Payload Information

General Information of This Payload

Payload ID	PAY0VDATG
Name	SG2000
Synonyms	SJG-136; 232931-57-6; SJG 136; NSC-694501; SG-2000; BN-2629; UNII-KT0ZQ64X1A; NSC 694501; UP 2001; KT0ZQ64X1A; SJG136; (6aS)-3-[3-[[(6aS)-2-methoxy-8-methylidene-11-oxo-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]propoxy]-2-methoxy-8-methylidene-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-11-one; SP-2001; UP-2001; 5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one, 8,8'-[1,3-propanediylbis(oxy)]bis[1,2,3,11a-tetrahydro-7-methoxy-2-methylene-, (11aS,11'aS)-; 5H-PYRROLO(2,1-C)(1,4)BENZODIAZEPIN-5-ONE, 8,8'-(1,3-PROPANEDIYLBIS(OXY))BIS(1,2,3,11A-TETRAHYDRO-7-METHOXY-2-METHYLENE-, (11AS,11'AS)-; NSC694501; CHEMBL16498; SCHEMBL12020905; SJG 136 [WHO-DD]; DTXSID20177864; CS-4593; DB11965; BS-42683; HY-14573; NCI60_033825; C74198; A858346; Q27282424; (11AS,11a'S)-8,8'-(propane-1,3-diylbis(oxy))bis(7-methoxy-2-methylene-1,2,3,11a-tetrahydro-5H-benzo[e]pyrrolo[1,2-a][1,4]diazepin-5-one); (11aS,11a'S)-8,8'-(propane-1,3-diylbis(oxy))bis(7-methoxy-2-methylene-1,2,3,11a-tetrahydro-5H-benzo[e]pyrrolo[1,2-a][1,4]diazepin-5-one);1,1'-(propane-1,3-diylbis(oxy))bis(7-methoxy-2-methylene-1,2,3,11a-tetrahydro-5H-benzo[e]pyrrolo[1,2-a][1,4]diazepine-5,11(10H)-dione); (6AS)-3-(3-(((6AS)-2-METHOXY-8-METHYLENE-11-OXO-7,9-DIHYDRO-6AH-PYRROLO(2,1-C)(1,4)BENZODIAZEPIN-3-YL)OXY)PROPOXY)-2-METHOXY-8-METHYLENE-7,9-DIHYDRO-6AH-PYRROLO(2,1-C)(1,4)BENZODIAZEPIN-11-ONE; 1,1'-((Propane-1,3-diyl)dioxy)bis(7-methoxy-2-methylidene-1,2,3,10,11,11a-hexahydro-5H-pyrrolo(2,1-c)(1,4)benzodiazepin-5,11-dione); 5H-Pyrrolo[2,4]benzodiazepin-5-one, 8,8'-[1,3-propanediylbis(oxy)]bis[1,2,3,11a-tetrahydro- 7-methoxy-2-methylene-, (11aS, 11'aS)- Click to Show/Hide
Target(s)	Human Deoxyribonucleic acid (hDNA)			Target Info
Structure
Structure	3D MOL		2D MOL
Formula	C31H32N4O6
Isosmiles	COC1=C(C=C2C(=C1)C(=O)N3CC(=C)C[C@H]3C=N2)OCCCOC4=C(C=C5C(=C4)N=C[C@@H]6CC(=C)CN6C5=O)OC
PubChem CID	393111
InChI	InChI=1S/C31H32N4O6/c1-18-8-20-14-32-24-12-28(26(38-3)10-22(24)30(36)34(20)16-18)40-6-5-7-41-29-13-25-23(11-27(29)39-4)31(37)35-17-19(2)9-21(35)15-33-25/h10-15,20-21H,1-2,5-9,16-17H2,3-4H3/t20-,21-/m0/s1
InChIKey	RWZVMMQNDHPRQD-SFTDATJTSA-N
IUPAC Name	(6aS)-3-[3-[[(6aS)-2-methoxy-8-methylidene-11-oxo-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]propoxy]-2-methoxy-8-methylidene-7,9-dihydro-6aH-pyrrolo[2,1-c][1,4]benzodiazepin-11-one
Pharmaceutical Properties	Molecule Weight	556.6	Polar area	102
	Complexity	1020	xlogp Value	1.9
	Heavy Count	41	Rot Bonds	8
	Hbond acc	8	Hbond Donor	0

