Peptide Information
General Information of This Peptide
| Peptide ID |
PEP00078
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| Peptide Name |
P-(A5G27scrm)-FITC
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| Structure |
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| Sequence |
KVLFGFLRIYSRIN-NH2
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| Peptide Type |
Linear
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| Receptor Name |
CD44 antigen (CD44)
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Receptor Info | ||||
| PDC Transmembrane Types | Cell targeting peptides (CTPs) | |||||
| Formula |
C83H133N23O17
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| Isosmiles |
[H]NCCCC[C@H](N[H])C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC/N=C(\N)N[H])C(=O)N[C@]([H])(C(=O)N[C@@H](Cc1ccc(O[H])cc1)C(=O)N[C@@H](CO[H])C(=O)N[C@@H](CCC/N=C(\N)N[H])C(=O)N[C@]([H])(C(=O)N[C@@H](CC(=O)N[H])C(N)=O)[C@@H](C)CC)[C@@H](C)CC)C(C)C
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| InChI |
InChI=1S/C83H133N23O17/c1-11-48(9)67(80(122)98-57(69(87)111)42-64(86)109)105-73(115)56(29-22-36-93-83(90)91)97-78(120)63(44-107)103-77(119)62(41-52-30-32-53(108)33-31-52)102-81(123)68(49(10)12-2)106-72(114)55(28-21-35-92-82(88)89)96-74(116)58(37-45(3)4)99-76(118)61(40-51-25-17-14-18-26-51)95-65(110)43-94-71(113)60(39-50-23-15-13-16-24-50)100-75(117)59(38-46(5)6)101-79(121)66(47(7)8)104-70(112)54(85)27-19-20-34-84/h13-18,23-26,30-33,45-49,54-63,66-68,107-108H,11-12,19-22,27-29,34-44,84-85H2,1-10H3,(H2,86,109)(H2,87,111)(H,94,113)(H,95,110)(H,96,116)(H,97,120)(H,98,122)(H,99,118)(H,100,117)(H,101,121)(H,102,123)(H,103,119)(H,104,112)(H,105,115)(H,106,114)(H4,88,89,92)(H4,90,91,93)/t48-,49-,54-,55-,56-,57-,58-,59-,60-,61-,62-,63-,66-,67-,68-/m0/s1
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| InChIKey |
FRUJCYBMVDKHFQ-NWDMPNHUSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1725.121
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Polar area
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685.78
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Complexity
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1724.02498
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xlogp Value
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-3.8892
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Heavy Count
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123
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Rot Bonds
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61
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Hbond acc
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21
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Hbond Donor
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23
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The Activity Data of This Peptide
| Peptide Activity Information 1 | [1] | |||||
| Percentage of labeled cells | 62% | |||||
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| Binding Affinity Assay |
4T1-Luc and B16-F10 cells were collected after trypsinization of cell monolayers. Cells (5 105) were incubated in 3% BSA for 30 min at room temperature and then treated with 50 μg/mL of the FITC-labeled P-(A5G27) or P-(A5G27scrm) in 0.5 mL of PBS containing 1% BSA for 1 h at 4 °C or for 4 h at 37 °C. Cells were then washed twice with PBS, and the fluorescence intensity was analyzed by Guava easyCyte flow cytometer (EMD Millipore, excitation at 488 nm and emission at 525 nm).
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| Experimental Condition | 4T1-Luc and B16-F10 cells | |||||
Each Peptide-drug Conjugate Related to This Peptide
Full Information of The Activity Data of The PDC(s) Related to This Peptide
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 | ||
References