Antibody Information

General Information of This Antibody (ID: ANTI0WHQPD)

Antibody Name	enapotamab
Antigen Name	Axl	Antigen Info
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence	EVQLLESGGGLVQPGGSLRLSCAASGFTFSSYAMNWVRQAPGKGLEWVSTTSGSGASTYY ADSVKGRFTISRDNSKNTLYLQMNSLRAEDTAVYYCAKIWIAFDIWGQGTMVTVSSASTK GPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYS LSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPAPELLGGPSVF LFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYR VVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKN QVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGN VFSCSVMHEALHNHYTQKSLSLSPG Click to Show/Hide
Heavy Chain Varible Domain	EVQLLESGGGLVQPGGSLRLSCAASGFTFSSYAMNWVRQAPGKGLEWVSTTSGSGASTYY ADSVKGRFTISRDNSKNTLYLQMNSLRAEDTAVYYCAKIWIAFDIWGQGTMVTVSSASTK GPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSGLYS LSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPAPELLGGPSVF LFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYR VVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEMTKN QVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGN VFSCSVMHEALHNHYTQKSLSLSPG Click to Show/Hide
Light Chain Sequence	EIVLTQSPGTLSLSPGERATLSCRASQSVSSSYLAWYQQKPGQAPRLLIYGASSRATGIP DRFSGSGSGTDFTLTISRLEPEDFAVYYCQQYGSSPYTFGQGTKLEIKRTVAAPSVFIFP PSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTL TLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC Click to Show/Hide
Light Chain Varible Domain	EIVLTQSPGTLSLSPGERATLSCRASQSVSSSYLAWYQQKPGQAPRLLIYGASSRATGIP DRFSGSGSGTDFTLTISRLEPEDFAVYYCQQYGSSPYTFGQGTKLEIKRTVAAPSVFIFP PSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTL TLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC Click to Show/Hide

Each Antibody-drug Conjugate Related to This Antibody

Full Information of The Activity Data of The ADC(s) Related to This Antibody

Enapotamab vedotin [Phase 1/2 (discontinued)]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Objective Response Rate (ORR)	19%
Patients Enrolled	Eligible participants must have advanced/metastatic solid tumors refractory to standard therapy, measurable disease, and adequate organ function (ECOG 0-1). Exclusions cover uncontrolled cardiac disease, recent thrombosis, active infections, prior auristatin therapy, major surgery within 4 weeks, pregnancy, and significant comorbidities (e.g., Grade 2+ neuropathy, pneumonitis). Click to Show/Hide
Administration Dosage	Participants in all cohorts of the trial (both in escalation and expansion phase) will be administered enapotamab vedotin (HuMax-AXL-ADC) intravenously (IV).
*Related Clinical Trial*
NCT Number	NCT02988817	Clinical Status	PHASE1\|\|\|PHASE2
Clinical Description	First-in-human, Open-label, Dose-escalation Trial With Expansion Cohorts to Evaluate Safety of Axl-specific Antibody-drug Conjugate (Enapotamab Vedotin, HuMax®-AXL-ADC) in Patients With Solid Tumors
Primary Endpoint	Safety measures include dose-limiting toxicities (DLTs) during Cycle 1 (Grade 4 hematologic events, severe non-hematologic AEs, and infusion reactions) and treatment-emergent adverse events (TEAEs), including serious events (TESAEs), ≥Grade 3 toxicities per NCI-CTCAE v4.03, and lab abnormalities, monitored up to 1130 days post-dose.
Other Endpoint	Pharmacokinetic analysis evaluates conjugated enapotamab vedotin and free MMAE parameters (AUC0-inf, AUC0-last, Cmax, CL, Tmax, t1/2, Vss) across dosing regimens (1Q3W, 3Q4W). Secondary outcomes include ADA development and efficacy metrics (OR per RECIST v1.1, CA-125 response, DoR, PFS, OS, AXL expression changes) in solid tumor patients.
Experiment 2 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Disease control rate (DCR)	50%
Patients Enrolled	Eligible participants must have advanced/metastatic solid tumors refractory to standard therapy, measurable disease, and adequate organ function (ECOG 0-1). Exclusions cover uncontrolled cardiac disease, recent thrombosis, active infections, prior auristatin therapy, major surgery within 4 weeks, pregnancy, and significant comorbidities (e.g., Grade 2+ neuropathy, pneumonitis). Click to Show/Hide
Administration Dosage	Participants in all cohorts of the trial (both in escalation and expansion phase) will be administered enapotamab vedotin (HuMax-AXL-ADC) intravenously (IV).
*Related Clinical Trial*
NCT Number	NCT02988817	Clinical Status	PHASE1\|\|\|PHASE2
Clinical Description	First-in-human, Open-label, Dose-escalation Trial With Expansion Cohorts to Evaluate Safety of Axl-specific Antibody-drug Conjugate (Enapotamab Vedotin, HuMax®-AXL-ADC) in Patients With Solid Tumors
Primary Endpoint	Safety measures include dose-limiting toxicities (DLTs) during Cycle 1 (Grade 4 hematologic events, severe non-hematologic AEs, and infusion reactions) and treatment-emergent adverse events (TEAEs), including serious events (TESAEs), ≥Grade 3 toxicities per NCI-CTCAE v4.03, and lab abnormalities, monitored up to 1130 days post-dose.
Other Endpoint	Pharmacokinetic analysis evaluates conjugated enapotamab vedotin and free MMAE parameters (AUC0-inf, AUC0-last, Cmax, CL, Tmax, t1/2, Vss) across dosing regimens (1Q3W, 3Q4W). Secondary outcomes include ADA development and efficacy metrics (OR per RECIST v1.1, CA-125 response, DoR, PFS, OS, AXL expression changes) in solid tumor patients.

