Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0MCWQA
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| ADC Name |
Enapotamab vedotin
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| Synonyms |
AXL-107-MMAE; Humax axl adc; HuMax-AXL; HuMax-AXL-ADC
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| Organization |
Seagen Inc.; Genmab A/S
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| Drug Status |
Phase 2
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| Indication |
In total 7 Indication(s)
Cervical cancer [ICD11:2C77]
Phase 2
Endometrial cancer [ICD11:2C76]
Phase 2
Melanoma [ICD11:2C30]
Phase 2
Non-small cell lung cancer [ICD11:2C25]
Phase 2
Ovarian cancer [ICD11:2C73]
Phase 2
Sarcoma [ICD11:2B50-2B59]
Phase 2
Thyroid cancer [ICD11:2D10]
Phase 2
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| Drug-to-Antibody Ratio |
4
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| Structure |
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| Antibody Name |
AXL-107
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Antibody Info | ||||
| Antigen Name |
Tyrosine-protein kinase receptor UFO (AXL)
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Antigen Info | ||||
| Payload Name |
Monomethyl auristatin E
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Payload Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Mc-Val-Cit-PABC
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Combination Type |
Vedotin
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| Puchem SID | ||||||
| Drugbank ID | ||||||
| DrugMap ID | ||||||
| TTD ID | ||||||
| ChEBI ID | ||||||
General Information of The Activity Data Related to This ADC
Discovered Using Patient-derived Xenograft Model
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Patient-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 0.00% (Day 35) | Positive AXL expression (AXL+++/++) | ||
| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LXFE772; EGFR mutation) | ||||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 6.00% (Day 25) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
Antitumor activity of EnaV in Nonresponder.
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| In Vivo Model | NSCLC PDX model | ||||
| Experiment 3 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 13.30% (Day 21) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (0.30 mg/kg,q.d.). Enapotamab vedotin and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
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| In Vivo Model | Pancreatic cancer PDX model (PDX: PAXF1657) | ||||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 16.50% (Day 35) | Positive AXL expression (AXL+++/++) | ||
| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LU2511; EGFR mutation) | ||||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 16.50% (Day 35) | Positive AXL expression (AXL+++/++) | ||
| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LU0858; EGFR L858R mutation) | ||||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 29.60% (Day 49) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
EnaV=2 mg/kg.
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| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LU0395) | ||||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 46.90% (Day 49) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
EnaV=4 mg/kg.
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| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LU0395) | ||||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 50.00% (Day 35) | Positive AXL expression (AXL+++/++) | ||
| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LXFA677; EGFR mutation) | ||||
| Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 50.00% (Day 35) | Positive AXL expression (AXL+++/++) | ||
| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LU1868; EGFR L858R and T790Mmutations) | ||||
| Experiment 10 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 50.00% (Day 35) | Positive AXL expression (AXL+++/++) | ||
| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LCx-MR007; Osimertinib resistant) | ||||
| Experiment 11 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 56.40% (Day 15) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
Antitumor activity of EnaV in intermediate.
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| In Vivo Model | NSCLC PDX model | ||||
| Experiment 12 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 60.00% (Day 10) | Moderate AXL expression (AXL++; IHC H-score=121) | ||
| Method Description |
EnaV=4 mg/kg.
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| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LU2511) | ||||
| Experiment 13 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 66.50% (Day 35) | Moderate AXL expression (AXL++; IHC H-score=101) | ||
| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LXFA526) | ||||
| Experiment 14 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 67.00% (Day 35) | High AXL expression (AXL+++; IHC H-score=248) | ||
| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LU0395; EGFR mutation) | ||||
| Experiment 15 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 72.70% (Day 23) | Moderate AXL expression (AXL++; IHC H-score=142) | ||
| Method Description |
The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas ,esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 2 mg/kg once a week for two weeks.
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| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LXFA526) | ||||
| Experiment 16 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 84.10% (Day 14) | Moderate AXL expression (AXL++; IHC H-score=141) | ||
| Method Description |
The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 2.00 mg/kg in a single dose.
