Antibody ID	ANI0TYNXL
Antibody Name	XMT-1535
Synonyms	Rebmab200; Upifitamab    Click to Show/Hide
Antibody Type	Monoclonal antibody (mAb)
Antibody Subtype	Humanized IgG1-kappa
Antigen Name	Sodium-dependent phosphate transport protein 2B (SLC34A2)					Antigen Info
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence	QVQLVQSGAEVVKPGASVKMSCKASGYTFTGYNIHWVKQAPGQGLEWIGAIYPGNGDTSY KQKFRGRATLTADTSTSTVYMELSSLRSEDSAVYYCARGETARATFAYWGQGTLVTVSSG ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSCDKTHTCPPCPAPELLGG PSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYN STYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREE MTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRW QQGNVFSCSVMHEALHNHYTQKSLSLSPG     Click to Show/Hide
Light Chain Sequence	DIQMTQSPSSLSASVGDRVTITCSASQDIGNFLNWYQQKPGKTVKVLIYYTSSLYSGVPS RFSGSGSGTDYTLTISSLQPEDFATYYCQQYSKLPLTFGQGTKLELKRRTVAAPSVFIFP PSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTL TLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC     Click to Show/Hide

Antibody Activity Information 1						[1]
Dissociation Constant (Kd)	0.73±0.34	nM
Antibody Function	Confirm the effect of the drug conjugation with the anti-NaPi2b Ab and ADC on binding activity to target.
Antibody Antigen Binding Assay	The optical density (OD) was measured at 450 nm with a SpectraMax M5 microplate reader. The Kd was calculated with GraphPad Prism software by nonlinear regression using the one site-specific binding model.XMT-1536 and the unconjugated antibody XMT-1535 bound to a peptide corresponding to the epitope of human NaPi2b.
Antibody Activity Information 2						[1]
Dissociation Constant (Kd)	4.05±2.62	nM	OVCAR-3 cells		CVCL_0465
Antigen Expression	Positive SLC34A2 expression (SLC34A2+++/++)
Antibody Function	Confirm the effect of the drug conjugation with the anti-NaPi2b Ab and ADC on binding activity to target.
Antibody Antigen Binding Assay	The median fluorescence value for each treatment was determined from 5,000 cells quantified on a MACSQuant flow cytometer. The Kd was calculated with GraphPad Prism software by nonlinear regression using the one site-specific binding model. Both XMT-1536 and the unconjugated XMT-1535 antibody bound to the NaPi2b-expressing OVCAR3 ovarian cancer cell line (~66000 NaPi2b antigens per cell) with nanomolar affinity.

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Objective Response Rate (ORR)	34.00% (all) 35.00% (SLC34A2 high) 29.00% (SLC34A2 low)	High SLC34A2 expression (SLC34A2+++; 66,000 SLC34A2 antigens/cell)
Patients Enrolled	Ovarian cancer patients with 1-3 prior lines in platinum-resistant; 4 prior lines patients regardless of platinum status.
Administration Dosage	36 or 43 mg/m 2 IV once every 4 weeks.
Related Clinical Trial
NCT Number	NCT03319628	Clinical Status	Phase 1/2
Clinical Description	Open-label, dose escalation to reach mtd. the mtd will be confirmed in parallel cohorts: patients with platinum-resistant ovarian cancer; patients with non-squamous nsclc, adenocarcinoma subtype.
Experiment 2 Reporting the Activity Date of This ADC					[3]
Related Clinical Trial
NCT Number	NCT05329545	Clinical Status	Phase 3
Clinical Description	A phase 3, randomized, double-blind, placebo-controlled, multicenter study of upifitamab rilsodotin (XMT-1536) as post-platinum maintenance therapy for participants with recurrent, platinum-sensitive, ovarian cancer (up-next).
Experiment 3 Reporting the Activity Date of This ADC					[4]
Patients Enrolled	Patients with a histological diagnosis of metastatic or recurrent high-grade serous ovarian cancer, including fallopian tube, or primary peritoneal cancer and have received 1-3 prior lines of therapy.
Related Clinical Trial
NCT Number	NCT04907968	Clinical Status	Phase 1
Clinical Description	Upifitamab rilsodotin (XMT-1536) an open-label, multicenter, dose escalation and expansion study of upifitamab rilsodotin in combination with carboplatin in participants with high grade serous ovarian cancer (UP GRADE-A).

