1. Apoptosis
  2. Apoptosis
  3. Evofosfamide

Evofosfamide  (Synonyms: TH-302)

目录号: HY-10535 纯度: ≥98.0%
COA 产品使用指南

Evofosfamide (TH-302) 是一种缺氧 (hypoxia) 激活前体,缺氧 (N2) 和常氧 (21% O2) 环境下,IC50 分别为 10 μM 和 1000 μM。

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Evofosfamide Chemical Structure

Evofosfamide Chemical Structure

CAS No. : 918633-87-1

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10 mM * 1 mL in DMSO ¥1383
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1 mg ¥636
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5 mg ¥1400
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10 mg ¥1850
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50 mg ¥5600
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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Evofosfamide (TH-302) is a hypoxia-activated proagent with IC50 of 10 μM and 1000 μM in hypoxia (N2) and normoxia (21% O2), respectively.

IC50 & Target

Hypoxia-activated prodrug[1]

体外研究
(In Vitro)

Evofosfamide (TH-302) induces γH2AX and apoptosis. Evofosfamide displays hypoxia-selective and concentration-dependent cytotoxic activity that is comparable in both p53-proficient and -deficient cells. Treatment with Evofosfamide (TH-302) alone causes an accumulation of G2/M cells. Inhibition of Chk1 by PF47736 in cells treated with Evofosfamide reduces Evofosfamide (TH-302)-mediated G2/M arrest under both normoxia and hypoxia[1].

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

体内研究
(In Vivo)

Evofosfamide (TH-302) is a hypoxia-activated prodrug known to activate selectively under the hypoxic conditions commonly found in solid tumors. The mean values of normalized Ktrans decrease 69.2% for Evofosfamide (TH-302)-treated mice in Hs766t tumors, decrease 46.1% for Mia PaCa-2 tumors and increase 4.9% in SU.86.86 tumors. Both changes for Hs766t and Mia PaCa-2 treatment groups are statistically significant (P<0.01) when compare to their own control group[2]. A significant reduction in the hypoxic fraction (HF) to 2.1%±4.7% is seen after 95% oxygen breathing (P<0.001), whereas 7% oxygen breathing significantly increase the HF to 29.5%±14.7% (P=0.029). Exposing rhabdomyosarcoma-bearing rats to increasing oxygen conditions abolish the effect of TH-302 and reduce the T4×SV from 20.4±3.5 to 15.3±2.5 days (P=0.007), whereas control animals have an increased T4×SV. Upon combination with radiotherapy, the T4×SV of TH-302-treated tumors decrease from 30.8±5.9 (Evofosfamide (TH-302)+radiotherapy) to 25.7±2.9 days (Evofosfamide (TH-302)+radiotherapy+95% O2)[3].

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

Clinical Trial
分子量

449.04

Formula

C9H16Br2N5O4P

CAS 号
性状

固体

颜色

White to yellow

中文名称

艾伏磷酰胺

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
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 94 mg/mL (209.34 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 4.35 mg/mL (9.69 mM; 超声助溶 (<60°C))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2270 mL 11.1349 mL 22.2697 mL
5 mM 0.4454 mL 2.2270 mL 4.4539 mL
查看完整储备液配制表

* 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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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

  • 方案 一

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

    Solubility: ≥ 2.5 mg/mL (5.57 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

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

    Solubility: ≥ 2.5 mg/mL (5.57 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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。

    20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: 50% PEG300    50% Saline

    Solubility: 10 mg/mL (22.27 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: ≥98.0%

参考文献
Cell Assay
[1]

Cells are treated with 0.1 μM of either PF477736 or AZD7762 and Evofosfamide (TH-302) for 2 h under either normoxia (21% O2) or hypoxia (N2). Following wash, cells are cultured for additional 22 h in the presence of Chk1 inhibitor under normoxia. Cells are fixed in 75% ethanol and cell cycle distribution is determined using cell cycle reagent and Guava flow cytometry. HT-29 cells are exposed to Evofosfamide (TH-302)e (8 nM, 40 nM, 200 nM, 1 μM, and 5 μM) and 0.1 μM of AZD7762 for 2 h under either normoxia (21% O2) or hypoxia (N2). After wash, cells are continuously cultured for additional 46 h in the presence of 0.1 μM of AZD7762. Luminescence-based caspase activity assay is performed[1].