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| In Vivo Model | Pancreatic cancer PDX model (PDX: PAXF1657) | ||||
| Experiment 17 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 94.80% (Day 32) | Moderate AXL expression (AXL++; IHC H-score=183) | ||
| Method Description |
The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 2 mg/kg once a week for two weeks.
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| In Vivo Model | Cervical cancer PDX model (PDX: CV1664) | ||||
| Experiment 18 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 97.40% (Day 32) | Moderate AXL expression (AXL++; IHC H-score=104) | ||
| Method Description |
The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 4 mg/kg once a week for two weeks.
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| In Vivo Model | Cervical cancer PDX model (PDX: CV1664) | ||||
| Experiment 19 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.30% (Day 14) | Negative AXL expression (AXL-; IHC H-score=0) | ||
| Method Description |
The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 4.00 mg/kg in a single dose.
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| In Vivo Model | Pancreatic cancer PDX model (PDX: PAXF1657) | ||||
| Experiment 20 Reporting the Activity Date of This ADC | [2] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.30% (Day 21) | High AXL expression (AXL+++; IHC H-score=305) | ||
| Method Description |
The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (4 mg/kg,q.d.). Enapotamab vedotin and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
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| In Vivo Model | Pancreatic cancer PDX model (PDX: PAXF1657) | ||||
| Experiment 21 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 99.80% (Day 23) | Moderate AXL expression (AXL++; IHC H-score=117) | ||
| Method Description |
The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 4 mg/kg once a week for two weeks.
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| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LXFA526) | ||||
| Experiment 22 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 35) | Positive AXL expression (AXL+++/++) | ||
| In Vivo Model | Non-small cell lung cancer PDX model (PDX: LXFA677_R, EGFRi resistant) | ||||
| Experiment 23 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 100.00% (Day 30) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
Antitumor activity of EnaV in responder.
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| In Vivo Model | NSCLC PDX model | ||||
| Experiment 24 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 70.55 ng/mL | Moderate AXL expression (AXL++; 22,304 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
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| In Vivo Model | Melanoma PDX model (PDX: M019R.X1.CL) | ||||
| In Vitro Model | Melanoma | M019R.X1.CL cells | Homo sapiens | ||
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [4] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 1.00% (Day 34) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
Treated with MART-1 T cells.
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| In Vivo Model | SkMel-147 cell line xenograft model | ||||
| In Vitro Model | Melanoma | SK-MEL-147 cells | CVCL_3876 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [4] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 17.70% (Day 28) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
Treated with MART-1 T cells + Ctrl ADC.
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| In Vivo Model | SkMel-147 cell line xenograft model | ||||
| In Vitro Model | Melanoma | SK-MEL-147 cells | CVCL_3876 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 34.30% (Day 10) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
EnaV=2 mg/kg.
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| In Vivo Model | LU2511 in NSCLC CDX model | ||||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 40.90% (Day 21) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
EnaV=0.5 mg/kg.
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| In Vivo Model | LCLC-103H in NSCLC CDX model | ||||
| In Vitro Model | Lung large cell carcinoma | LCLC-103H cells | CVCL_1375 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [4] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 43.40% (Day 34) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
Treated with MART-1 T cells.
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| In Vivo Model | LCLC-103H xenograft model | ||||
| In Vitro Model | Lung large cell carcinoma | LCLC-103H cells | CVCL_1375 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [4] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 64.00% (Day 28) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
Treated with Ctrl T cells + EnaV.
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| In Vivo Model | SkMel-147 cell line xenograft model | ||||
| In Vitro Model | Melanoma | SK-MEL-147 cells | CVCL_3876 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [4] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 64.70% (Day 22) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
Treated with MART-1 T cells.
