General Information of This Linker
Linker ID
LIN0VXZMV
Linker Name
L19 linker
Linker Type
Cathepsin-cleavable linker
Antibody-Linker Relation
Cleavable
Structure
Formula
C178H317N19O76
Isosmiles
CC([C@H](NC(OCCN(CCOC(N[C@H](C(N[C@@H](CCCNC(N)=O)C(NC1=CC=C(C)C(COCC2=CN(N=N2)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(O)=O)=C1)=O)=O)C(C)C)=O)C(CCNC(CCOCCOCCOCCOCCOCCOCCOCCOCCN3C(C=CC3=O)=O)=O)=O)=O)C(N[C@@H](CCCNC(N)=O)C(NC4=CC=C(C)C(COCC5=CN(N=N5)CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(O)=O)=C4)=O)=O)C
InChI
InChI=1S/C178H317N19O76/c1-151(2)169(173(208)186-161(9-7-21-182-175(179)210)171(206)184-157-13-11-153(5)155(143-157)147-270-149-159-145-195(192-190-159)26-32-217-40-46-223-52-58-229-64-70-235-77-81-240-85-89-244-93-97-248-101-105-252-109-113-256-117-121-260-125-129-264-133-137-268-141-139-266-135-131-262-127-123-258-119-115-254-111-107-250-103-99-246-95-91-242-87-83-238-79-74-233-68-62-227-56-50-221-44-38-215-30-19-167(202)203)188-177(212)272-35-24-194(164(199)17-23-181-163(198)18-29-214-37-43-220-49-55-226-61-67-232-73-76-237-72-66-231-60-54-225-48-42-219-34-28-197-165(200)15-16-166(197)201)25-36-273-178(213)189-170(152(3)4)174(209)187-162(10-8-22-183-176(180)211)172(207)185-158-14-12-154(6)156(144-158)148-271-150-160-146-196(193-191-160)27-33-218-41-47-224-53-59-230-65-71-236-78-82-241-86-90-245-94-98-249-102-106-253-110-114-257-118-122-261-126-130-265-134-138-269-142-140-267-136-132-263-128-124-259-120-116-255-112-108-251-104-100-247-96-92-243-88-84-239-80-75-234-69-63-228-57-51-222-45-39-216-31-20-168(204)205/h11-16,143-146,151-152,161-162,169-170H,7-10,17-142,147-150H2,1-6H3,(H,181,198)(H,184,206)(H,185,207)(H,186,208)(H,187,209)(H,188,212)(H,189,213)(H,202,203)(H,204,205)(H3,179,182,210)(H3,180,183,211)/t161-,162-,169-,170-/m0/s1
InChIKey
UCZAPVUDDTUPIS-JRMPWWJNSA-N
Pharmaceutical Properties
Molecule Weight
3939.551
Polar area
1061.45
Complexity
.
xlogp Value
1.39444
Heavy Count
273
Rot Bonds
214
Hbond acc
80
Hbond Donor
13
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
NY920-P1-L19-P2 [Investigative]
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-L19-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)
0.06 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L19-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)
0.146 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L19-P2 was tested in KMS-21-BM
In Vitro Model Multiple myeloma KMS-21-BM cells CVCL_2991
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.16 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L19-P2 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)
0.216 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L19-P2 was tested in KMS-27
In Vitro Model Plasma cell myeloma, Multiple myeloma KMS-27 cells CVCL_2993
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal inhibitory Concentration (lC50)
0.407 nM
High CD48 expression (CD48 +++)
Method Description
NY920-P1-L19-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) > 10 nM High CD48 expression (CD48 +++)
Method Description
NY920-P1-L19-P2 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-L19-P2 was tested in WSU-DLCL2
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
References
Ref 1 Antibody-drug conjugates of antineoplastic compounds and methods of use thereof