The activity data of This Payload

Standard Type	Value	Units	Cell line	Disease Model	Cell line ID	Reference
Half Maximal Inhibitory Concentration (IC50)	0.0225	nM	A2780 cells	Ovarian endometrioid adenocarcinoma	CVCL_0134	[1]
Half Maximal Inhibitory Concentration (IC50)	0.0225	nM	A2780 cells	Ovarian endometrioid adenocarcinoma	CVCL_0134	[2]
Half Maximal Inhibitory Concentration (IC50)	0.024	nM	A2780 cells	Ovarian endometrioid adenocarcinoma	CVCL_0134	[1]
Half Maximal Inhibitory Concentration (IC50)	0.12	nM	CH1 cells	Ovarian carcinoma	CVCL_4992	[2]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	0.1361	nM	MOLT-4 cells	Adult T acute lymphoblastic leukemia	CVCL_0013	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	0.8318	nM	SF268 cells	Astrocytoma	CVCL_1689	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	1.4	nM	NCI-H522 cells	Non-small cell lung carcinoma	CVCL_1567	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	1.66	nM	NCI-H23 cells	Lung adenocarcinoma	CVCL_1547	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	HL-60 cells	Adult acute myeloid leukemia	CVCL_0002	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	SN12C cells	Renal cell carcinoma	CVCL_1705	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	K-562 cells	Chronic myelogenous leukemia	CVCL_0004	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	U-251MG cells	Astrocytoma	CVCL_0021	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	CCRF-CEM cells	T acute lymphoblastic leukemia	CVCL_0207	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	COLO 205 cells	Colon adenocarcinoma	CVCL_0218	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	Caki-1 cells	Clear cell renal cell carcinoma	CVCL_0234	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	NCI-H460 cells	Lung large cell carcinoma	CVCL_0459	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	SK-MEL-5 cells	Cutaneous melanoma	CVCL_0527	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	SNB-19 cells	Astrocytoma	CVCL_0535	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	T-47D cells	Invasive breast carcinoma	CVCL_0553	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	786-O cells	Renal cell carcinoma	CVCL_1051	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	IGROV-1 cells	Ovarian endometrioid adenocarcinoma	CVCL_1304	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	SF539 cells	Gliosarcoma	CVCL_1691	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	SNB-75 cells	Glioblastoma	CVCL_1706	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	ACHN cells	Renal adenocarcinoma	CVCL_1067	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	LOX IMVI cells	Melanoma	CVCL_1381	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	SF-295 cells	Glioblastoma	CVCL_1690	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	SR cells	Leukemia	CVCL_1711	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10	nM	UACC-62 cells	Melanoma	CVCL_1780	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10.33	nM	HCT 116 cells	Colon carcinoma	CVCL_0291	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10.64	nM	HOP-62 cells	Non-small cell lung carcinoma	CVCL_1285	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10.67	nM	RXF 393 cells	Renal carcinoma	CVCL_1673	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10.76	nM	MDA-MB-231 cells (5T4 overexpression)	Breast adenocarcinoma	CVCL_0062	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	10.91	nM	Malme-3M cells	Melanoma	CVCL_1438	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	11.12	nM	BT-549 cells	Breast ductal carcinoma	CVCL_1092	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	11.86	nM	OVCAR-8 cells	High grade ovarian serous adenocarcinoma	CVCL_1629	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	12.02	nM	MCF7-F (fulvestrant resistant) cells	Invasive