Linker Information
General Information of This Linker
| Linker ID |
LIN00062
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| Linker Name |
4-(2-(glycylglycyl)hydrazineylidene)pentanoic acid
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| Linker Type |
Enzyme-sensitive linkers
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| Structure |
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| Formula |
C9H16N4O4
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| #Ro5 Violations (Lipinski): 0 | Molecular Weight (mw) | 244.251 | ||||
| Lipid-water partition coefficient (xlogp) | -1.5818 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 4 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 5 | |||||
| Rotatable Bond Count (rotbonds) | 7 | |||||
| Canonical smiles |
CC(CCC(=O)O)=NNC(=O)CNC(=O)CN
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| InChI |
InChI=1S/C9H16N4O4/c1-6(2-3-9(16)17)12-13-8(15)5-11-7(14)4-10/h2-5,10H2,1H3,(H,11,14)(H,13,15)(H,16,17)
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| InChIKey |
NMCVDYCDYFFPHB-UHFFFAOYSA-N
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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
P-(A5G27scrm)-PTX [Investigative]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Metastatic Tumor | ||||
| Efficacy Data | Median overall survival (mOS) |
40.5 days
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| Administration Dosage | 15 mg/kg PTX equivalent dose | ||||
| Description |
The median survival of mice in the P-(A5G27)-PTX treatment group was longer than in P-(A5G27scrm)-PTX, P-(A5G27), and free PTX-treated groups (48.50 vs 40.5, 43, and 45.5, respectively); however, differences were nonsignificant (Figure 6B).
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| In Vivo Model | 4T1 tumor-bearing mice. | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Metastatic Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.221 ± 0.055 µM
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| Administration Time | 72 h | ||||
| Description |
P-(A5G27)-PTX was ˜4-fold more toxic than the nontargeted P-(A5G27scrm)-PTX copolymer, suggesting a faster (receptor-mediated) internalization (Figure 4).
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| In Vitro Model | Mammary carcinoma | 4T1 cell | CVCL_0125 | ||
P-(A5G27)-PTX [Investigative]
Identified from the Human Clinical Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Metastatic Tumor | ||||
| Efficacy Data | Median overall survival (mOS) |
48.50 days
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| Administration Dosage | 15 mg/kg PTX equivalent dose | ||||
| Description |
The median survival of mice in the P-(A5G27)-PTX treatment group was longer than in P-(A5G27scrm)-PTX, P-(A5G27), and free PTX-treated groups (48.50 vs 40.5, 43, and 45.5, respectively); however, differences were nonsignificant (Figure 6B).
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| In Vivo Model | 4T1 tumor-bearing mice. | ||||
Obtained from the Model Organism Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Metastatic Tumor | ||||
| Efficacy Data | Survival rate |
40%
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| Administration Time | 7 days | ||||
| Administration Dosage | 15 mg/kg PTX equivalent dose | ||||
| Description |
P-(A5G27)-PTX prolonged mice survival in 7 and 20% relative to the survival rates of free PTX and nontreated mice, respectively (Figure 5).
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| In Vivo Model | B16-F10 melanoma tumor-bearing mice model. | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Metastatic Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.058 ± 0.015 µM
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| Administration Time | 72 h | ||||
| Description |
P-(A5G27)-PTX was ˜4-fold more toxic than the nontargeted P-(A5G27scrm)-PTX copolymer, suggesting a faster (receptor-mediated) internalization (Figure 4).
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| In Vitro Model | Mammary carcinoma | 4T1 cell | CVCL_0125 | ||
References
