Linker Information

General Information of This Linker
Linker ID
LIN0AAOUH
Linker Name
L12 linker
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Formula
C190H345N19O79
Isosmiles
CN(CC1=C(CC)C=CC(NC([C@H](CCCNC(N)=O)NC([C@@H](NC(CCOCCOCCOCCN(C)C(CN(CC(N(C)CCOCCOCCOCCC(N[C@@H](C(C)C)C(N[C@H](C(NC2=CC(CN(C(NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(O)=O)=O)C)=C(CC)C=C2)=O)CCCNC(N)=O)=O)=O)=O)C(CCOCCNC(CCOCCOCCOCCOCCN3C(C=CC3=O)=O)=O)=O)=O)=O)C(C)C)=O)=O)=C1)C(NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(O)=O)=O
InChI
InChI=1S/C190H345N19O79/c1-11-163-17-19-167(155-165(163)157-206(9)189(228)196-32-44-236-54-64-246-72-77-251-81-85-255-89-93-259-97-101-263-105-109-267-113-117-271-121-125-275-129-133-279-137-141-283-145-149-287-153-151-285-147-143-281-139-135-277-131-127-273-123-119-269-115-111-265-107-103-261-99-95-257-91-87-253-83-79-249-75-70-244-62-52-234-41-27-179(218)219)198-183(222)169(15-13-29-194-187(191)226)200-185(224)181(161(3)4)202-172(211)24-38-232-50-60-241-66-56-238-46-34-204(7)177(216)159-208(174(213)26-40-230-43-31-193-171(210)23-37-231-49-59-243-69-74-248-68-58-240-48-36-209-175(214)21-22-176(209)215)160-178(217)205(8)35-47-239-57-67-242-61-51-233-39-25-173(212)203-182(162(5)6)186(225)201-170(16-14-30-195-188(192)227)184(223)199-168-20-18-164(12-2)166(156-168)158-207(10)190(229)197-33-45-237-55-65-247-73-78-252-82-86-256-90-94-260-98-102-264-106-110-268-114-118-272-122-126-276-130-134-280-138-142-284-146-150-288-154-152-286-148-144-282-140-136-278-132-128-274-124-120-270-116-112-266-108-104-262-100-96-258-92-88-254-84-80-250-76-71-245-63-53-235-42-28-180(220)221/h17-22,155-156,161-162,169-170,181-182H,11-16,23-154,157-160H2,1-10H3,(H,193,210)(H,196,228)(H,197,229)(H,198,222)(H,199,223)(H,200,224)(H,201,225)(H,202,211)(H,203,212)(H,218,219)(H,220,221)(H3,191,194,226)(H3,192,195,227)/t169-,170-,181-,182-/m0/s1
InChIKey
FIZRKHLYESTWPR-KPHGHQCLSA-N
Pharmaceutical Properties
Molecule Weight
4159.904
Polar area
1096.1
Complexity
.
xlogp Value
0.0954
Heavy Count
288
Rot Bonds
225
Hbond acc
77
Hbond Donor
15
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
NY920-P1-L12-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)
0.011 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P4 was tested in KMS-27
In Vitro Model Plasma cell myeloma, Multiple myeloma KMS-27 cells CVCL_2993
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.027 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P4 was tested in Ke97
In Vitro Model Bladder carcinoma Ke97 cells CVCL_3386
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.036 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P4 was tested in KHM-1B
In Vitro Model Plasma cell myeloma, Multiple myeloma KHM-1B cells CVCL_2972
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.07 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P4 was tested in NCI-H929
In Vitro Model Plasma cell myeloma NCI-H929 cells CVCL_1600
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.254 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P4 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)
0.531 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P4 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) > 10 nM High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P4 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)
19.67 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P4 was tested in RL
In Vitro Model Diffuse large B-cell lymphoma RL cells CVCL_1660
Experiment 9 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-L12-P4 was tested in WSU-DLCL2
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
CD74 Milatuzumab DANAPAE152C S375C-P1-L12-P4 [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)
0.03 nM
High CD74 expression (CD74 +++)
Method Description
CD74 Milatuzumab DANAPAE152C S375C-P1-L12-P4 was tested in EOL-1
In Vitro Model Chronic eosinophilic leukemia EoL-1 cells CVCL_0258
NY920-P1-L12-P3 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 8 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.033 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-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)
0.174 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P3 was tested in KMS-21-BM
In Vitro Model Multiple myeloma KMS-21-BM cells CVCL_2991
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.185 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P3 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) < 1 nM High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P3 was tested in KMS-27
In Vitro Model Plasma cell myeloma, Multiple myeloma KMS-27 cells CVCL_2993
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
1.07 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P3 was tested in AMO-1
In Vitro Model Multiple myeloma, Plasma cell myeloma AMO-1 cells CVCL_1806
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 10 nM High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P3 was tested in MOLP-8
In Vitro Model Plasma cell myeloma MOLP-8 cells CVCL_2124
Experiment 7 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-L12-P3 was tested in WSU-DLCL2
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
221.8 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P3 was tested in RL
In Vitro Model Diffuse large B-cell lymphoma RL cells CVCL_1660
NY920-P1-L12-P2 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 8 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.037 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P2 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)
0.217 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P2 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)
0.305 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P2 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)
0.38 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P2 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 nM High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P2 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) < 5 nM High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P2 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) > 50 nM High CD48 expression (CD48 +++)
Method Description
NY920-P1-L12-P2 was tested in WSU-DLCL2
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
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-L12-P2 was tested in MOLP-8
In Vitro Model Plasma cell myeloma MOLP-8 cells CVCL_2124
CD74 Milatuzumab DANAPAE152C S375C-P1-L12-P3 [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)
0.292 nM
High CD74 expression (CD74 +++)
Method Description
CD74 Milatuzumab DANAPAE152C S375C-P1-L12-P3 was tested in EOL-1
In Vitro Model Chronic eosinophilic leukemia EoL-1 cells CVCL_0258
IgG-P1-L12-P4 [Investigative]
 ADC Info 
Revealed Based on the Cell Line Data
Click To Hide/Show 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
3.05 nM
High CD48 expression (CD48 +++)
Method Description
lgG-P1-L12-P4 was tested in KMS-27
In Vitro Model Plasma cell myeloma, Multiple myeloma KMS-27 cells CVCL_2993
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
20.47 nM
High CD48 expression (CD48 +++)
Method Description
lgG-P1-L12-P4 was tested in RL
In Vitro Model Diffuse large B-cell lymphoma RL cells CVCL_1660
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50) > 50 nM High CD48 expression (CD48 +++)
Method Description
lgG-P1-L12-P4 was tested in KHM-1B
In Vitro Model Plasma cell myeloma, Multiple myeloma KHM-1B cells CVCL_2972
References
Ref 1 Antibody-drug conjugates of antineoplastic compounds and methods of use thereof