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

Animal Administration
[2][3]

Mice[2]
Female SCID mice of age 5-6 weeks are inoculated with SU.86.86, Hs766t or Mia-PaCa2 cells (5×106) subcutaneously on the left hind leg. Tumors are allowed to grow for an average of three weeks to an average size of ~150 mm3. Mice are then randomized and placed into cohorts and treated with saline (control) or Evofosfamide (TH-302) (50 mg/kg) injected intraperitoneally. A total of 34 mice underwent MR imaging studies. The SU.86.86 group consist of 5 TH-302 treated and 5 control animals; Mia-PaCa2 consist of 6 Evofosfamide treated and 5 control animals; Hs766t consist of 7 Evofosfamide treated and 6 control animals. Animals are sacrificed when tumors reach 2000 mm3.
Rats[2]
Syngeneic rhabdomyosarcoma R1 tumors (1 mm3) are implanted subcutaneously in the lateral flank of adult WAG/Rij rats. Experiments are started upon a mean tumor volume of 4.2 cm3(range, 2.0-8.1) to ensure a stable HF. Treatment is administered on 4 consecutive days and consist of an intraperitoneal injection (i.p.; QD×4) with either NaCl or Evofosfamide (TH-302) (25, 50, or 75 mg/kg). Before the start of treatment, a PET scan is made using [18F]HX4. Radiotherapy is applied in a single dose of 0, 4, 8, or 12 Gy on day 3 of the treatment, 3 hours after NaCl or Evofosfamide (TH-302) injection, 1 hour after oxygen modification. During both PET imaging and radiotherapy, rats are anesthetized using a mixture of ketamine/xylazine (i.p; 66.7 and 6.7 mg/kg, respectively). During the 5 days of treatment (1 day PET imaging, 4 days of injections with Evofosfamide or vehicle), animals are exposed to modified oxygen concentrations for 4 hours per day in order to alter the HF of the tumor. The combination oxygen modification of nicotinamide (i.p. 500 mg/kg) and carbogen (95% oxygen, 5% CO2; 5 L/minute) consist of a nicotinamide injection and 30 minutes later the exposure to carbogen breathing for 3.5 hours. In the middle of the nicotinamide/carbogen treatment, NaCl/Evofosfamide is administered. Reduced oxygen breathing (7%, residual N2; 2.5 L/minute) is given for 4 hours with the NaCl/Evofosfamide injection after the first 2 hours. The injection of the [18F]HX4 PET tracer [mean 18.8 MBq, range 7.1-25.1 MBq; lateral tail vein using an intravenous line (Venoflux 0.4 mm G27) flushed with 10% heparine)] is given 2 hours before the end of the oxygen modification. PET imaging is performed 3 hours after tracer injection.

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

参考文献

Evofosfamide 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.2270 mL 11.1349 mL 22.2697 mL 55.6743 mL
5 mM 0.4454 mL 2.2270 mL 4.4539 mL 11.1349 mL
DMSO 10 mM 0.2227 mL 1.1135 mL 2.2270 mL 5.5674 mL
15 mM 0.1485 mL 0.7423 mL 1.4846 mL 3.7116 mL
20 mM 0.1113 mL 0.5567 mL 1.1135 mL 2.7837 mL
25 mM 0.0891 mL 0.4454 mL 0.8908 mL 2.2270 mL
30 mM 0.0742 mL 0.3712 mL 0.7423 mL 1.8558 mL
40 mM 0.0557 mL 0.2784 mL 0.5567 mL 1.3919 mL
50 mM 0.0445 mL 0.2227 mL 0.4454 mL 1.1135 mL
60 mM 0.0371 mL 0.1856 mL 0.3712 mL 0.9279 mL
80 mM 0.0278 mL 0.1392 mL 0.2784 mL 0.6959 mL
100 mM 0.0223 mL 0.1113 mL 0.2227 mL 0.5567 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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