Vc-seco-DUBA
- CAS No.
- 1345681-58-4
- Chemical Name:
- Vc-seco-DUBA
- Synonyms
- MGC018;Vc-seco-DUBA;Vc-seco-DUBA (SYD985)/Duocarmazine;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];L-Ornithinamide, N-[[2-[2-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)ethoxy]ethoxy]carbonyl]-L-valyl-N5-(aminocarbonyl)-N-[4-[7-[[[(1S)-1-(chloromethyl)-2,3-dihydro-3-[[6-[(4-hydroxybenzoyl)amino]imidazo[1,2-a]pyridin-2-yl]carbonyl]-9-methyl-1H-benz[e]indol-5-yl]oxy]carbonyl]-12-hydroxy-4-methyl-3-oxo-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 (2-((((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)oxy)carbonyl)(methyl)amino)ethyl)(2-(2-hydroxyethoxy)ethyl)carbamate;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
- CBNumber:
- CB24783895
- Molecular Formula:
- C65H75ClN12O17
- Molecular Weight:
- 1331.81
- MDL Number:
- MFCD32201146
- MOL File:
- 1345681-58-4.mol
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) |
pka | 8.08±0.15(Predicted) |
form | Solid |
color | Off-white to light yellow |
FDA UNII | DY9HDN3I6S |
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() GHS08 |
---|---|
Signal word | Danger |
Hazard statements | H373-H351-H340 |
Precautionary statements | P201-P202-P281-P308+P313-P405-P501-P260-P314-P501 |
Vc-seco-DUBA Chemical Properties,Uses,Production
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 ( based on trastuzumab and 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.
Vc-seco-DUBA Preparation Products And Raw materials
Raw materials
Preparation Products
Vc-seco-DUBA Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Xilinglab Co., Ltd. | +8618381337976 | bd@xilinglab.com | China | 86 | 58 |
Jinan Carbotang Biotech Co.,Ltd. | +8615866703830 | figo.gao@foxmail.com | China | 7287 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Levena (Suzhou) Biopharma Co., Ltd. | 0512-81877925 051281877925 | info@levena.cn | China | 48 | 58 |
Chembest Research Laboratories Limited | 021-20908456 | sales@BioChemBest.com | China | 6008 | 61 |
Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696,15000506266 15000506266 | China | 4217 | 55 | |
Twochem Co.Ltd | 021-021-58111628 15800915896 | sales@twochem.com | China | 304 | 55 |
Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9730 | 58 |
Changzhou Chenhong Biotechnology Co., Ltd. | 0519-85788828 13775037613 | sales@chemrenpharm.com | China | 3574 | 58 |
Zhengzhou Converging Chemical Co. LTD | 0371-0371-53399770 18037166334 | 2853031800@qq.com | China | 2751 | 58 |