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 24 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	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					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 6%	Positive AXL expression (AXL+++/++)
Method Description	Antitumor activity of EnaV in Nonresponder.
In Vivo Model	NSCLC PDX model
Experiment 3 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 13.30%	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.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 4 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 16.50%	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU0858; EGFR L858R mutation)
Experiment 5 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 16.50%	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU2511; EGFR mutation)
Experiment 6 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	29.60%	Positive AXL expression (AXL+++/++)
Method Description	EnaV=2 mg/kg.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU0395)
Experiment 7 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	46.90%	Positive AXL expression (AXL+++/++)
Method Description	EnaV=4 mg/kg.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU0395)
Experiment 8 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50%	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LCx-MR007; Osimertinib resistant)
Experiment 9 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50%	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					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50%	Positive AXL expression (AXL+++/++)
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFA677; EGFR mutation)
Experiment 11 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.40%	Positive AXL expression (AXL+++/++)
Method Description	Antitumor activity of EnaV in intermediate.
In Vivo Model	NSCLC PDX model
Experiment 12 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	60%	Moderate AXL expression (AXL++; IHC H-score=121)
Method Description	EnaV=4 mg/kg.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU2511)
Experiment 13 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.50%	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					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67%	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					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72.70%	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.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFA526)
Experiment 16 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.10%	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.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 17 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.80%	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.
In Vivo Model	Cervical cancer PDX model (PDX: CV1664)
Experiment 18 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.40%	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.
In Vivo Model	Cervical cancer PDX model (PDX: CV1664)
Experiment 19 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.30%	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.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 20 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.30%	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.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 21 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.80%	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.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LXFA526)
Experiment 22 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	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					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive AXL expression (AXL+++/++)
Method Description	Antitumor activity of EnaV in responder.
In Vivo Model	NSCLC PDX model
Experiment 24 Reporting the Activity Date of This ADC					[4]
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.
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