breast carcinoma	CVCL_0031	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	12.11	nM	RPMI-8226 cells	Plasma cell myeloma	CVCL_0014	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	12.25	nM	NCI-H226 cells	Pleural epithelioid mesothelioma	CVCL_1544	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	12.3	nM	SW620 cells	Colon adenocarcinoma	CVCL_0547	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	12.39	nM	KM12 cells	Colon adenocarcinoma	CVCL_1331	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	12.56	nM	HCC 2998 cells	Colon adenocarcinoma	CVCL_1266	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	123.59	nM	HCT 15 cells	Colon adenocarcinoma	CVCL_0292	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	14.06	nM	SK-MEL-28 cells (BRAF inhibitor resistant)	Cutaneous melanoma	CVCL_0526	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	14.29	nM	MDA-N cells	Breast carcinoma	CVCL_1910	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	14.55	nM	SK-MEL-2 cells (MEK inhibitor-resistant)	Melanoma	CVCL_0069	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	14.62	nM	A498 cells	Renal carcinoma	CVCL_1056	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	14.62	nM	UACC-257 cells	Melanoma	CVCL_1779	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	14.69	nM	HT-29 cells	Colon adenocarcinoma	CVCL_0320	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	15.7	nM	A-549 cells	Lung adenocarcinoma	CVCL_0023	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	16.9	nM	M14 cells	Melanoma	CVCL_1395	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	17.18	nM	OVCAR-3 cells (FZD7 overexpression)	Ovarian serous adenocarcinoma	CVCL_0465	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	17.74	nM	DU145 cells	Prostate carcinoma	CVCL_0105	[3]
Half Maximal Inhibitory Concentration (IC50)	170	nM	CHO cells	Normal	CVCL_0213	[4]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	18.07	nM	MDA-MB-435 cells	Amelanotic melanoma	CVCL_0417	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	19.05	nM	PC-3 cells	Prostate carcinoma	CVCL_0035	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	20.84	nM	UO-31 cells	Renal carcinoma	CVCL_1911	[3]
Half Maximal Inhibitory Concentration (IC50)	200	nM	OE33 cells	Barrett adenocarcinoma	CVCL_0471	[5]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	21.58	nM	SK-OV-3 cells (FZD7 overexpression)	Ovarian serous cystadenocarcinoma	CVCL_0532	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	29.31	nM	OVCAR-5 cells	Ovarian serous adenocarcinoma	CVCL_1628	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	29.92	nM	NCI-H322M cells	Minimally invasive lung adenocarcinoma	CVCL_1557	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	30.55	nM	OVCAR-4 cells	Ovarian adenocarcinoma	CVCL_1627	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	31.62	nM	TK-10 cells	Renal carcinoma	CVCL_1773	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	32.73	nM	EKVX cells	Non-small cell lung carcinoma	CVCL_1195	[3]
Half Maximal Inhibitory Concentration (IC50)	42.5	nM	K-562 cells	Chronic myelogenous leukemia	CVCL_0004	[2]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	42.56	nM	Hs 578T cells	Invasive breast carcinoma	CVCL_0332	[3]
Half Maximal Inhibitory Concentration (IC50)	43	nM	K-562 cells	Chronic myelogenous leukemia	CVCL_0004	[6]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	6.823	nM	HOP-92 cells	Non-small cell lung carcinoma	CVCL_1286	[3]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	8	nM	K-562 cells	Chronic myelogenous leukemia	CVCL_0004	[7]
Half Maximal Cell Growth Inhibitory Concentration (GI50)	83.37	nM	NCI-ADR-RES cells	High grade ovarian serous adenocarcinoma	CVCL_1452	[3]
Half Maximal Inhibitory Concentration (IC50)	9.1	nM	SK-OV-3 cells (FZD7 overexpression)	Ovarian serous cystadenocarcinoma	CVCL_0532	[2]

