Mc-MMAE is a protective group (maleimidocaproyl)-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Mc-MMAE is a drug-linker conjugate for ADC.
IC50 & Target
Auristatin
体外研究 (In Vitro)
Synthesis of maleimidocaproyl-MMAE (mc-MMAE) requires the addition of maleimidocaproic acid to a solution of MMAE in dichloromethane followed by the addition of diethyl cyanophosphonate and diisopropylethylamine[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.
分子量
911.18
Formula
C49H78N6O10
CAS 号
863971-24-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, 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 : 180 mg/mL (197.55 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
[1]. Sanderson RJ, et al. In vivo drug-linker stability of an anti-CD30 dipeptide-linked auristatin immunoconjugate. Clin Cancer Res. 2005 Jan 15;11(2 Pt 1):843-52.
Kinase Assay [1]
Horseradish peroxidase (HRP) is thiolated with 2-iminothiolane and conjugated to mc-MMAE to generate the HRP-MMAE reporter enzyme-drug conjugate. Briefly, a thiolation reaction mixture containing 0.2 mM HRP (8 mg/mL) and 50 mM 2-iminothiolane in 25 mM sodium borate decahydrate (Na2B4O7•10H2O) buffer (pH 9.0) is incubated for 1 hour at 37°C. Unreacted 2-iminothiolane is removed by passage through a PD-10 desalting column equilibrated in PBS (pH 7.4). Peak fractions are pooled and mc-MMAE is coupled to thiolated HRP (HRP-SH) at a molar ratio of 3:1. The final conjugation reaction mixture contained 80 μM HRP-SH (3.2 mg/mL) in sodium borate buffer [50 mM H3BO3, 50 mM NaCl (pH 8.0); 80% v/v] and 240 μM mc-MMAE in ice-cold CH3CN (20% v/v). After 30 minutes on ice, the reaction is terminated with a 20-fold molar excess of free cysteine (4.8 mM) before PD-10 chromatography. Peak fractions containing HRP-MMAE (exchanged into PBS) are pooled and evaluated for extent of modification using the thiol-reactive dye, Alexa Fluor 594 C5 maleimide[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]. Sanderson RJ, et al. In vivo drug-linker stability of an anti-CD30 dipeptide-linked auristatin immunoconjugate. Clin Cancer Res. 2005 Jan 15;11(2 Pt 1):843-52.
Gly3-VC-PAB-MMAE consists a cleavable ADC linker (Gly3-VC-PAB) and a potent tubulin inhibitor (MMAE). Gly3-VC-PAB-MMAE can be used in the synthesis of antibody-drug conjugates (ADCs)[1].
IC50 & Target
Auristatin
体外研究 (In Vitro)
ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker[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.
分子量
1294.58
Formula
C64H103N13O15
CAS 号
2684216-48-4
运输条件
Room temperature in continental US; may vary elsewhere.
Acetylene-linker-Val-Cit-PABC-MMAE Chemical Structure
CAS No. : 1411977-95-1
规格
价格
是否有货
数量
1 mg
¥3500
In-stock
5 mg
¥8500
In-stock
10 mg
¥13500
In-stock
50 mg
询价
100 mg
询价
* Please select Quantity before adding items.
生物活性
Acetylene-linker-Val-Cit-PABC-MMAE (LCB14-0602) consists the ADCs linker (Acetylene-linker-Val-Cit-PABC) and potent tubulin inhibitor (MMAE). Acetylene-linker-Val-Cit-PABC-MMAE (LCB14-0602) is a drug-linker conjugate for ADC.
IC50 & Target
Auristatin
分子量
1307.62
Formula
C67H106N10O16
CAS 号
1411977-95-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, 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。
参考文献
[1]. PROTEIN-ACTIVE AGENT CONJUGATES AND METHOD FOR PREPARING THE SAME. WIPO Patent Application WO/2012/153193.
MMAE-SMCC is a drug-linker conjugate for ADC. MMAE-SMCC is composed of a potent mitotic and a tubulin inhibitor MMAE and a linker SMCC to make antibody drug conjugate[1].
IC50 & Target[1]
Auristatin
分子量
1140.43
Formula
C58H89N7O14S
CAS 号
2021179-11-1
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Tang F, et al. One-pot N-glycosylation remodeling of IgG with non-natural sialylglycopeptides enables glycosite-specific and dual-payload antibody-drug conjugates. Org Biomol Chem. 2016 Oct 12;14(40):9501-9518.
Toxins for Antibody-Drug Conjugate Research Library
生物活性
Fmoc-MMAE is a protective group-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Fmoc-MMAE can be used in the synthesis of ADC[1].
