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AZD-3463 Sale

(Synonyms: ALK/IGF1R inhibitor) 目录号 : GC14189

An ALK and IGF-1R inhibitor

AZD-3463 Chemical Structure

Cas No.:1356962-20-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥553.00
现货
5mg
¥495.00
现货
10mg
¥765.00
现货
50mg
¥1,785.00
现货
100mg
¥2,671.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

ALK wild type cell lines (SK-N-AS, IMR-32, NGP, NB-19) and ALK mutant cell lines (LA-N-6 (D1091N) and SH-SY5Y (WT/F1174L))

Preparation method

The solubility of this compound in DMSO is >11.2mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0~50 μM, 72h

Applications

AZD-3463 effectively suppressed the proliferation of neuroblastoma cell lines with wild type ALK as well as ALK activating mutations by blocking the ALK-mediated PI3K/AKT/mTOR pathway and ultimately induced apoptosis and autophagy.

Animal experiment [1]:

Animal models

Orthotopic Neuroblastoma Mouse Model

Dosage form

15 mg/kg intraperitoneal injection once daily for 2 days.

Application

AZD-3463 exhibited significant therapeutic efficacy on the growth of the neuroblastoma tumors with WT and F1174L activating mutation ALK in orthotopic xenograft mouse models.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Wang Y, Wang L, Guan S, Cao W, Wang H, Chen Z, et al. Novel ALK inhibitor AZD3463 inhibits neuroblastoma growth by overcoming crizotinib resistance and inducing apoptosis. Sci Rep. 2016;6:19423.

产品描述

Target: ALK, IGF1R

IC50: 0.75 nM(Ki)

AZD3463 is a novel orally bioavailable ALK/IGF1R inhibitor with Ki value of 0.75 nM. ALK expression is largely restricted to neurons and upregulated in neuroblastoma. Activated ALK has been shown to promote cell survival and growth. High ALK expression or mutations in the ALK gene correlates with adverse outcomes in neuroblastoma. Therefore, ALK receptor tyrosine kinase is an important therapeutic target for drug development against neuroblastoma [1].

In vitro: AZD3463 (5, 10, 20, and 50 μM) effectively inhibited the proliferation of neuroblastoma cell lines with wild type ALK (WT) and ALK activating mutations (F1174L and D1091N) via targeting the ALK-mediated PI3K/AKT/mTOR pathway and ultimately induced apoptosis and autophagy in vitro. Moreover, AZD3463 (1 μM) significantly enhanced the cytotoxic effects of doxorubicin (1 μM) on neuroblastoma cells [1]. AZD3463 simultaneously inhibited STAT3 and AKT to augment the cytotoxic effects of temozolomide and further reduce cell growth [2].

In vivo: AZD3463 (15 mg/kg, i.p. injection) showed significant therapeutic efficacy on the growth of the neuroblastoma tumors with WT and F1174L oncogenic mutant ALK in orthotopic xenograft mouse models [1].

References:
1.  Wang Y, Wang L, Guan S, Cao W, Wang H, Chen Z, et al. Novel ALK inhibitor AZD3463 inhibits neuroblastoma growth by overcoming crizotinib resistance and inducing apoptosis. Sci Rep. 2016;6:19423.
2.  Sampson VB, Vetter NS, Kamara DF, Collier AB, Gresh RC, Kolb EA. Vorinostat Enhances Cytotoxicity of SN-38 and Temozolomide in Ewing Sarcoma Cells and Activates STAT3/AKT/MAPK Pathways. PLoS One. 2015;10(11):e0142704.

Chemical Properties

Cas No. 1356962-20-3 SDF
别名 ALK/IGF1R inhibitor
化学名 N-[4-(4-aminopiperidin-1-yl)-2-methoxyphenyl]-5-chloro-4-(1H-indol-3-yl)pyrimidin-2-amine
Canonical SMILES COC1=C(C=CC(=C1)N2CCC(CC2)N)NC3=NC=C(C(=N3)C4=CNC5=CC=CC=C54)Cl
分子式 C24H25ClN6O 分子量 448.95
溶解度 ≥ 11.22mg/mL in DMSO 储存条件 Store at -20°C
General tips 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.2274 mL 11.1371 mL 22.2742 mL
5 mM 0.4455 mL 2.2274 mL 4.4548 mL
10 mM 0.2227 mL 1.1137 mL 2.2274 mL
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