Linker Information

General Information of This Linker
Linker ID
LIN0ULDHZ
Linker Name
L17 linker
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C186H337N19O78
Isosmiles
CN(CC(C=C(NC([C@@H](NC([C@@H](NC(CCOCCOCCC(NCCN(C(CCOCCNC(CCOCCOCCOCCOCCN1C(C=CC1=O)=O)=O)=O)CCNC(CCOCCOCCOCCC(N[C@@H](C(C)C)C(N[C@H](C(NC2=CC(CN(C)C(NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(O)=O)=O)=C(C)C=C2)=O)CCCNC(N)=O)=O)=O)=O)=O)=O)C(C)C)=O)CCCNC(N)=O)=O)C=C3)=C3C)C(NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(O)=O)=O
InChI
InChI=1S/C186H337N19O78/c1-157(2)177(181(220)198-165(11-9-27-192-183(187)222)179(218)196-163-15-13-159(5)161(153-163)155-202(7)185(224)194-32-46-234-56-64-241-70-75-246-79-83-250-87-91-254-95-99-258-103-107-262-111-115-266-119-123-270-127-131-274-135-139-278-143-147-282-151-149-280-145-141-276-137-133-272-129-125-268-121-117-264-113-109-260-105-101-256-97-93-252-89-85-248-81-77-244-73-68-239-62-54-232-43-25-175(214)215)200-170(209)22-40-230-50-49-227-37-19-167(206)189-29-34-204(172(211)24-42-226-45-31-191-169(208)21-39-229-52-60-238-67-72-243-66-58-236-48-36-205-173(212)17-18-174(205)213)35-30-190-168(207)20-38-228-51-59-237-61-53-231-41-23-171(210)201-178(158(3)4)182(221)199-166(12-10-28-193-184(188)223)180(219)197-164-16-14-160(6)162(154-164)156-203(8)186(225)195-33-47-235-57-65-242-71-76-247-80-84-251-88-92-255-96-100-259-104-108-263-112-116-267-120-124-271-128-132-275-136-140-279-144-148-283-152-150-281-146-142-277-138-134-273-130-126-269-122-118-265-114-110-261-106-102-257-98-94-253-90-86-249-82-78-245-74-69-240-63-55-233-44-26-176(216)217/h13-18,153-154,157-158,165-166,177-178H,9-12,19-152,155-156H2,1-8H3,(H,189,206)(H,190,207)(H,191,208)(H,194,224)(H,195,225)(H,196,218)(H,197,219)(H,198,220)(H,199,221)(H,200,209)(H,201,210)(H,214,215)(H,216,217)(H3,187,192,222)(H3,188,193,223)/t165-,166-,177-,178-/m0/s1
InChIKey
WYUCSFVPUXMHKP-JOBAYZJRSA-N
Pharmaceutical Properties
Molecule Weight
4087.797
Polar area
1104.45
Complexity
.
xlogp Value
-0.33336
Heavy Count
283
Rot Bonds
222
Hbond acc
76
Hbond Donor
17
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
NY920-P1-L17-P4 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 9 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.031 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P4 was tested in KNM-1B
In Vitro Model Plasma cell myeloma, Multiple myeloma KHM-1B cells CVCL_2972
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.041 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P4 was tested in KMS-27
In Vitro Model Plasma cell myeloma, Multiple myeloma KMS-27 cells CVCL_2993
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.133 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P4 was tested in NCI-H929
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.33 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P4 was tested in KMS-21-BM
In Vitro Model Multiple myeloma KMS-21-BM cells CVCL_2991
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.11 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P4 was tested in Ke97
In Vitro Model Bladder carcinoma Ke97 cells CVCL_3386
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.48 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P4 was tested in WSU-DLCL2
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.49 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P4 was tested in AMO-1
In Vitro Model Multiple myeloma, Plasma cell myeloma AMO-1 cells CVCL_1806
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 5 nM High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P4 was tested in MOLP-8
In Vitro Model Plasma cell myeloma MOLP-8 cells CVCL_2124
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
23.6 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P4 was tested in RL
In Vitro Model Diffuse large B-cell lymphoma RL cells CVCL_1660
NY920-P1-L17-P3 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 9 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.046 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P3 was tested in KHM-1B
In Vitro Model Plasma cell myeloma, Multiple myeloma KHM-1B cells CVCL_2972
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.121 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P3 was tested in NCI-H929
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 (lC50)
0.257 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P3 was tested in KMS-27
In Vitro Model Plasma cell myeloma, Multiple myeloma KMS-27 cells CVCL_2993
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.287 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P3 was tested in Ke97
In Vitro Model Bladder carcinoma Ke97 cells CVCL_3386
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.32 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P3 was tested in KMS-21-BM
In Vitro Model Multiple myeloma KMS-21-BM cells CVCL_2991
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.832 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P3 was tested in AMO-1
In Vitro Model Multiple myeloma, Plasma cell myeloma AMO-1 cells CVCL_1806
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 5 nM High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P3 was tested in MOLP-8
In Vitro Model Plasma cell myeloma MOLP-8 cells CVCL_2124
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 50 nM High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P3 was tested in WSU-DLCL2
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 250 nM High CD48 expression (CD48 +++)
Method Description
NY920-P1-L17-P3 was tested in RL
In Vitro Model Diffuse large B-cell lymphoma RL cells CVCL_1660
CD74 Milatuzumab DANAPAE152C S375C-P1-L17-P2 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.122 nM
High CD74 expression (CD74 +++)
Method Description
CD74 Milatuzumab DANAPAE152C S375C-P1-L17-P2 was tested in EOL-1
In Vitro Model Chronic eosinophilic leukemia EoL-1 cells CVCL_0258
References
Ref 1 Antibody-drug conjugates of antineoplastic compounds and methods of use thereof