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 58.60% (Day 35)	Moderate SLC34A2 expression (SLC34A2++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0178)
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 60.60% (Day 28)	Moderate SLC34A2 expression (SLC34A2++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0178)
Experiment 3 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.40% (Day 17)	Moderate SLC34A2 expression (SLC34A2++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Non-small cell lung cancer PDX model (PDX: CTG-0860)
Experiment 4 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.10% (Day 28)	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0852)
Experiment 5 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.40% (Day 35)	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0852)
Experiment 6 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.70% (Day 62)	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg qwk x 3.    Click to Show/Hide
In Vivo Model	Lung cancer PDX model (PDX: CTG-0852)

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.00% (Day 28)	High SLC34A2 expression (SLC34A2+++)
Method Description	Animals were randomized into treatment groups (n = 10) when the tumor target volume reached 100-150 mm3. Test articles were administered intravenously via tail vein injection. Mice received a single dose of either saline vehicle; XMT-1535 at 3 mg/kg; XMT-1536 (DAR 12.4) at 3 mg/kg; IgG1-Dolaflexin (DAR 18.1) at 3 mg/kg,or lifastuzumab vedotin (DAR 4.1) at 3 mg/kg. Tumors were measured twice per week. XMT-1536 and lifastuzumab vedotin were administered at a single dose of 3 mg/kg.    Click to Show/Hide
In Vivo Model	Ovarian adenocarcinoma CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.52 nM
Method Description	OVCAR3 cells were grown in RPMI1640 media supplemented with 20% FBS and 1% penicillin/streptomycin,seeded at a density of 5, 000 cells per well in 100 L of growth media in a 96-well,white flat-bottom plate. Following overnight incubation,the media was replaced with 100 L of fresh media containing the test compounds at a 3-fold titration up to 33 nmol/L. The treated cells were incubated for 96 hours at 37°C in the presence of 5% CO2. In the OVCAR3 cell line,XMT-1536 was cytotoxic in a 96-hour cellular cytotoxicity assay.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 42.53% (Day 30)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (1.5 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.72% (Day 43)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (3 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.70% (Day 32)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (3 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 51.69% (Day 30)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (1.5 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.84% (Day 30)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (3 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 54.09% (Day 30)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (1.5 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.71% (Day 32)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (3 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.72% (Day 43)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (3 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.51% (Day 43)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (3.72 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.12% (Day 32)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (3 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.64% (Day 43)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (3 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.71% (Day 32)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (3 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.03% (Day 32)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (3 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.03% (Day 32)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (3 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.45% (Day 32)	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (3 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.00 pM	Positive SLC34A2 expression (SLC34A2+++/++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive SLC34A2 expression (SLC34A2+++/++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Ovarian clear cell adenocarcinoma	TOV-21G cells		CVCL_3613
Experiment 3 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive SLC34A2 expression (SLC34A2+++/++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC4006 cells		CVCL_1269
Experiment 4 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 nM	Positive SLC34A2 expression (SLC34A2+++/++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.69 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive SLC34A2 expression (SLC34A2+++/++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	Positive SLC34A2 expression (SLC34A2+++/++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC4006 cells		CVCL_1269
Experiment 3 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Positive SLC34A2 expression (SLC34A2+++/++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304
Experiment 4 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.68 nM	Positive SLC34A2 expression (SLC34A2+++/++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Ovarian clear cell adenocarcinoma	TOV-21G cells		CVCL_3613

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Ref 1	Targeting Multiple EGFR-expressing Tumors with a Highly Potent Tumor-selective Antibody-Drug Conjugate. Mol Cancer Ther. 2020 Oct;19(10):2117-2125.
Ref 2	Safety and efficacy of XMT-1536 in ovarian cancer: A subgroup analysis from the phase I expansion study of XMT-1536, a NaPi2b antibody-drug conjugate. Ann. Oncol. 2020 Sept; 31(4):Supplement S627-S628.
Ref 3	A Phase 3, Randomized, Double-blind, Placebo-controlled, Multicenter Study of Upifitamab Rilsodotin (XMT-1536) as Post-Platinum Maintenance Therapy for Participants With Recurrent, Platinum-Sensitive, Ovarian Cancer (UP-NEXT), NCT05329545
Ref 4	Upifitamab Rilsodotin (Xmt-1536) An Open-Label, Multicenter, Dose Escalation And Expansion Study Of Upifitamab Rilsodotin In Combination With Carboplatin In Participants With High Grade Serous Ovarian Cancer (Upgrade-A), NCT04907968
Ref 5	The Dolaflexin-based Antibody-Drug Conjugate XMT-1536 Targets the Solid Tumor Lineage Antigen SLC34A2/NaPi2b. Mol Cancer Ther. 2021 May;20(5):896-905.
Ref 6	Peptide-containing linkers for antibody-drug conjugates.
Ref 7	NaPi2b targeting antibody-drug conjugates and methods of use thereof.