| Identification | Back Directory | [Name]
Vc-seco-DUBA | [CAS]
1345681-58-4 | [Synonyms]
Vc-seco-DUBA
4-((2S,5S)-13-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-5-isopropyl-4,7-dioxo-2-(3-ureidopropyl)-8,11-dioxa-3,6-diazatridecanamido)benzyl (2-(((((S)-1-(chloromethyl)-3-(6-(4-hydroxybenzamido)imidazo[1,2-a]pyridine-2-carbonyl)-9-methyl-2,3-dihydro-1H-benzo[e]
4-((2S,5S)-13-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-5-isopropyl-4,7-dioxo-2-(3-ureidopropyl)-8,11-dioxa-3,6-diazatridecanamido)benzyl (2-(((((S)-1-(chloromethyl)-3-(6-(4-hydroxybenzamido)imidazo[1,2-a]pyridine-2-carbonyl)-9-methyl-2,3-dihydro-1H-benzo[e]indol-5-yl)oxy)carbonyl)(2-(2-hydroxyethoxy)ethyl)amino)ethyl)(methyl)carbamate | [EINECS(EC#)]
813-138-9 | [Molecular Formula]
C65H75ClN12O17 | [MDL Number]
MFCD32201146 | [MOL File]
1345681-58-4.mol | [Molecular Weight]
1331.81 |
| Chemical Properties | Back Directory | [density ]
1.43±0.1 g/cm3(Predicted) | [solubility ]
DMSO : 146.67 mg/mL (110.13 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [pka]
8.08±0.15(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Description]
Vc-seco-DUBA is a novel HER2-targeting antibody–drug conjugate used in the treatment of cancer. Trastuzumab duocarmycin, also known as SYD985, is a new HER2-targeted ADC with a cleavable payload (vc-seco-DUBA) conjugated with trastuzumab[1]. | [Uses]
Vc-seco-DUBA, a cleavable linker-duocarmycin payload, could used to synthsis SYD985 with trastuzumab. | [Hazard]
Vc-seco-DUBA is Danger.
H340 (100%): May cause genetic defects [Danger Germ cell mutagenicity]
H351 (100%): Suspected of causing cancer [Warning Carcinogenicity]
H373 (100%): Causes damage to organs through prolonged or repeated exposure [Warning Specific target organ toxicity, repeated exposure]
| [Cytotoxicity]
SYD985 (Vc-seco-DUBA) and T-DM1 induced similar ADCC in the presence of peripheral blood lymphocytes (PBL) against EOC cell lines with differential HER2/neu expression. In contrast, SYD985 was 3 to 42 fold more cytotoxic in the absence of PBL when compared to T-DM1 (p?<?0.0001). Unlike T-DM1, SYD985 induced efficient bystander killing of HER2/neu 0/1+ tumor cells when admixed with HER2/neu 3+ EOC cells. In vivo studies confirmed that SYD985 is significantly more active than T-DM1 against HER2/neu 3+ EOC xenografts[2]. | [References]
[1] Ubink R, et al. Unraveling the interaction between carboxylesterase 1c and the antibody-drug conjugate SYD985: improved translational PKPD by using CES1c knockout mice. Molecular Cancer Therapeutics, 2018; 17: 2389–2398.
[2] Menderes G, et al. SYD985, a novel duocarmycin-based HER2-targeting antibody-drug conjugate, shows promising antitumor activity in epithelial ovarian carcinoma with HER2/Neu expression. Gynecologic Oncology, 2017; 146: 179-186.
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| Company Name: |
Twochem Co.Ltd
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| Tel: |
021-021-58111628 15800915896 |
| Website: |
www.twochem.com |
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