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| In Vivo Model | BLM cell line xenograft model | ||||
| In Vitro Model | Amelanotic melanoma | BLM cells | CVCL_7035 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 66.50% (Day 35) | Positive AXL expression (AXL+++/++) | ||
| In Vivo Model | LCLC-103H CDX model | ||||
| In Vitro Model | Lung large cell carcinoma | LCLC-103H cells | CVCL_1375 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 78.50% (Day 10) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 2 mg/kg once a week for two weeks.
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| In Vivo Model | Melanoma CDX model | ||||
| In Vitro Model | Melanoma | SK-MEL-147 cells | CVCL_3876 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [4] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 85.20% (Day 28) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
Treated with MART-1 T cells + EnaV.
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| In Vivo Model | SkMel-147 cell line xenograft model | ||||
| In Vitro Model | Melanoma | SK-MEL-147 cells | CVCL_3876 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 92.70% (Day 18) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
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| In Vivo Model | Lung cancer CDX model | ||||
| In Vitro Model | Lung large cell carcinoma | LCLC-103H cells | CVCL_1375 | ||
| Experiment 12 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 93.60% (Day 10) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
The in vivo activity of Enapotamab vedotin was evaluated in additional cell line-derived and patient-derived xenograft (PDX) models representing different cancer types, including pancreas, esophageal, lung, thyroid, ovarian, cervical cancer, melanoma and sarcoma. Enapotamab vedotin was administered at a dose of 4 mg/kg once a week for two weeks.
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| In Vivo Model | Melanoma CDX model | ||||
| In Vitro Model | Melanoma | SK-MEL-147 cells | CVCL_3876 | ||
| Experiment 13 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | 96.80% (Day 21) | Positive AXL expression (AXL+++/++) | ||
| Method Description |
EnaV=1 mg/kg.
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| In Vivo Model | LCLC-103H in NSCLC CDX model | ||||
| In Vitro Model | Lung large cell carcinoma | LCLC-103H cells | CVCL_1375 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [5] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.08 nM±0.016 nM | High AXL expression (AXL+++) | ||
| Method Description |
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
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| In Vitro Model | Lung large cell carcinoma | LCLC-103H cells | CVCL_1375 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [5] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.09 nM±0.005 nM | High AXL expression (AXL+++) | ||
| Method Description |
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [5] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.09 nM±0.005 nM | Moderate AXL expression (AXL++) | ||
| Method Description |
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
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| In Vitro Model | Lung adenocarcinoma | PC-9 cells | CVCL_B260 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [5] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.17 nM | High AXL expression (AXL+++) | ||
| Method Description |
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
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| In Vitro Model | Lung squamous cell carcinoma | Calu-1 cells | CVCL_0608 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [5] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Low AXL expression (AXL+) | ||
| Method Description |
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
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| In Vitro Model | Lung large cell carcinoma | NCI-H460 cells | CVCL_0459 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [5] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 100 nM | Low AXL expression (AXL+) | ||
| Method Description |
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-453 cells | CVCL_0418 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 5.50 ng/mL | Moderate AXL expression (AXL++; 37,235 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
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| In Vitro Model | Melanoma | A-875 cells | CVCL_4733 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 15.34 ng/mL | Moderate AXL expression (AXL++; 54,946 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
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| In Vitro Model | Cutaneous melanoma | SK-MEL-28 cells (BRAF inhibitor resistant) | CVCL_0526 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 20.70 ng/mL | High AXL expression (AXL+++; 117,665 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
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| In Vitro Model | Lung large cell carcinoma | LCLC-103H cells | CVCL_1375 | ||
| Experiment 10 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 24.30 ng/mL | Moderate AXL expression (AXL++; 46,701 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cells | CVCL_0062 | ||