Each Antibody-drug Conjugate Related to This Payload

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

WO2021044208A1 ADC6 [Investigative]

ADC Info

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					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0.00% (Day 41)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 10⁷ cells/head of human ROR-1 expressing breast cancer cell line HCC1187 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 110 mm³ on average (Day 1), and 1.25 mg/kg of ADC5.
In Vivo Model	HCC1187 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1187 cells		CVCL_1247
Experiment 2 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.74% (Day 26)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 10⁷ cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm³ on average (Day 1), and 1 mg/kg QDx1 of ADC5.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 3 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.97% (Day 19)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 10⁷ cells/head of human ROR-1 expressing breast cancer cell line MDA-MB231 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 110 mm³ on average (Day 1), and 0.33 mg/kg ADC5 was intravenously injected twice weekly a total of three times (Days 1, 7 and 14). Click to Show/Hide
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.51% (Day 19)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 10⁷ cells/head of human ROR-1 expressing breast cancer cell line MDA-MB231 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 110 mm³ on average (Day 1), and 0.5 mg/kg of ADC5.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 5 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.90% (Day 19)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 10⁷ cells/head of human ROR-1 expressing breast cancer cell line MDA-MB231 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 110 mm³ on average (Day 1), and 1 mg/kg of ADC5.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 6 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.95% (Day 35)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 10⁷ cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 184mm³ on average (Day 1), and 1 mg/kg QDx1 of ADC5.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 7 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.09% (Day 33)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 10⁷ cells/head of human ROR-1 expressing mantle cell lymphoma cell line JeKo-1 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 184mm³ on average (Day 1), and 0.25 mg/kg QWx4 of ADC5.
In Vivo Model	JeKo-1 CDX model
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 8 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.16% (Day 41)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 10⁷ cells/head of human ROR-1 expressing breast cancer cell line HCC1187 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 110 mm³ on average (Day 1), and 3.75 mg/kg QWx4 of ADC2.
In Vivo Model	HCC1187 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1187 cells		CVCL_1247
Experiment 9 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.98% (Day 19)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 10⁷ cells/head of human ROR-1 expressing breast cancer cell line MDA-MB231 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 110 mm³ on average (Day 1), and 2 mg/kg of ADC5.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 10 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.97% (Day 35)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 10⁷ cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 184mm³ on average (Day 1), and 0.25 mg/kg QWx4 of ADC5.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 11 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.79% (Day 56)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 10⁷ cells/head of human ROR-1 expressing breast cancer cell line MDA-MB-468 were grafted to female Balb/C nude mice to prepare human cancer grafted mice. After grafting.the mice were grouped when tumor size reached 166mm³ on average (Day 1), and 1 mg/kg of ADC5 was intravenously injected into the mice. In the control group, 10ml/kg PBS was intravenously injected into the mice. Click to Show/Hide
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 12 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.97% (Day 26)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 10⁷ cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm³ on average (Day 1), and 4 mg/kg of ADC5.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 13 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 33)	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 10⁷ cells/head of human ROR-1 expressing mantle cell lymphoma cell line JeKo-1 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 184mm³ on average (Day 1), and 1 mg/kg QDx1 of ADC5.
In Vivo Model	JeKo-1 CDX model
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865

Revealed Based on the Cell Line Data

Click To Hide/Show 5 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.09 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 2 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543
Experiment 3 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	243 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 5 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	247 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865

OHPAS ADC-2 [Investigative]

ADC Info

Discovered Using Cell Line-derived Xenograft Model

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

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 37.00% (Day 78)	High HER2 expression (HER2 +++)
Method Description	We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (0.5 mg/kg) on day one (initial tumor volume 100 mm³).
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.60% (Day 78)	High HER2 expression (HER2 +++)
Method Description	We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (2 mg/kg) on day one (initial tumor volume 100 mm³).
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Revealed Based on the Cell Line Data

Click To Hide/Show 5 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Moderate HER2 expression (HER2 ++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50.00 nM	Negative HER2 expression (HER2 -)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

HER2-HC-Me-SS-PBD [Investigative]

ADC Info

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.00% (Day 24)	High HER2 expression (HER2+++)
Method Description	All animals were euthanized before tumors reached 3000 mm³ or showed signs of impending ulceration. Mice were dosed IV via the tail vein with ADC conjugates A1-A4. A1 and A2 were dosed at 4 mg/kg.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus

Anti-CLL-1-ds-PBD [Investigative]