IC50 & Target[1]
Auristatin
分子量
940.22
Formula
C54H77N5O9
CAS 号
474645-26-6
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Pan D, et al. An antibody-drug conjugate targeting a GSTA glycosite-signature epitope of MUC1 expressed by non-small cell lung cancer. Cancer Med. 2020;9(24):9529-9540.
Fmoc-Val-Cit-PAB-MMAE consists the ADCs linker (Fmoc-Val-Cit-PAB) and potent tubulin inhibitor (MMAE). Fmoc-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC.
IC50 & Target
Auristatin
分子量
1345.67
Formula
C73H104N10O14
CAS 号
1350456-56-2
运输条件
Room temperature in continental US; may vary elsewhere.
SuO-Glu-Val-Cit-PAB-MMAE consists a cleavable ADC linker (SuO-Glu-Val-Cit-PAB) and a potent tubulin inhibitor (MMAE). SuO-Glu-Val-Cit-PAB-MMAE can be used in the synthesis of antibody-drug conjugates (ADCs)[1].
IC50 & Target
Auristatin
体外研究 (In Vitro)
ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker[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.
分子量
1334.60
Formula
C67H103N11O17
CAS 号
1895916-24-1
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°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。
参考文献
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017 May;16(5):315-337.
Mal-Phe-C4-VC-PAB-MMAE is made by MMAE conjugated to Mal-Phe-C4-VC-PAB linker. Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.
IC50 & Target
Auristatin
分子量
1364.67
Formula
C72H105N11O15
CAS 号
2259318-51-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
Mal-PEG8-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC. Mal-PEG8-Val-Cit-PAB-MMAE contains a cleavable ADC linker and a potent tubulin inhibitor MMAE (HY-15162)[1].
IC50 & Target
Auristatin
体外研究 (In Vitro)
ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
1626.97
Formula
C81H131N11O23
CAS 号
2353409-69-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017 May;16(5):315-337.
Mal-PEG8-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC. Mal-PEG8-Val-Cit-PAB-MMAE contains a cleavable ADC linker and a potent tubulin inhibitor MMAE (HY-15162)[1].
IC50 & Target
Auristatin
体外研究 (In Vitro)
ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
1626.97
Formula
C81H131N11O23
CAS 号
2353409-69-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017 May;16(5):315-337.
MC-betaglucuronide-MMAE-2 is a drug-linker conjugate for ADC with potent antitumor activity by using MMAE (a tubulin polymerization inhibitor), linked via the cleavable ADC linker MC-betaglucuronide.
IC50 & Target
Auristatin
分子量
1296.46
Formula
C63H93N9O20
CAS 号
1703778-81-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
MC-betaglucuronide-MMAE-2 is a drug-linker conjugate for ADC with potent antitumor activity by using MMAE (a tubulin polymerization inhibitor), linked via the cleavable ADC linker MC-betaglucuronide.
IC50 & Target
Auristatin
分子量
1296.46
Formula
C63H93N9O20
CAS 号
1703778-81-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
MC-betaglucuronide-MMAE-2 is a drug-linker conjugate for ADC with potent antitumor activity by using MMAE (a tubulin polymerization inhibitor), linked via the cleavable ADC linker MC-betaglucuronide.
IC50 & Target
Auristatin
分子量
1296.46
Formula
C63H93N9O20
CAS 号
1703778-81-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
Azido-PEG4-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the cleavable linker Azido-PEG4-Val-Cit-PAB-OH[1].
IC50 & Target
Drug-Linker Conjugates for ADC[1]
分子量
1396.71
Formula
C69H113N13O17
CAS 号
1869126-64-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Moreadith R, et, al. Polyoxazoline antibody drug conjugates. WO2016019340A1.
Azido-PEG4-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the cleavable linker Azido-PEG4-Val-Cit-PAB-OH[1].
IC50 & Target
Drug-Linker Conjugates for ADC[1]
分子量
1396.71
Formula
C69H113N13O17
CAS 号
1869126-64-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Moreadith R, et, al. Polyoxazoline antibody drug conjugates. WO2016019340A1.
Azido-PEG4-Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the cleavable linker Azido-PEG4-Val-Cit-PAB-OH[1].
IC50 & Target
Drug-Linker Conjugates for ADC[1]
分子量
1396.71
Formula
C69H113N13O17
CAS 号
1869126-64-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Moreadith R, et, al. Polyoxazoline antibody drug conjugates. WO2016019340A1.
DBCO-PEG4-VC-PAB-MMAE consists a ADC linker (DBCO-PEG4-VC-PAB) and a tubulin polymerization inhibitor MMAE (HY-15162). DBCO-PEG4-VC-PAB-MMAE can be used in the synthesis of antibody-drug conjugates (ADCs). MMAE is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization[1].
