AZ-23 (AZ23)

目录号: GC33090纯度: >98.50%同义词: 5-氯-N-[(1S)-1-(5-氟吡啶-2-基)乙基]-N'-(5-异丙氧基-1H-吡唑-3-基)嘧啶-2,4-二胺,AZ23; AZ 23
AZ-23 (AZ23) 是一种 ATP 竞争性和口服生物可利用的 Trk 激酶 A/B/C 抑制剂,IC50 为 2 nM (TrkA)、8 nM (TrkB)、24 nM (FGFR1)、52 nM (Flt3)、55分别为 nM (Ret)、84 nM (MuSk)、99 nM (Lck)。

AZ-23 (AZ23)
Cas No.: 915720-21-7
规格价格库存数量操作
2mg¥599.00现货
1
5mg¥897.00现货
1
10mg¥1,751.00现货
1
25mg¥4,201.00现货
1
10mM (in 1mL DMSO)¥773.00现货
1

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产品描述 Description

AZ-23 is an ATP-competitive and orally bioavailable Trk kinase A/B/C inhibitor with IC50s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1), 52 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM (Lck), respectively.

AZ-23 potently and selectivity inhibits Trk phosphorylation in cells. AZ-23 potently inhibits Trk-mediated survival (EC50 of 2 nM). AZ-23 Inhibits Trk-Dependent Survival in MCF10ATrkA-δ and TF-1 Cell Lines[1].

AZ-23 shows in vivo TrkA kinase inhibition and efficacy in mice following oral administration in a TrkA-driven allograft model and significant tumor growth inhibition in a Trk-expressing xenograft model of neuroblastoma[1].

[1]. Thress K, et al. Identification and preclinical characterization of AZ-23, a novel, selective, and orally bioavailable inhibitor of the Trk kinase pathway. Mol Cancer Ther. 2009 Jul; 8(7):1818-27.

实验参考方法 Experimental Reference Method

Cell experiment:

Exponentially growing TF-1 cells are treated with various concentrations of AZ-23 and then incubated for an additional 72 h at 37°C in either growth or basal medium plus 100 ng/mL NGF. Cell proliferation is measured using MTS solution[1].

Animal experiment:

Mice[1] Tumor-bearing mice are given a single, oral dose of compound and individual mice are sacrificed at various time points postdose (2, 6, 16, or 24 hours). Tumors are excised and homogenized and the resulting tumor lysates are analyzed using an ELISA for pTrkA[1].

References:

[1]. Thress K, et al. Identification and preclinical characterization of AZ-23, a novel, selective, and orally bioavailable inhibitor of the Trk kinase pathway. Mol Cancer Ther. 2009 Jul; 8(7):1818-27.

产品文档 Product Documents

Purity:>98.50%

化学性质Chemical Properties

CAS 号
915720-21-7
同义词
5-氯-N-[(1S)-1-(5-氟吡啶-2-基)乙基]-N'-(5-异丙氧基-1H-吡唑-3-基)嘧啶-2,4-二胺,AZ23; AZ 23
SMILES
CC(OC1=CC(NC2=NC(N[C@H](C3=NC=C(F)C=C3)C)=NC=C2Cl)=NN1)C
分子式
C17H19ClFN7O
分子量
391.83 g/mol
溶解性
DMSO : 125 mg/mL (319.02 mM)
保存条件
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°C,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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

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