ADC Info

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 9 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 47.85% (Day 11)	Positive CLL-1 expression (CLL-1+++/++)
Method Description	Three human AML cell lines, were used to establish subcutaneous xenograft models for evaluation of anti-CLL-1-ds-PBD efficacy. When mean tumor size reached the desired volume (200 mm³), animals were randomized into groups of n = 8, each with similar mean tumor size. Four hours later, animals in each group were given a single intravenous dose of vehicle or ADC (0.25 mg/kg) through the tail vein. Click to Show/Hide
In Vivo Model	HL-60 CDX model
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 2 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 57.73% (Day 14)	Moderate CLL-1 expression (CLL-1++)
Method Description	Three human AML cell lines, were used to establish subcutaneous xenograft models for evaluation of anti-CLL-1-ds-PBD efficacy. When mean tumor size reached the desired volume (200 mm³), animals were randomized into groups of n = 8, each with similar mean tumor size. Four hours later, animals in each group were given a single intravenous dose of vehicle or ADC (0.75 mg/kg) through the tail vein. Click to Show/Hide
In Vivo Model	THP1 CDX model
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006
Experiment 3 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72.19% (Day 14)	Moderate CLL-1 expression (CLL-1++)
Method Description	Three human AML cell lines, were used to establish subcutaneous xenograft models for evaluation of anti-CLL-1-ds-PBD efficacy. When mean tumor size reached the desired volume (200 mm³), animals were randomized into groups of n = 8, each with similar mean tumor size. Four hours later, animals in each group were given a single intravenous dose of vehicle or ADC (1.5 mg/kg) through the tail vein. Click to Show/Hide
In Vivo Model	THP1 CDX model
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006
Experiment 4 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.28% (Day 11)	Positive CLL-1 expression (CLL-1+++/++)
Method Description	Three human AML cell lines, were used to establish subcutaneous xenograft models for evaluation of anti-CLL-1-ds-PBD efficacy. When mean tumor size reached the desired volume (200 mm³), animals were randomized into groups of n = 8, each with similar mean tumor size. Four hours later, animals in each group were given a single intravenous dose of vehicle or ADC (0.5 mg/kg) through the tail vein. Click to Show/Hide
In Vivo Model	HL-60 CDX model
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 5 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.38% (Day 7)	Positive CLL-1 expression (CLL-1+++/++)
Method Description	Three human AML cell lines, were used to establish subcutaneous xenograft models for evaluation of anti-CLL-1-ds-PBD efficacy. When mean tumor size reached the desired volume (200 mm³), animals were randomized into groups of n = 8, each with similar mean tumor size. Four hours later, animals in each group were given a single intravenous dose of vehicle or ADC (0.25 mg/kg) through the tail vein. Click to Show/Hide
In Vivo Model	EOL-1 CDX model
In Vitro Model	Chronic eosinophilic leukemia	EoL-1 cells		CVCL_0258
Experiment 6 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.48% (Day 14)	Moderate CLL-1 expression (CLL-1++)
Method Description	Three human AML cell lines, were used to establish subcutaneous xenograft models for evaluation of anti-CLL-1-ds-PBD efficacy. When mean tumor size reached the desired volume (200 mm³), animals were randomized into groups of n = 8, each with similar mean tumor size. Four hours later, animals in each group were given a single intravenous dose of vehicle or ADC (3 mg/kg) through the tail vein. Click to Show/Hide
In Vivo Model	THP1 CDX model
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006
Experiment 7 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.88% (Day 7)	Positive CLL-1 expression (CLL-1+++/++)
Method Description	Three human AML cell lines, were used to establish subcutaneous xenograft models for evaluation of anti-CLL-1-ds-PBD efficacy. When mean tumor size reached the desired volume (200 mm³), animals were randomized into groups of n = 8, each with similar mean tumor size. Four hours later, animals in each group were given a single intravenous dose of vehicle or ADC (0.5 mg/kg) through the tail vein. Click to Show/Hide
In Vivo Model	EOL-1 CDX model
In Vitro Model	Chronic eosinophilic leukemia	EoL-1 cells		CVCL_0258
Experiment 8 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.23% (Day 7)	Positive CLL-1 expression (CLL-1+++/++)
Method Description	Three human AML cell lines, were used to establish subcutaneous xenograft models for evaluation of anti-CLL-1-ds-PBD efficacy. When mean tumor size reached the desired volume (200 mm³), animals were randomized into groups of n = 8, each with similar mean tumor size. Four hours later, animals in each group were given a single intravenous dose of vehicle or ADC (1 mg/kg) through the tail vein. Click to Show/Hide
In Vivo Model	EOL-1 CDX model
In Vitro Model	Chronic eosinophilic leukemia	EoL-1 cells		CVCL_0258
Experiment 9 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.90% (Day 11)	Positive CLL-1 expression (CLL-1+++/++)
Method Description	Three human AML cell lines, were used to establish subcutaneous xenograft models for evaluation of anti-CLL-1-ds-PBD efficacy. When mean tumor size reached the desired volume (200 mm³), animals were randomized into groups of n = 8, each with similar mean tumor size. Four hours later, animals in each group were given a single intravenous dose of vehicle or ADC (1 mg/kg) through the tail vein. Click to Show/Hide
In Vivo Model	HL-60 CDX model
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002

