Linker Information
General Information of This Linker
| Linker ID |
LIN0OYJEN
|
|||||
|---|---|---|---|---|---|---|
| Linker Name |
ADC-4 Linker
|
|||||
| Linker Type |
Cathepsin-cleavable linker
|
|||||
| Antibody-Linker Relation |
Cleavable
|
|||||
| Structure |
|
|||||
| Formula |
C134H199N17O48
|
|||||
| Isosmiles |
CC([C@H](NC([C@@H](NC(CCOCCOCCOCCOCCOCCOCCOCCOC)=O)CCCCNC(CCN1C2=CC=C(NC(CCC(NCCCC[C@H](NC(CCOCCOCCOCCOCCOCCOCCOCCOC)=O)C(N[C@@H](C(C)C)C(N[C@@H](C)C(NC3=C(O[C@H]4[C@H](O)[C@@H](O)[C@H](O)[C@@H](C(O)=O)O4)C=C(C=C3)COC(N(CCC(C5=CC=CC=C5N=C6C7=CC([C@@]8(O)CC)=C9COC8=O)=C6CN7C9=O)C(C)C)=O)=O)=O)=O)=O)=O)C=C2C=C1CN(NC)C)=O)=O)C(N[C@@H](C)C(NC%10=C(O[C@H]%11[C@H](O)[C@@H](O)[C@H](O)[C@@H](C(O)=O)O%11)C=C(C=C%10)CO)=O)=O)C
|
|||||
| InChI |
InChI=1S/C134H199N17O48/c1-14-134(177)95-75-102-112-93(77-151(102)127(170)94(95)80-194-132(134)175)91(92-21-15-16-22-96(92)143-112)33-39-149(83(6)7)133(176)195-79-87-26-29-98(104(72-87)197-131-118(163)114(159)116(161)120(199-131)129(173)174)145-122(165)85(9)139-126(169)111(82(4)5)146-123(166)99(141-108(156)35-41-180-47-49-184-55-57-188-63-65-192-69-67-190-61-59-186-53-51-182-45-43-178-12)23-17-19-37-136-105(153)31-32-107(155)140-89-27-30-101-88(73-89)74-90(76-148(11)135-10)150(101)40-34-106(154)137-38-20-18-24-100(142-109(157)36-42-181-48-50-185-56-58-189-64-66-193-70-68-191-62-60-187-54-52-183-46-44-179-13)124(167)147-110(81(2)3)125(168)138-84(8)121(164)144-97-28-25-86(78-152)71-103(97)196-130-117(162)113(158)115(160)119(198-130)128(171)172/h15-16,21-22,25-30,71-75,81-85,99-100,110-111,113-120,130-131,135,152,158-163,177H,14,17-20,23-24,31-70,76-80H2,1-13H3,(H,136,153)(H,137,154)(H,138,168)(H,139,169)(H,140,155)(H,141,156)(H,142,157)(H,144,164)(H,145,165)(H,146,166)(H,147,167)(H,171,172)(H,173,174)/t84-,85-,99-,100-,110-,111-,113-,114-,115-,116-,117+,118+,119-,120-,130+,131+,134-/m0/s1
|
|||||
| InChIKey |
DCFHVKBUEILDLA-ORRLLZSFSA-N
|
|||||
| Pharmaceutical Properties |
Molecule Weight
|
2816.137
|
Polar area
|
852.07
|
||
|
Complexity
|
.
|
xlogp Value
|
0.7497
|
|||
|
Heavy Count
|
199
|
Rot Bonds
|
98
|
|||
|
Hbond acc
|
51
|
Hbond Donor
|
22
|
|||
Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
WO2025019787A1 ADC-8 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.318 nM
|
Positive huROR1 expression (huROR1+++/++) | ||
| Method Description |
ADC-8 was tested in HEK293-huROR1 cells, starting with a top concentration of 60 nM (4x the final top concentration),each of the samples was serially diluted 5 times (1:4 for ADC-8), 5 days.
|
||||
| In Vitro Model | Normal | HEK293-huROR1 cells | CVCL_0045 | ||
References
