标签归档：monomethylauristatin

MMAF sodium(Synonyms: Monomethylauristatin F sodium)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MMAF sodium (Synonyms: Monomethylauristatin F sodium)

MMAF sodium (Monomethylauristatin F sodium) 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 sodium (Monomethylauristatin F sodium) 广泛用作抗体偶联药物 (ADCs) 的细胞毒性成分，如Vorsetuzumab mafodotin 和 SGN-CD19A。

MMAF sodium(Synonyms: Monomethylauristatin F sodium)

MMAF sodium Chemical Structure

CAS No. : 1799706-65-2

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥800 In-stock
10 mg ￥1200 In-stock
25 mg ￥1800 In-stock
50 mg ￥2500 In-stock
100 mg ￥3400 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MMAF sodium 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Toxins for Antibody-Drug Conjugate Research Library

生物活性

MMAF sodium (Monomethylauristatin F sodium) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF sodium (Monomethylauristatin F sodium) 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

 

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

753.94

Formula

C39H64N5NaO8
CAS 号

1799706-65-2
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
In Vitro: 

DMSO : ≥ 200 mg/mL (265.27 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3264 mL 6.6318 mL 13.2637 mL
5 mM 0.2653 mL 1.3264 mL 2.6527 mL
10 mM 0.1326 mL 0.6632 mL 1.3264 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

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: ≥ 5 mg/mL (6.63 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (6.63 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (6.63 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (6.63 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (6.63 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (6.63 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 50.0 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Lee JW, et al. EphA2 targeted chemotherapy using an antibody drug conjugate in endometrial carcinoma. Clin Cancer Res. 2010 May 1;16(9):2562-70.

    [2]. Lee JJ, et al. Enzymatic prenylation and oxime ligation for the synthesis of stable and homogeneous protein-drug conjugates for targeted therapy. Angew Chem Int Ed Engl. 2015 Oct 5;54(41):12020-4.

    [3]. Kim EG, et al. Strategies and Advancement in Antibody-Drug Conjugate Optimization for Targeted CancerTherapeutics.

    [4]. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

MMAF(Synonyms: Monomethylauristatin F)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MMAF (Synonyms: Monomethylauristatin F)

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。

MMAF(Synonyms: Monomethylauristatin F)

MMAF Chemical Structure

CAS No. : 745017-94-1

规格 价格 是否有货 数量
5 mg ￥800 In-stock
10 mg ￥1200 In-stock
25 mg ￥1800 In-stock
50 mg ￥2500 In-stock
100 mg ￥3400 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MMAF 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Toxins for Antibody-Drug Conjugate Research Library
  • Peptidomimetic Library

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

 

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

The maximum tolerated dose in mice of MMAF (Monomethylauristatin F) (>16 mg/kg) is much higher than MMAF (Monomethylauristatin F) (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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

731.96

Formula

C39H65N5O8
CAS 号

745017-94-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*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
In Vitro: 

DMSO : 140 mg/mL (191.27 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3662 mL 6.8310 mL 13.6619 mL
5 mM 0.2732 mL 1.3662 mL 2.7324 mL
10 mM 0.1366 mL 0.6831 mL 1.3662 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3.5 mg/mL (4.78 mM); Clear solution

    此方案可获得 ≥ 3.5 mg/mL (4.78 mM，饱和度未知) 的澄清溶液。

    以 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。

    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
  • 2.

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

    Solubility: ≥ 3.5 mg/mL (4.78 mM); Clear solution

    此方案可获得 ≥ 3.5 mg/mL (4.78 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 35.0 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Lee JW, et al. EphA2 targeted chemotherapy using an antibody drug conjugate in endometrial carcinoma. Clin Cancer Res. 2010 May 1;16(9):2562-70.

    [2]. Lee JJ, et al. Enzymatic prenylation and oxime ligation for the synthesis of stable and homogeneous protein-drug conjugates for targeted therapy. Angew Chem Int Ed Engl. 2015 Oct 5;54(41):12020-4.