Revealed Based on the Cell Line Data

Click To Hide/Show 3 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 ng/mL±2.00 ng/mL	Positive CLL-1 expression (CLL-1+++/++)
Method Description	Tumor cells were then blocked with excess amount of mouse IgG2a anti-ragweed antibody and treated with ADCs for 6 days at 37°C before cell viability was measured.
In Vitro Model	Chronic eosinophilic leukemia	EoL-1 cells		CVCL_0258
Experiment 2 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.00 ng/mL±2.00 ng/mL	Positive CLL-1 expression (CLL-1+++/++)
Method Description	Tumor cells were then blocked with excess amount of mouse IgG2a anti-ragweed antibody and treated with ADCs for 6 days at 37°C before cell viability was measured.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 3 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	81.00 ng/mL±9.00 ng/mL	Moderate CLL-1 expression (CLL-1++)
Method Description	Tumor cells were then blocked with excess amount of mouse IgG2a anti-ragweed antibody and treated with ADCs for 6 days at 37°C before cell viability was measured.
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006

HER2-LC-H-SS-PBD [Investigative]

ADC Info

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.00% (Day 24)	High HER2 expression (HER2+++)
Method Description	All animals were euthanized before tumors reached 3000 mm³ or showed signs of impending ulceration. Mice were dosed IV via the tail vein with ADC conjugates A1-A4. A1 and A2 were dosed at 4 mg/kg.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus

HER2-HC-H-SS-PBD [Investigative]

ADC Info

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.00% (Day 24)	High HER2 expression (HER2+++)
Method Description	All animals were euthanized before tumors reached 3000 mm³ or showed signs of impending ulceration. Mice were dosed IV via the tail vein with ADC conjugates A1-A4. A1 and A2 were dosed at 4 mg/kg.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus

HER2-LC-Me-SS-PBD [Investigative]

ADC Info

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 24)	High HER2 expression (HER2+++)
Method Description	All animals were euthanized before tumors reached 3000 mm³ or showed signs of impending ulceration. Mice were dosed IV via the tail vein with ADC conjugates A1-A4. A1 and A2 were dosed at 4 mg/kg.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus

WO2013055987A1 Tmab-110 [Investigative]

ADC Info

Obtained from the Model Organism Data

Click To Hide/Show 3 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 5.82% (Day 14)	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 1 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 2 Reporting the Activity Date of This ADC				[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 31.56% (Day 14)	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 3 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 3 Reporting the Activity Date of This ADC				[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 47.90% (Day 14)	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 6 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5

Revealed Based on the Cell Line Data

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

Experiment 1 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	102.78 ug/mL	High HER2 expression (HER2 +++)
Method Description	Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 ug/mL	Negative HER2 expression (HER2 -)
Method Description	Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

WO2013055987A1 Tmab-101 [Investigative]