| Experiment 11 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 42.06 ng/mL | Moderate AXL expression (AXL++; 35,452 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
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| In Vitro Model | Melanoma | SK-MEL-147 cells | CVCL_3876 | ||
| Experiment 12 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 68.54 ng/mL | High AXL expression (AXL+++; 169,192 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
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| In Vitro Model | Lung squamous cell carcinoma | Calu-1 cells | CVCL_0608 | ||
| Experiment 13 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 189.30 ng/mL | Moderate AXL expression (AXL++; 70,222 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
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| In Vitro Model | Melanoma | SK-MEL-2 cells (MEK inhibitor-resistant) | CVCL_0069 | ||
| Experiment 14 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 190.90 ng/mL | Moderate AXL expression (AXL++; 83,986 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
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| In Vitro Model | Skin squamous cell carcinoma | A431 cells | CVCL_0037 | ||
| Experiment 15 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 370.40 ng/mL | Moderate AXL expression (AXL++; 16,611 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
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| In Vitro Model | Amelanotic melanoma | A375/R cells | CVCL_IW10 | ||
| Experiment 16 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 887.20 ng/mL | Moderate AXL expression (AXL++; 16,611 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
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| In Vivo Model | Melanoma PDX model (PDX: M016.X1.CL) | ||||
| In Vitro Model | Cutaneous melanoma | SK-MEL-5 cells | CVCL_0527 | ||
| Experiment 17 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 1828.30 ng/mL | Moderate AXL expression (AXL++; 66,691 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
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| In Vitro Model | Lung large cell carcinoma | NCI-H1299 cells | CVCL_0060 | ||
| Experiment 18 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 2090.30 ng/mL | Moderate AXL expression (AXL++; 34,978 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
|
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| In Vitro Model | Ovarian serous cystadenocarcinoma | SK-OV-3 cells | CVCL_0532 | ||
| Experiment 19 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 2895.70 ng/mL | Moderate AXL expression (AXL++; 28,000 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
|
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| In Vitro Model | Pancreatic ductal adenocarcinoma | BxPC-3 cells | CVCL_0186 | ||
| Experiment 20 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 6881.00 ng/mL | Low AXL expression (AXL+; 9,138 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
|
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| In Vitro Model | Lung large cell carcinoma | NCI-H661 cells | CVCL_1577 | ||
| Experiment 21 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Negative AXL expression (AXL-; 528 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
|
||||
| In Vitro Model | Colon adenocarcinoma | LS174T cells | CVCL_1384 | ||
| Experiment 22 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Moderate AXL expression (AXL++; 37,506 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
|
||||
| In Vitro Model | Pleural epithelioid mesothelioma | NCI-H226 cells | CVCL_1544 | ||
| Experiment 23 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Low AXL expression (AXL+; 2,326 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
|
||||
| In Vitro Model | Pancreatic ductal adenocarcinoma | HPAF-II cells | CVCL_0313 | ||
| Experiment 24 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Negative AXL expression (AXL-; 150 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
|
||||
| In Vitro Model | Gastric tubular adenocarcinoma | NCI-N87 cells | CVCL_1603 | ||
| Experiment 25 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Negative AXL expression (AXL-; 250 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
|
||||
| In Vitro Model | Cutaneous melanoma | SK-MEL-5 cells | CVCL_0527 | ||
| Experiment 26 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Negative AXL expression (AXL-; 325 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
|
||||
| In Vitro Model | Cutaneous melanoma | SK-MEL-28 cells | CVCL_0526 | ||
| Experiment 27 Reporting the Activity Date of This ADC | [3] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | > 10.00 ug/mL | Negative AXL expression (AXL-; 100 AXL receptor copy number) | ||
| Method Description |
All cell lines except melanoma were seeded at 1 x103 cells per well in 96 well culture plates (Greiner) and incubated for 3 h at 37°C, 5% CO2.
|
||||
| In Vitro Model | Melanoma | SK-MEL-2 cells | CVCL_0069 | ||
| Experiment 28 Reporting the Activity Date of This ADC | [5] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.195±0.068 | Moderate AXL expression (AXL++) | ||
| Method Description |
Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
|
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| In Vitro Model | Glioblastoma | U-87MG cells | CVCL_0022 | ||
References
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