    [3]. Kim EG, et al. Strategies and Advancement in Antibody-Drug Conjugate Optimization for Targeted CancerTherapeutics.

    [4]. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24.
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].

上海金畔生物科技有限公司 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Lee JW, et al. EphA2 targeted chemotherapy using an antibody drug conjugate in endometrial carcinoma. Clin Cancer Res. 2010 May 1;16(9):2562-70.

    [2]. Lee JJ, et al. Enzymatic prenylation and oxime ligation for the synthesis of stable and homogeneous protein-drug conjugates for targeted therapy. Angew Chem Int Ed Engl. 2015 Oct 5;54(41):12020-4.

    [3]. Kim EG, et al. Strategies and Advancement in Antibody-Drug Conjugate Optimization for Targeted CancerTherapeutics.

    [4]. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

MMAF hydrochloride(Synonyms: Monomethylauristatin F hydrochloride)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MMAF hydrochloride (Synonyms: Monomethylauristatin F hydrochloride) 纯度: 99.52%

MMAF (Monomethylauristatin F) hydrochloride 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 hydrochloride 广泛用作抗体偶联药物 (ADCs) 的细胞毒性成分，如 Vorsetuzumab mafodotin 和 SGN-CD19A。

MMAF hydrochloride(Synonyms: Monomethylauristatin F hydrochloride)

MMAF hydrochloride Chemical Structure

CAS No. : 1415246-68-2

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥800 In-stock
10 mg ￥1200 In-stock
25 mg ￥1800 In-stock
50 mg ￥2500 In-stock
100 mg ￥3400 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MMAF hydrochloride 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Toxins for Antibody-Drug Conjugate Research Library
  • Peptidomimetic Library

生物活性

MMAF (Monomethylauristatin F) hydrochloride is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF hydrochloride 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

 

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

The maximum tolerated dose in mice of MMAF (>16 mg/kg) is much higher than MMAE (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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

768.42

Formula

C39H66ClN5O8
CAS 号

1415246-68-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*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
In Vitro: 

DMSO : 27 mg/mL (35.14 mM; Need ultrasonic and warming)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3014 mL 6.5069 mL 13.0137 mL
5 mM 0.2603 mL 1.3014 mL 2.6027 mL
10 mM 0.1301 mL 0.6507 mL 1.3014 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

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 (3.25 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.25 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 (3.25 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.25 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 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 (3.25 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.25 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Lee JW, et al. EphA2 targeted chemotherapy using an antibody drug conjugate in endometrial carcinoma. Clin Cancer Res. 2010 May 1;16(9):2562-70.

    [2]. Lee JJ, et al. Enzymatic prenylation and oxime ligation for the synthesis of stable and homogeneous protein-drug conjugates for targeted therapy. Angew Chem Int Ed Engl. 2015 Oct 5;54(41):12020-4.

    [3]. Kim EG, et al. Strategies and Advancement in Antibody-Drug Conjugate Optimization for Targeted CancerTherapeutics.

    [4]. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24.
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[1].

上海金畔生物科技有限公司 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Lee JW, et al. EphA2 targeted chemotherapy using an antibody drug conjugate in endometrial carcinoma. Clin Cancer Res. 2010 May 1;16(9):2562-70.

    [2]. Lee JJ, et al. Enzymatic prenylation and oxime ligation for the synthesis of stable and homogeneous protein-drug conjugates for targeted therapy. Angew Chem Int Ed Engl. 2015 Oct 5;54(41):12020-4.

    [3]. Kim EG, et al. Strategies and Advancement in Antibody-Drug Conjugate Optimization for Targeted CancerTherapeutics.

    [4]. Doronina SO, et al. Enhanced activity of monomethylauristatin F through monoclonal antibody delivery: effects of linker technology on efficacy and toxicity. Bioconjug Chem. 2006 Jan-Feb;17(1):114-24.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务