Click To Hide/Show 13 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 1%	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells.
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					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 17.70%	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells + Ctrl ADC.
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					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	34.30%	Positive AXL expression (AXL+++/++)
Method Description	EnaV=2 mg/kg.
In Vivo Model	LU2511 in NSCLC CDX model
Experiment 4 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	40.90%	Positive AXL expression (AXL+++/++)
Method Description	EnaV=0.5 mg/kg.
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					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 43.40%	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells.
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					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64%	Positive AXL expression (AXL+++/++)
Method Description	Treated with Ctrl T cells + EnaV.
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					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.70%	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells.
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					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.50%	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					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.50%	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.
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					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.20%	Positive AXL expression (AXL+++/++)
Method Description	Treated with MART-1 T cells + EnaV.
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					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.70%	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.
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					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.60%	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.
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					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	96.80%	Positive AXL expression (AXL+++/++)
Method Description	EnaV=1 mg/kg.
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

Click To Hide/Show 28 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 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.
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 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.
In Vitro Model	Lung adenocarcinoma	PC-9 cells		CVCL_B260
Experiment 3 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 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.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[6]
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.
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608
Experiment 5 Reporting the Activity Date of This ADC					[6]
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.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 6 Reporting the Activity Date of This ADC					[6]
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.
In Vitro Model	Lung large cell carcinoma	NCI-H460 cells		CVCL_0459
Experiment 7 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.5 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.
In Vitro Model	Melanoma	A-875 cells		CVCL_4733
Experiment 8 Reporting the Activity Date of This ADC					[4]
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.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells (BRAF inhibitor resistant)		CVCL_0526
Experiment 9 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.7 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.
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 10 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.3 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.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 11 Reporting the Activity Date of This ADC					[4]
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.
In Vitro Model	Melanoma	SK-MEL-147 cells		CVCL_3876
Experiment 12 Reporting the Activity Date of This ADC					[4]
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.
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608
Experiment 13 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	189.3 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.
In Vitro Model	Melanoma	SK-MEL-2 cells (MEK inhibitor-resistant)		CVCL_0069
Experiment 14 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	190.9 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.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 15 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	370.4 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.
In Vitro Model	Amelanotic melanoma	A375/R cells		CVCL_IW10
Experiment 16 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	887.2 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.
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					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1828.3 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.
In Vitro Model	Lung large cell carcinoma	NCI-H1299 cells		CVCL_0060
Experiment 18 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2090.3 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.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 19 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2895.7 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.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 20 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6881 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.
In Vitro Model	Lung large cell carcinoma	NCI-H661 cells		CVCL_1577
Experiment 21 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 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 22 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 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 23 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 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 24 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 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					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 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 26 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 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 27 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 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 28 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 .	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.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

References

Ref 1	Enapotamab Vedotin (HuMax-AXL-ADC) Safety Study in Patients With Solid Tumors
Ref 2	Enapotamab vedotin, an AXL-specific antibody-drug conjugate, shows preclinical antitumor activity in non-small cell lung cancer. JCI Insight. 2019 Nov 1;4(21):e128199.
Ref 3	Preclinical Development of ADCT-601, a Novel Pyrrolobenzodiazepine Dimer-based Antibody-drug Conjugate Targeting AXL-expressing Cancers. Mol Cancer Ther. 2022 Apr 1;21(4):582-593.
Ref 4	Cooperative targeting of melanoma heterogeneity with an AXL antibody-drug conjugate and BRAF/MEK inhibitors. Nat Med. 2018 Feb;24(2):203-212.
Ref 5	Cooperative Targeting of Immunotherapy-Resistant Melanoma and Lung Cancer by an AXL-Targeting Antibody-Drug Conjugate and Immune Checkpoint Blockade. Cancer Res. 2021 Apr 1;81(7):1775-1787.
Ref 6	AXL antibody and AXL-ADC mediate antitumor efficacy via targeting AXL in tumor-intrinsic epithelial-mesenchymal transition and tumor-associated M2-like macrophage. Acta Pharmacol Sin. 2023 Jun;44(6):1290-1303. doi: 10.1038/s41401-022-01047-6. Epub 2023 Jan 17.

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Correspondence

Prof. Feng ZHU (zhufeng@zju.edu.cn)

Prof. Xiaowu DONG (dongxw@zju.edu.cn)

Prof. Luo FANG (fangluo@zjcc.org.cn)