Payload Information
General Information of This Payload
| Payload ID | PAY0SOLYV |
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| Name | FD-19 |
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| Synonyms |
FD-19
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| Target | Deoxyribonucleic acid (DNA) | |||||
| Formula | C61H81N13O14 |
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| Isosmiles | CN([C@H](C(NC[C@@H](NC(C1=NC(C=CC=C2)=C2C=C1O)=O)C(N(CCCC3)[C@@H]3C4=O)=O)=O)C(C)C)C(CN(C)C(CNC(C5CCCCN5C([C@H](NC(C6=C(O)C=C7C=CC=CC7=N6)=O)COC[C@@H](N(C)C(CN(C(CN4)=O)C)=O)[C@H](CC)C)=O)=O)=O)=O |
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| InChI |
InChI=1S/C61H81N13O14/c1-9-36(4)45-34-88-33-42(68-58(84)53-47(76)27-38-19-11-13-21-40(38)66-53)61(87)74-25-17-15-23-44(74)56(82)64-30-49(78)70(6)32-51(80)72(8)54(35(2)3)59(85)62-28-41(67-57(83)52-46(75)26-37-18-10-12-20-39(37)65-52)60(86)73-24-16-14-22-43(73)55(81)63-29-48(77)69(5)31-50(79)71(45)7/h10-13,18-21,26-27,35-36,41-45,54,75-76H,9,14-17,22-25,28-34H2,1-8H3,(H,62,85)(H,63,81)(H,64,82)(H,67,83)(H,68,84)/t36-,41+,42+,43-,44?,45+,54-/m0/s1
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| InChIKey |
CZXFGNQZHVMHRX-FWVACMSVSA-N
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| Pharmaceutical Properties | Molecule Weight |
1220.396 |
Polar area |
342.83 |
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Complexity |
3184.524658 |
xlogp Value |
0.5051 |
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Heavy Count |
88 |
Rot Bonds |
7 |
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Hbond acc |
16 |
Hbond Donor |
7 |
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Each Antibody-drug Conjugate Related to This Payload
Full Information of The Activity Data of The ADC(s) Related to This Payload
37307297 ADC 33 [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.02 nM
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High FRalpha expression (FRalpha +++) | ||
| Method Description |
The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).
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| In Vitro Model | Endometrioid carcinoma of ovary, Ovarian endometrioid adenocarcinoma | IGROV cells | CVCL_C1M7 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
0.43 nM
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Moderate FRalpha expression (FRalpha++) | ||
| Method Description |
The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).
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| In Vitro Model | High grade ovarian serous adenocarcinoma | OVKATE cells | CVCL_3110 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal inhibitory Concentration (lC50) |
40.59 nM
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Low FRalpha expression (FRalpha+) | ||
| Method Description |
The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).
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| In Vitro Model | Ovarian serous adenocarcinoma | OVCAR-3 cells | CVCL_0465 | ||
References