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AZD7507 Sale

目录号 : GC19404

AZD7507 是一种有效且具有口服活性的 CSF-1R 抑制剂,具有抗肿瘤活性。

AZD7507 Chemical Structure

Cas No.:1041852-85-0

规格 价格 库存 购买数量
5mg
¥1,710.00
现货
25mg
¥3,420.00
现货

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Animal experiment:

Mice[2]Male CD1 nude mice are injected subcutaneously with 5 × 105 human ICC cells from human cell line WITT-1, CC-LP-1, or SNU-1079 (n = 24 in all cases) suspended in culture media/RGF Matrigel (Gibco) mix (1:1). Cells are engrafted bilaterally in the flank and allowed to form tumors over 3 weeks. Once palpable tumors have formed, mice are randomized into 3 groups using GraphPad online software. Xenografted mice are injected with liposomal clodronate at 4 μL/g intravenously. The control for this treatment is saline alone or liposomes not containing clodronate (both given at 4 μL/g intravenously). All of these treatments are given every 48 hours for 3 weeks. CSFR1 inhibitors AZD7507 and GW2580 are made up in sterile water containing 0.5% methylcellulose and 0.1% Tween-80. AZD7507 is given twice daily at 100 mg/kg, whereas GW2580 is given daily at 160 mg/kg. Control animals are given water containing 0.5% methylcellulose and 0.1% Tween-80. ICG-001 (5 mg/kg) or C-59 (20 mg/kg) is given by intraperitoneal injection. The vehicle for this is physiological saline. Control animals are given vehicle alone. In all cases inhibitors and vehicle are given 3 times per week[2].

References:

[1]. Scott DA, et al. Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4591-6.
[2]. Boulter L, et al. WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited. Send to J Clin Invest. 2015 Mar 2;125(3):1269-85.

产品描述

AZD7507 is a potent and selective CSF-1R inhibitor (32 nM cell activity), AZD7507 is considered a promising compound as it retained the desired potency and oral pharmacokinetic properties of AZ683. Moreover, in a telemetry study in dogs given a single oral dose, there was no cardiovascular toxicity, no elevation of troponin related to the treatment, and no alteration in the ECG.

Reference

1: Boulter L, Guest RV, Kendall TJ, Wilson DH, Wojtacha D, Robson AJ, Ridgway RA, Samuel K, Van Rooijen N, Barry ST, Wigmore SJ, Sansom OJ, Forbes SJ. WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited. J Clin Invest. 2015 Mar 2;125(3):1269-85. doi: 10.1172/JCI76452. Epub 2015 Feb 17. PubMed PMID: 25689248; PubMed Central PMCID: PMC4362247.

2: Scott DA, Dakin LA, Daly K, Del Valle DJ, Diebold RB, Drew L, Ezhuthachan J, Gero TW, Ogoe CA, Omer CA, Redmond SP, Repik G, Thakur K, Ye Q, Zheng X. Mitigation of cardiovascular toxicity in a series of CSF-1R inhibitors, and the identification of AZD7507. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4591-6. doi: 10.1016/j.bmcl.2013.06.031. Epub 2013 Jun 20. PubMed PMID: 23842474.

Chemical Properties

Cas No. 1041852-85-0 SDF
化学名 4-(2-fluoro-4-methylanilino)-6-[4-(2-hydroxyethyl)piperazin-1-yl]-7-methoxycinnoline-3-carboxamide
Canonical SMILES O=C(C1=NN=C2C=C(OC)C(N3CCN(CCO)CC3)=CC2=C1NC4=CC=C(C)C=C4F)N
分子式 C23H27FN6O3 分子量 454.51
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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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 2.2002 mL 11.0009 mL 22.0017 mL
5 mM 0.44 mL 2.2002 mL 4.4003 mL
10 mM 0.22 mL 1.1001 mL 2.2002 mL
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