Linker Information
General Information of This Linker
| Linker ID |
LIN0YAMYI
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|---|---|---|---|---|---|---|
| Linker Name |
H1H21234N-N297Q- LP8 lINKER
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| Linker Type |
Cathepsin-cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C110H170N16O44
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| Isosmiles |
CC([C@H](NC([C@H](NC(CCOCCOCCOCCOCCNC(CCC(N1C2=C(C=CC=C2)C3=C(N(N=N3)CCCCCOCCOCCN)C4=C(C1)C=CC=C4)=O)=O)=O)CCCCNC(COC5CCCCCC6=C5N=NN6CC7O[C@@H](O[C@H]([C@H](O8)CO)C(O)[C@@H](O)[C@H]8O[C@H]([C@H]9CO)[C@H](O)[C@@H](O)[C@H](O9)O[C@@H](C(O)[C@@H](O)[C@@H](O[C@H]([C@@H](O)[C@H](O)[C@@H](O%10)O[C@H]([C@@H](O)C[C@H](O)O%11)[C@@H]%11CO)[C@@H]%10CO)O%12)[C@H]%12CO)[C@@H](O)C(O)[C@H]7C)=O)=O)C(N[C@@H](CCCNC(N)=O)C(NC%13=CC=C(CO)C=C%13)=O)=O)C
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| InChI |
InChI=1S/C110H170N16O44/c1-59(2)83(104(151)118-67(21-16-34-115-110(112)152)102(149)116-63-27-25-61(52-127)26-28-63)119-103(150)66(117-79(135)31-38-154-42-45-157-47-48-158-46-44-156-40-35-114-78(134)29-30-81(137)124-50-62-17-8-9-18-64(62)86-84(65-19-10-11-22-68(65)124)120-122-125(86)36-14-5-15-37-153-41-43-155-39-32-111)20-12-13-33-113-80(136)58-159-71-24-7-4-6-23-69-85(71)121-123-126(69)51-72-60(3)87(139)92(144)105(161-72)167-98-75(55-130)163-107(94(146)89(98)141)169-100-77(57-132)165-109(96(148)91(100)143)170-101-76(56-131)164-108(95(147)90(101)142)168-99-74(54-129)162-106(93(145)88(99)140)166-97-70(133)49-82(138)160-73(97)53-128/h8-11,17-19,22,25-28,59-60,66-67,70-77,82-83,87-101,105-109,127-133,138-148H,4-7,12-16,20-21,23-24,29-58,111H2,1-3H3,(H,113,136)(H,114,134)(H,116,149)(H,117,135)(H,118,151)(H,119,150)(H3,112,115,152)/t60-,66+,67-,70-,71?,72?,73-,74-,75+,76+,77+,82+,83-,87?,88-,89?,90?,91+,92-,93-,94+,95+,96+,97+,98+,99-,100+,101+,105-,106-,107+,108+,109+/m0/s1
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| InChIKey |
JLPADZHQEGYUBG-XALIORMVSA-N
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| Pharmaceutical Properties |
Molecule Weight
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2420.638
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Polar area
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867.75
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Complexity
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.
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xlogp Value
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-7.3586
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Heavy Count
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170
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Rot Bonds
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67
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Hbond acc
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51
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Hbond Donor
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27
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Each Antibody-drug Conjugate Related to This Linker
Full Information of The Activity Data of The ADC(s) Related to This Linker
H1H21234N-N297Q-LP8 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Effective Concentration (EC50) |
0.619 nM
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Positive MSR1 expression (MSR1+++/++) | ||
| Method Description |
Anti-MSR1-LXR Agonist Conjugate Activity in Differentiated THP-4/LXR-Luc cells
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| In Vitro Model | Acute monoblastic/monocytic leukemia, Childhood acute monocytic leukemia | THP-1/LXR-Luc cells | CVCL_5115 | ||
References