NAZ2329,99.57%

产品编号:Bellancom-103693| 分子式:C21H18F3NO4S3| 分子量:501.56

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-103693
4000.00 杭州 北京(现货)
Bellancom-103693
6800.00 杭州 北京(现货)
Bellancom-103693
13500.00 杭州 北京(现货)

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NAZ2329

产品介绍 NAZ2329 是受体型蛋白质酪氨酸磷酸酶 (RPTPs) R5 亚家族的第一个细胞可渗透抑制剂,相对于其他 PTPs,它变构且优先抑制PTPRZ (hPTPRZ1 的IC50 = 7.5 µM) 和 PTPRG (hPTPRG IC50 = 4.8 µM)。NAZ2329 与 PTPRZ 的 D1结构域结合,相对于 PTPRZ 整个 (D1 + D2) 片段,其更有效地抑制 PTPRZ1-D1片段,其 IC50 为1.1 µM。NAZ2329 可有效抑制胶质母细胞瘤细胞的肿瘤生长并抑制干细胞样特性。
生物活性

NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties.

体外研究

NAZ2329 (0-25 µM; 48 hours) dose-dependently inhibits cell proliferation and migration in all cell lines (rat glioblastoma cells bearing C6 clone and human U251 glioblastoma cells) .
NAZ2329 (25 µM; 0-90 min) obviously promotes the phosphorylation level of paxillin at Tyr-118 site, leading to inhibition for PTPR substrate.

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

Cell Proliferation Assay

Cell Line: Rat glioblastoma cells bearing C6 clone, human U251 glioblastoma cells
Concentration: 0 µM, 6.3 µM, 12.5 µM, 25 µM
Incubation Time: 48 hours
Result: Exerted inhibition in cell proliferation and migration in a dose-dependent manner.

Western Blot Analysis

Cell Line: Rat glioblastoma cells bearing C6 clone
Concentration: 25 µM
Incubation Time: 0 min, 15 min, 30 min, 60 min, 90min
Result: Promoted the phosphorylation level of paxillin at Tyr-118 site.
体内研究
(In Vivo)

NAZ2329 (22.5 mg/kg; intraperitoneal injection; twice per week; 40 days) alone has a moderate inhibitory effect. However, the combination of Temozolomide and NAZ2329 exerts a significantly increased inhibition of tumor growth compared with the control group, the NAZ2329 monotherapy group and the Temozolomide monotherapy group.

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

Animal Model: Female BALB/c- nu/nu mice aged 4 week-old bearing parental or Ptprz-knockdown C6 cells
Dosage: 22.5 mg/kg; Temozolomide (TMZ, 50 mg/kg)
Administration: Intraperitoneal injection; twice per week; 40 days
Result: The combination of NAZ2329 and TMZ significantly delayed tumor growth compared to NAZ2329 or TMZ alone.
体内研究

NAZ2329 (22.5 mg/kg; intraperitoneal injection; twice per week; 40 days) alone has a moderate inhibitory effect. However, the combination of Temozolomide and NAZ2329 exerts a significantly increased inhibition of tumor growth compared with the control group, the NAZ2329 monotherapy group and the Temozolomide monotherapy group.

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

Animal Model: Female BALB/c- nu/nu mice aged 4 week-old bearing parental or Ptprz-knockdown C6 cells
Dosage: 22.5 mg/kg; Temozolomide (TMZ, 50 mg/kg)
Administration: Intraperitoneal injection; twice per week; 40 days
Result: The combination of NAZ2329 and TMZ significantly delayed tumor growth compared to NAZ2329 or TMZ alone.
体内研究

NAZ2329 (22.5 mg/kg; intraperitoneal injection; twice per week; 40 days) alone has a moderate inhibitory effect. However, the combination of Temozolomide and NAZ2329 exerts a significantly increased inhibition of tumor growth compared with the control group, the NAZ2329 monotherapy group and the Temozolomide monotherapy group.

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

Animal Model: Female BALB/c- nu/nu mice aged 4 week-old bearing parental or Ptprz-knockdown C6 cells
Dosage: 22.5 mg/kg; Temozolomide (TMZ, 50 mg/kg)
Administration: Intraperitoneal injection; twice per week; 40 days
Result: The combination of NAZ2329 and TMZ significantly delayed tumor growth compared to NAZ2329 or TMZ alone.
性状Solid
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (199.38 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9938 mL 9.9689 mL 19.9378 mL
5 mM 0.3988 mL 1.9938 mL 3.9876 mL
10 mM 0.1994 mL 0.9969 mL 1.9938 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: ≥ 2.5 mg/mL (4.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.98 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.98 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.98 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

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

    Solubility: ≥ 2.5 mg/mL (4.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.98 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 25.0 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 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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