IC50 & Target
Duocarmycins
分子量
1658.03
Formula
C88H128N12O19
CAS 号
2129164-91-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897.
MC-betaglucuronide-MMAE-1 is a drug-linker conjugate for ADC with potent antitumor activity by using MMAE (a tubulin polymerization inhibitor), linked via the cleavable ADC linker MC-betaglucuronide.
IC50 & Target
Auristatin
分子量
1323.53
Formula
C66H98N8O20
CAS 号
1703778-92-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897.
Toxins for Antibody-Drug Conjugate Research Library
生物活性
Monomethyl auristatin E (MMAE; SGD-1010) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
IC50 & Target
Auristatin
体外研究 (In Vitro)
Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30+ cancer cells and, due to its membrane permeability, is able to exert cytotoxic activity on bystander cells[1]. MMAE sensitizes colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells[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.
体内研究 (In Vivo)
Monomethyl auristatin E (MMAE) in combination with IR results in tumor growth delay, tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolongs tumor regression in xenograft models[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.
分子量
717.98
Formula
C39H67N5O7
CAS 号
474645-27-7
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897.
[2]. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87.
Cell Assay [2]
Monomethyl auristatin E (MMAE, 5 nM) and ionizing radiation (IR) treated cells are harvested and lysed in RIPA buffer with protease and phosphatase inhibitors. Thirty μg of lysate undergo electrophoresis using 4-12% Bis-Tris gels, transferred to PVDF membranes and incubated with indicated primary antibodies. Blots are developed by ECL.
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 [2]
Mice[2] 6-8 week old female athymic nu/nu mice are injected subcutaneously into thighs with 5×106 HCT-116 or PANC-1 cells in a 1:1 Matrigel and PBS solution. Mice are treated with IR or intravenous (IV) injection of ACPP-cRGD-MMAE (6 nmoles/day, 18 nmoles total, i.v.), tumor tissue is harvested, formalin fixed and paraffin embedded followed by staining with indicated antibodies. The primary antibody is used at a 1:250 dilution and is visualized using DAB as a chromagen with the UltraMap system.
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]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897.
[2]. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87.
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
IC50 & Target
Auristatin
体外研究 (In Vitro)
Monomethyl auristatin E (MMAE) is efficiently released from SGN-35 within CD30+ cancer cells and, due to its membrane permeability, is able to exert cytotoxic activity on bystander cells[1]. MMAE sensitized colorectal and pancreatic cancer cells to IR in a schedule and dose dependent manner correlating with mitotic arrest. Radiosensitization is evidenced by decreased clonogenic survival and increased DNA double strand breaks in irradiated cells[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.
体内研究 (In Vivo)
Monomethyl auristatin E (MMAE) in combination with IR results in tumor growth delay, tumor-targeted ACPP-cRGD-MMAE with IR produces a more robust and significantly prolonged tumor regression in xenograft models[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.
分子量
1316.63
Formula
C68H105N11O15
CAS 号
646502-53-6
运输条件
Room temperature in continental US; may vary elsewhere.
VcMMAE is dissolved in DMSO and then diluted with 0.9% NaCl[3].
参考文献
[1]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897.
[2]. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87.
[3]. Jianmin Fang, et al. Anti-her2 antibody and conjugate thereof. US 20160304621 A1.
Cell Assay [2]
Monomethyl auristatin E (MMAE, 5 nM) and ionizing radiation (IR) treated cells are harvested and lysed in RIPA buffer with protease and phosphatase inhibitors. 30μg of lysate undergo electrophoresis using 4-12% Bis-Tris gels, transferred to PVDF membranes and incubated with indicated primary antibodies. Blots are developed by ECL.
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 [2]
6-8 week old female athymic nu/nu mice are injected subcutaneously into thighs with 5×106 HCT-116 or PANC-1 cells in a 1:1 Matrigel and PBS solution. Mice are treated with IR or intravenous (IV) injection of ACPP-cRGD-MMAE (6 nmoles/day, 18 nmoles total, i.v.), tumor tissue is harvested, formalin fixed and paraffin embedded followed by staining with indicated antibodies. The primary antibody is used at a 1:250 dilution and is visualized using DAB as a chromagen with the UltraMap system.
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]. Okeley, et al. Intracellular Activation of SGN-35, a Potent Anti-CD30 Antibody-Drug Conjugate. Clinical Cancer Research (2010), 16(3), 888-897.
[2]. Lisa Buckel, et al. Tumor radiosensitization by monomethyl auristatin E: mechanism of action and targeted delivery. Cancer Res. 2015 Apr 1;75(7):1376-87.
[3]. Jianmin Fang, et al. Anti-her2 antibody and conjugate thereof. US 20160304621 A1.