h),并呈浓度依赖性关系[2]。在狗中,终末半衰期为22.8±11.0 h,比在大鼠中(5.1±1.6 h)长。这一差异可能与物种间总的血浆清除率差异相关。在人类血浆中,anlotinib主要与白蛋白、脂蛋白相结合[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

- 合并

Enzyme-linked immunosorbent assay:

Inhibitory activity of anlotinib against tyrosine kinases was determined using ELISA. Reaction of ATP with tyrosine kinase was initiated in reaction buffer (50 mmol/L HEPES pH 7.4, 50 mmol/L MgCl2, 0.5 mmol/L MnCl2, 0.2 mmol/L Na3VO4, 1 mmol/L DTT) and incubated for 1 hour at 37°C in 96-well plates precoated with 20 μg/mL Poly(Glu,Tyr)4:1. The plate was incubated with PY99 antibody and then with HRP-conjugated anti-mouse IgG. After reaction with o-phenylenediamine solution and then termination with the addition of 2N H2SO4, absorbance was measured at 490 nm using a Synergy H4 Hybrid reader.
细胞实验:

[1]

- 合并
  • Cell lines: HUVEC, Mo7e, U-87MG and A431 cells
  • Concentrations: 0-10 μM
  • Incubation Time: 1.5 h
  • Method:

    Serum-starved HUVEC, Mo7e, U-87MG and A431 cells are treated with different concentrations of test agents for 1.5 h and then stimulated with vascular endothelial growth factor (VEGF; 20 ng/mL), stem cell factor-1 (SCF-1; 2.5 ng/mL), platelet-derived growth factor-BB (PDGF-BB; 10 ng/mL), or epidermal growth factor (EGF; 10 ng/mL) for 10 min, respectively. Cell lysates are probed with the indicated antibodies.


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: human colon cancer SW620 xenograft model(Balb/cA-nude mice, 5-6 weeks old)
  • Dosages: 0.75, 1.5, 3 and 6 mg/kg
  • Administration: oral
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 96 mg/mL (199.85 mM)
Water 96 mg/mL (199.85 mM)
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 480.36
化学式

C23H22FN3O3.2HCl

CAS号 1360460-82-7
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04803851 Not yet recruiting Drug: Anlotinib plus AK105 Anlotinib|Anti-PD-1 Antibody|Advanced Pancreatic Cancer Peking Union Medical College Hospital March 2021 Phase 1|Phase 2
NCT02825563 Completed Drug: Anlotinib Advanced Cancer Chia Tai Tianqing Pharmaceutical Group Co. Ltd. June 2016 Phase 1
NCT02752516 Unknown status Drug: Anlotinib Cancer Chia Tai Tianqing Pharmaceutical Group Co. Ltd. April 27 2016 Phase 1
NCT02622932 Completed Drug: Anlotinib and 14C-labeled Anlotinib Advanced Solid Tumors Chia Tai Tianqing Pharmaceutical Group Co. Ltd. December 2 2015 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID