1. Cell Cycle/DNA Damage Cytoskeleton Antibody-drug Conjugate/ADC Related
  2. Microtubule/Tubulin ADC Cytotoxin
  3. MMAF

MMAF  (Synonyms: Monomethylauristatin F)

目录号: HY-15579 纯度: 99.91%
COA 产品使用指南

MMAF (Monomethylauristatin F) 是一种有效的微管蛋白聚合 (tubulin polymerization) 抑制剂,用作抗肿瘤药物。MMAF (Monomethylauristatin F) 广泛用作抗体偶联药物 (ADCs) 的细胞毒性成分,如 Vorsetuzumab mafodotin 和 SGN-CD19A。

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MMAF Chemical Structure

MMAF Chemical Structure

CAS No. : 745017-94-1

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
5 mg ¥240
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10 mg ¥400
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50 mg ¥1200
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100 mg ¥1800
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500 mg   询价  

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Customer Review

Other Forms of MMAF:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

MMAF (Monomethylauristatin F) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF (Monomethylauristatin F) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin and SGN-CD19A[1][2][3].

IC50 & Target

Auristatin

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BT-474 GI50
0.24 nM
Compound: 6-OMe, MMAF-OMe
Cytotoxicity against human BT474 cells assessed as cell viability incubated fore 4 days by MTS assay
Cytotoxicity against human BT474 cells assessed as cell viability incubated fore 4 days by MTS assay
[PMID: 25431858]
BT-474 IC50
8.8 nM
Compound: MMAF
Cytotoxicity against human BT-474 cells assessed as reduction in cell viability incubated for 96 hrs by XTT assay
Cytotoxicity against human BT-474 cells assessed as reduction in cell viability incubated for 96 hrs by XTT assay
[PMID: 34676042]
MDA-MB-361 GI50
0.21 nM
Compound: 6-OMe, MMAF-OMe
Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay
Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay
[PMID: 25431858]
NCI-N87 GI50
0.44 nM
Compound: 6-OMe, MMAF-OMe
Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay
Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay
[PMID: 25431858]
SK-BR-3 IC50
5.3 nM
Compound: MMAF
Cytotoxicity against human SKBR3 cells assessed as reduction in cell viability incubated for 96 hrs by XTT assay
Cytotoxicity against human SKBR3 cells assessed as reduction in cell viability incubated for 96 hrs by XTT assay
[PMID: 34676042]
体外研究
(In Vitro)

MMAF inhibits anaplastic large cell lymphoma Karpas 299, breast carcinoma H3396, renal cell carcinoma 786-O and Caki-1 cells with IC50s of 119, 105, 257 and 200 nM in vitro cytotoxicity assay[4].

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

体内研究
(In Vivo)

The maximum tolerated dose (MTD) in mice of MMAF (Monomethylauristatin F) (>16 mg/kg) is much higher than MMAE (Monomethylauristatin E) (1 mg/kg). cAC10-L1-MMAF4 has an MTD of 50 mg/kg in mice and 15 mg/kg in rats. The corresponding cAC10-L4-MMAF4 ADC was much less toxic, having MTDs in mice and rats of >150 mg/ kg and 90 mg/kg in rats, respectively[4].

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

分子量

731.96

Formula

C39H65N5O8

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light, stored under nitrogen

*该产品在溶液状态不稳定,建议您现用现配,即刻使用。

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 140 mg/mL (191.27 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3662 mL 6.8310 mL 13.6619 mL
5 mM 0.2732 mL 1.3662 mL 2.7324 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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

  • 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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3.5 mg/mL (4.78 mM); 澄清溶液

    此方案可获得 ≥ 3.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 35.0 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。

    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。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 3.5 mg/mL (4.78 mM); 澄清溶液

    此方案可获得 ≥ 3.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 35.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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)。

*该产品在溶液状态不稳定,建议您现用现配,即刻使用。

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: 99.91%

参考文献
Cell Assay
[1]

Cells are treated with serial dilutions of test molecules and incubated 4-6 days depending on cell line. Assessment of cellular growth and data reduction to generate IC50 values is done using Alamar Blue dye reduction assay[2].

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

Animal Administration
[1]

Mice: When subcutaneous Karpas 299 tumor size reaches 300 mm3, three animals per group receives one injection of 10 mg antibody component/kg body weight of either cAC10-L1-MMAF4 or cBR96-L1-MMAF4 intravenously. Tumors are then removed and placed in optimal cutting temperature compound, and 5 μm-thin frozen tissue sections are stained using immunohistochemistry evaluation[1].

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

参考文献

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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3662 mL 6.8310 mL 13.6619 mL 34.1549 mL
5 mM 0.2732 mL 1.3662 mL 2.7324 mL 6.8310 mL
10 mM 0.1366 mL 0.6831 mL 1.3662 mL 3.4155 mL
15 mM 0.0911 mL 0.4554 mL 0.9108 mL 2.2770 mL
20 mM 0.0683 mL 0.3415 mL 0.6831 mL 1.7077 mL
25 mM 0.0546 mL 0.2732 mL 0.5465 mL 1.3662 mL
30 mM 0.0455 mL 0.2277 mL 0.4554 mL 1.1385 mL
40 mM 0.0342 mL 0.1708 mL 0.3415 mL 0.8539 mL
50 mM 0.0273 mL 0.1366 mL 0.2732 mL 0.6831 mL
60 mM 0.0228 mL 0.1138 mL 0.2277 mL 0.5692 mL
80 mM 0.0171 mL 0.0854 mL 0.1708 mL 0.4269 mL
100 mM 0.0137 mL 0.0683 mL 0.1366 mL 0.3415 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
MMAF
目录号:
HY-15579
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