Linker Information
General Information of This Linker
| Linker ID |
LIN00035
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| Linker Name |
4-(Disulfanyl)butanoic acid
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| Linker Type |
GSH concentration-sensitive linkers
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| Structure |
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| Formula |
C4H8O2S2
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| #Ro5 Violations (Lipinski): 0 | Molecular Weight (mw) | 152.2 | ||||
| Lipid-water partition coefficient (xlogp) | 0.8 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 2 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 4 | |||||
| Rotatable Bond Count (rotbonds) | 4 | |||||
| PubChem CID | ||||||
| Canonical smiles |
C(CC(=O)O)CSS
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| InChI |
InChI=1S/C4H8O2S2/c5-4(6)2-1-3-8-7/h7H,1-3H2,(H,5,6)
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| InChIKey |
NPNLDKQOMINEPE-UHFFFAOYSA-N
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| IUPAC Name |
4-(disulfanyl)butanoic acid
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Each Peptide-drug Conjugate Related to This Linker
Full Information of The Activity Data of The PDC(s) Related to This Linker
SN38-HKD [Investigative]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Triple-negative breast cancer | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
43% (Day 14)
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| Administration Time | 4-injection regimen (on day 0, 2, 4, and 6) | ||||
| Administration Dosage | 10 mg/kg | ||||
| Evaluation Method | Tumor volume detection assay | ||||
| MOA of PDC |
N38-HKD increases infiltration, activity, and viability of CD8+T cells, and thus inhibits the growth of primary tumors and pulmonary metastasis. This study highlights the synergistic modulation of cancerous cells and TECs with integrin-targeting PDC filaments as a promising strategy for TNBC chemoimmunotherapy.
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| Description |
SN38-HKD/RGDR slowed the 4T1 tumor growth by 74%, while irinotecan and SN38-HKD only showed 28% and 43% tumor growth inhibition, respectively, which was further confirmed by its capability in reducing tumor burden.
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| In Vivo Model | 4T1 tumor-bearing mice. | ||||
| In Vitro Model | Mammary carcinoma | 4T1 cell | CVCL_0125 | ||
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Triple-negative breast cancer | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
40% (Day 18)
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| Administration Time | 4-injection regimen (on day 0, 2, 4, and 6) | ||||
| Administration Dosage | 10 mg/kg | ||||
| Evaluation Method | Tumor volume detection assay | ||||
| MOA of PDC |
N38-HKD increases infiltration, activity, and viability of CD8+T cells, and thus inhibits the growth of primary tumors and pulmonary metastasis. This study highlights the synergistic modulation of cancerous cells and TECs with integrin-targeting PDC filaments as a promising strategy for TNBC chemoimmunotherapy.
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| Description |
SN38-HKD/RGDR slowed the 4T1 tumor growth by 74%, while irinotecan and SN38-HKD only showed 28% and 43% tumor growth inhibition, respectively, which was further confirmed by its capability in reducing tumor burden.
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| In Vivo Model | EMT6 tumor-bearing mice. | ||||
| In Vitro Model | Mammary gland malignant neoplasms | EMT6 cell | CVCL_1923 | ||
SN38-HKD/RGDR [Investigative]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Triple-negative breast cancer | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
74% (Day 14)
|
|||
| Administration Time | 4-injection regimen (on day 0, 2, 4, and 6) | ||||
| Administration Dosage | 10 mg/kg | ||||
| Evaluation Method | Tumor volume detection assay | ||||
| MOA of PDC |
N38-HKD/RGDR increases infiltration, activity, and viability of CD8+ T cells, and thus inhibits the growth of primary tumors and pulmonary metastasis. This study highlights the synergistic modulation of cancerous cells and TECs with integrin-targeting PDC filaments as a promising strategy for TNBC chemoimmunotherapy.
|
||||
| Description |
SN38-HKD/RGDR slowed the 4T1 tumor growth by 74%, while irinotecan and SN38-HKD only showed 28% and 43% tumor growth inhibition, respectively, which was further confirmed by its capability in reducing tumor burden.
|
||||
| In Vivo Model | 4T1 tumor-bearing mice. | ||||
| In Vitro Model | Mammary carcinoma | 4T1 cell | CVCL_0125 | ||
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Triple-negative breast cancer | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
75% (Day 18)
|
|||
| Administration Time | 4-injection regimen (on day 0, 2, 4, and 6) | ||||
| Administration Dosage | 10 mg/kg | ||||
| Evaluation Method | Tumor volume detection assay | ||||
| MOA of PDC |
N38-HKD/RGDR increases infiltration, activity, and viability of CD8+T cells, and thus inhibits the growth of primary tumors and pulmonary metastasis. This study highlights the synergistic modulation of cancerous cells and TECs with integrin-targeting PDC filaments as a promising strategy for TNBC chemoimmunotherapy.
|
||||
| Description |
SN38-HKD/RGDR slowed the 4T1 tumor growth by 74%, while irinotecan and SN38-HKD only showed 28% and 43% tumor growth inhibition, respectively, which was further confirmed by its capability in reducing tumor burden.
|
||||
| In Vivo Model | EMT6 tumor-bearing mice. | ||||
| In Vitro Model | Mammary gland malignant neoplasms | EMT6 cell | CVCL_1923 | ||
References