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

MMAF  (Synonyms: Monomethylauristatin F)

目錄號(hào): HY-15579 純度: 99.92%
COA 產(chǎn)品使用指南 技術(shù)支持

MMAF (Monomethylauristatin F) 是一種有效的微管蛋白聚合 (tubulin polymerization) 抑制劑，用作抗腫瘤藥物。MMAF (Monomethylauristatin F) 廣泛用作抗體偶聯(lián)藥物 (ADCs) 的細(xì)胞毒性成分，如 Vorsetuzumab mafodotin 和 SGN-CD19A。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

MMAF Chemical Structure

MMAF Chemical Structure

CAS No. : 745017-94-1

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規(guī)格 價(jià)格 是否有貨 數(shù)量
5 mg ￥240
In-stock
10 mg ￥400
In-stock
50 mg ￥1200
In-stock
100 mg ￥1800
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

Other Forms of MMAF:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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

 

細(xì)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]
體外研究
(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.
體內(nèi)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 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

4°C, protect from light, stored under nitrogen

*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 140 mg/mL (191.27 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

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

    此方案可獲得 ≥ 3.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 35.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
  • 方案 二

    請(qǐng)依序添加每種溶劑： 10% DMSO    90% Corn Oil

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

    此方案可獲得 ≥ 3.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

    以 1 mL 工作液為例，取 100 μL 35.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.92%

參考文獻(xiàn)
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.
參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱：
MMAF
目錄號(hào)：
HY-15579
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