Linker Information
General Information of This Linker
| Linker ID |
LIN0VKZYN
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| Linker Name |
b-glucuronidase cleavable linker
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| Antibody-Linker Relation |
Cleavable
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| Structure |
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| Formula |
C55H94N6O27S
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| Isosmiles |
COCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(=O)NCCCC[C@H](NC(=O)[C@H](CN)NC(=O)C(S)CC(=O)O)C(=O)NCCC(=O)Nc1cc(CO)ccc1O[C@@H]1O[C@H](C(=O)O)[C@@H](O)[C@H](O)[C@H]1O
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| InChI |
InChI=1S/C55H94N6O27S/c1-75-12-13-77-16-17-79-20-21-81-24-25-83-28-29-85-32-33-86-31-30-84-27-26-82-23-22-80-19-18-78-15-14-76-11-8-44(63)57-9-3-2-4-39(60-52(71)41(36-56)61-53(72)43(89)35-46(65)66)51(70)58-10-7-45(64)59-40-34-38(37-62)5-6-42(40)87-55-49(69)47(67)48(68)50(88-55)54(73)74/h5-6,34,39,41,43,47-50,55,62,67-69,89H,2-4,7-33,35-37,56H2,1H3,(H,57,63)(H,58,70)(H,59,64)(H,60,71)(H,61,72)(H,65,66)(H,73,74)/t39-,41-,43?,47-,48-,49+,50-,55+/m0/s1
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| InChIKey |
KXASUXMUBIMZFJ-BGLJFESASA-N
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| Pharmaceutical Properties |
Molecule Weight
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1303.439
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Polar area
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456.26
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Complexity
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1302.588763
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xlogp Value
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-3.8983
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Heavy Count
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89
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Rot Bonds
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57
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Hbond acc
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27
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Hbond Donor
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13
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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
SGN-CD228A [Phase 1 (Terminated)]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Related Clinical Trial | |||||
| NCT Number | NCT04042480 | Clinical Status | Phase 1 | ||
| Clinical Description |
A phase 1 study of SGN-CD228A in select advanced solid tumors.
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Discovered Using Patient-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
75.00%
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Positive CD228 expression (CD228+++/++) | ||
| Method Description |
SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 3.00 mg/kg.
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| In Vivo Model | NSCLC PDX model | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
100.00%
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Positive CD228 expression (CD228+++/++) | ||
| Method Description |
SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 1.00 mg/kg.
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| In Vivo Model | NSCLC PDX model | ||||
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
50.00%
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Positive CD228 expression (CD228+++/++) | ||
| Method Description |
SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 1.00 mg/kg.
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| In Vivo Model | Melanoma CDX model | ||||
| In Vitro Model | Cutaneous melanoma | SK-MEL-5 cells | CVCL_0527 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
62.50%
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Positive CD228 expression (CD228+++/++) | ||
| Method Description |
SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 1.00 mg/kg.
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| In Vivo Model | Melanoma CDX model | ||||
| In Vitro Model | Cutaneous melanoma | COLO 853 cells | CVCL_2003 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
100.00%
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Positive CD228 expression (CD228+++/++) | ||
| Method Description |
SGN-CD228A was evaluated for antitumor activity in melanoma and NSCLC xenograft and PDX models.SGN-CD228A was administered at a single dose of 1.00 mg/kg.
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| In Vivo Model | Squamous NSCLC CDX model | ||||
| In Vitro Model | Lung squamous cell carcinoma | Calu-1 cells | CVCL_0608 | ||
References