General Information of This Linker
Linker ID
LIN0BSKSQ
Linker Name
Mal-Val-Ala-PAB
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C22H28N4O6
Isosmiles
CC(NC(=O)C(NC(=O)CCN1C(=O)C=CC1=O)C(C)C)C(=O)Nc1ccc(CO)cc1
InChI
InChI=1S/C22H28N4O6/c1-13(2)20(25-17(28)10-11-26-18(29)8-9-19(26)30)22(32)23-14(3)21(31)24-16-6-4-15(12-27)5-7-16/h4-9,13-14,20,27H,10-12H2,1-3H3,(H,23,32)(H,24,31)(H,25,28)
InChIKey
NSHZSEBCOJNZHE-UHFFFAOYSA-N
Pharmaceutical Properties
Molecule Weight
444.488
Polar area
144.91
Complexity
32
xlogp Value
0.078
Heavy Count
32
Rot Bonds
10
Hbond acc
6
Hbond Donor
4
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
HDP-101 [Phase 2]
Revealed Based on the Cell Line Data
Click To Hide/Show 11 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.01 nM
Method Description
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
In Vitro Model Plasma cell myeloma U266B1 cells CVCL_0566
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.04 nM
Method Description
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.16 nM
Method Description
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
In Vitro Model Plasma cell myeloma MM1.S cells CVCL_8792
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.18 nM
Method Description
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
In Vitro Model Plasma cell myeloma INA-6 cells CVCL_5209
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.30 nM
Method Description
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
In Vitro Model Plasma cell myeloma LP-1 cells CVCL_0012
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
0.34 nM
Method Description
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
In Vitro Model Multiple myeloma SK-MM-1 cells CVCL_A478
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
4.83 nM
Method Description
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
In Vitro Model Plasma cell myeloma L-363 cells CVCL_1357
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
34.20 nM
Method Description
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
In Vitro Model Plasma cell myeloma OPM-2 cells CVCL_1625
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50)
142.00 nM
Method Description
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
In Vitro Model Plasma cell myeloma RPMI-8226 cells CVCL_0014
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 1000.00 nM
Method Description
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
In Vitro Model Normal HS-5 cells CVCL_3720
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 1000.00 nM
Method Description
The inhibitory activity of HDP-101 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 2 or 4 days.
In Vitro Model Osteosarcoma U2OS cells CVCL_0042
References
Ref 1 HDP-101, an Anti-BCMA Antibody-Drug Conjugate, Safely Delivers Amanitin to Induce Cell Death in Proliferating and Resting Multiple Myeloma Cells. Mol Cancer Ther. 2021 Feb;20(2):367-378.

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