General Information of This Linker
Linker ID
LIN0MFHKQ
Linker Name
Alkyl phosphoramide-PEG24-Val-Cit-PAB
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C75H131N6O31P
Isosmiles
C#CP(=O)(Nc1ccc(C(=O)NC(C(=O)NC(CCCNC(N)=O)C(=O)Nc2ccc(CO)cc2)C(C)C)cc1)OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO
InChI
InChI=1S/C75H131N6O31P/c1-4-113(88,81-69-13-9-67(10-14-69)72(84)80-71(65(2)3)74(86)79-70(6-5-15-77-75(76)87)73(85)78-68-11-7-66(64-83)8-12-68)112-63-62-111-61-60-110-59-58-109-57-56-108-55-54-107-53-52-106-51-50-105-49-48-104-47-46-103-45-44-102-43-42-101-41-40-100-39-38-99-37-36-98-35-34-97-33-32-96-31-30-95-29-28-94-27-26-93-25-24-92-23-22-91-21-20-90-19-18-89-17-16-82/h1,7-14,65,70-71,82-83H,5-6,15-64H2,2-3H3,(H,78,85)(H,79,86)(H,80,84)(H,81,88)(H3,76,77,87)
InChIKey
PLVBDTJIUHDXIM-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
1643.858
Polar area
433.5
Complexity
113
xlogp Value
2.0917
Heavy Count
113
Rot Bonds
86
Hbond acc
31
Hbond Donor
8
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
Brentuximab-8 [Clinical candidate]
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.60 pM
High CD30 expression (CD30+++)
Method Description
The inhibitory activity of Brentuximab-8 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model ALK-positive anaplastic large cell lymphoma Karpas-299 cells CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
1.50 pM
High CD30 expression (CD30+++)
Method Description
The inhibitory activity of Brentuximab-8 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Hodgkin lymphoma L-540 cells CVCL_1362
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.20 pM
High CD30 expression (CD30+++)
Method Description
The inhibitory activity of Brentuximab-8 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Anaplastic large cell lymphoma SU-DHL-1 cells CVCL_0538
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
5.10 pM
High CD30 expression (CD30+++)
Method Description
The inhibitory activity of Brentuximab-8 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model Adult acute myeloid leukemia HL-60 cells CVCL_0002
References
Ref 1 https://tubulis.com/

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