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  3. AZD7507

AZD7507 

目录号: HY-117244 纯度: 99.45%
产品使用指南

AZD7507 为一种有效的、可口服的 CSF-1R 抑制剂,具有抗肿瘤活性。

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AZD7507 Chemical Structure

AZD7507 Chemical Structure

CAS No. : 1041852-85-0

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥3850 In-stock
5 mg ¥3500 In-stock
10 mg ¥5500 In-stock
25 mg ¥11000 In-stock
50 mg ¥17500 In-stock
100 mg ¥27500 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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Description

AZD7507 is a potent and orally active CSF-1R inhibitor, with antitumor activity.

IC50 & Target

CSF-1R[1]

In Vitro

AZD7507 (Compound 31) inhibits the proliferation of 3T3 cells engineered to express CSF-1R and stimulated with CSF-1 (IC50, 32 nM), shows inhibitory activity against hERG and NaV1.5, with IC50s of >30 and 26 μM[1].

In Vivo

AZD7507 has good rat oral PK, with in vivo clearance of 7 mL/min/kg and 42% bioavailability. In the canine L-type Ca channel assay, the IC50 is >20 μM[1]. AZD7507 significantly decreases the number of CD68+ macrophages in mice, and also reduces the volume and mass in mice bearing CC-LP-1 and SNU-1079 cells, but not WITT-1 cells[2].

Molecular Weight

454.50

Formula

C₂₃H₂₇FN₆O₃

CAS No.

1041852-85-0

SMILES

O=C(N)C1=NN=C2C=C(C(N3CCN(CC3)CCO)=CC2=C1NC4=CC=C(C=C4F)C)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 130 mg/mL (286.03 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2002 mL 11.0011 mL 22.0022 mL
5 mM 0.4400 mL 2.2002 mL 4.4004 mL
10 mM 0.2200 mL 1.1001 mL 2.2002 mL
*

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。 -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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (4.77 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (4.77 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (4.77 mM); Clear solution

    此方案可获得 ≥ 2.17 mg/mL (4.77 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
References
Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.45%

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

AZD7507AZD 7507AZD-7507c-FmsCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RInhibitorinhibitorinhibit

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产品名称:
AZD7507
目录号:
HY-117244
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