ADC Info

Obtained from the Model Organism Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.27% (Day 11)	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. When tumor sreached desired volumes, the tumor-bearing mice were randomized and given a single dose by IV 1 mg/kg injection of the ADC.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 2 Reporting the Activity Date of This ADC				[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.68% (Day 14)	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 1 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 3 Reporting the Activity Date of This ADC				[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.51% (Day 11)	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. When tumor sreached desired volumes, the tumor-bearing mice were randomized and given a single dose by IV 3 mg/kg injection of the ADC.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 4 Reporting the Activity Date of This ADC				[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.92% (Day 11)	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. When tumor sreached desired volumes, the tumor-bearing mice were randomized and given a single dose by IV 10 mg/kg injection of the ADC.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5

Revealed Based on the Cell Line Data

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

Experiment 1 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.12 ug/mL	High HER2 expression (HER2 +++)
Method Description	Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 ug/mL	Negative HER2 expression (HER2 -)
Method Description	Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

WO2013055987A1 xCD22-103 [Investigative]

ADC Info

Obtained from the Model Organism Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.10% (Day 11)	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. When tumor sreached desired volumes, the tumor-bearing mice were randomized and given a single dose by IV 10 mg/kg injection of the ADC.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5

References

Ref 1	Synthesis of the first example of a C2-C3/C2'-C3'-endo unsaturated pyrrolo[2,1-c][1,4]benzodiazepine dimer. Bioorg Med Chem Lett. 2001 Nov 5;11(21):2859-62. doi: 10.1016/s0960-894x(01)00560-1.
Ref 2	Design, synthesis, and evaluation of a novel pyrrolobenzodiazepine DNA-interactive agent with highly efficient cross-linking ability and potent cytotoxicity. J Med Chem. 2001 Mar 1;44(5):737-48. doi: 10.1021/jm001064n.
Ref 3	PubChem BioAssay data set.
Ref 4	Design, synthesis, biological evaluation, and structure-activity relationships of substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonates as new tubulin inhibitors mimicking combretastatin A-4. J Med Chem. 2011 Jul 14;54(13):4559-80. doi: 10.1021/jm200488a. Epub 2011 Jun 13.
Ref 5	3-substituted 7-phenyl-pyrroloquinolinones show potent cytotoxic activity in human cancer cell lines. J Med Chem. 2007 Nov 1;50(22):5509-13. doi: 10.1021/jm070534b. Epub 2007 Oct 4.
Ref 6	Linker length modulates DNA cross-linking reactivity and cytotoxic potency of C8/C8' ether-linked C2-exo-unsaturated pyrrolo[2,1-c][1,4]benzodiazepine (PBD) dimers. J Med Chem. 2004 Feb 26;47(5):1161-74. doi: 10.1021/jm030897l.
Ref 7	An asymmetric C8/C8'-tripyrrole-linked sequence-selective pyrrolo[2,1-c][1,4]benzodiazepine (PBD) dimer DNA interstrand cross-linking agent spanning 11 DNA base pairs. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2073-7. doi: 10.1016/j.bmcl.2008.01.096. Epub 2008 Jan 30.
Ref 8	Antibody-drug conjugate comprising antibody against human ror1, and use for the same; 2021-04-01.
Ref 9	Aryl Sulfate is a Useful Motif for Conjugating and Releasing Phenolic Molecules: Sulfur Fluorine Exchange Click Chemistry Enables Discovery of Ortho-Hydroxy-Protected Aryl Sulfate Linker. Bioconjug Chem. 2019 Jul 17;30(7):1957-1968. doi: 10.1021/acs.bioconjchem.9b00340. Epub 2019 Jun 28.
Ref 10	Intratumoral Payload Concentration Correlates with the Activity of Antibody-Drug Conjugates. Mol Cancer Ther. 2018 Mar;17(3):677-685. doi: 10.1158/1535-7163.MCT-17-0697. Epub 2018 Jan 18.
Ref 11	An Anti-CLL-1 Antibody-Drug Conjugate for the Treatment of Acute Myeloid Leukemia. Clin Cancer Res. 2019 Feb 15;25(4):1358-1368. doi: 10.1158/1078-0432.CCR-18-0333. Epub 2018 Jun 29.
Ref 12	Pyrrolobenzodiazepines and conjugates thereof; 2013-04-18.

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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)