Payload Information

General Information of This Payload

Payload ID	PAY0KPCRM
Name	DM1 derivative 16
Synonyms	DM1 derivative 16 Click to Show/Hide
Target(s)	Microtubule (MT)			Target Info
Formula	C35H49ClN4O10
Isosmiles	CNCCC(=O)N[C@H](C)C(=O)O[C@H]1CC(=O)N(C)c2cc(cc(OC)c2Cl)C/C(C)=C/C=C/[C@H](OC)[C@]2(O)C[C@H](OC(=O)N2)[C@H](C)[C@H]2O[C@]12C
InChI	InChI=1S/C35H49ClN4O10/c1-19-10-9-11-26(47-8)35(45)18-25(48-33(44)39-35)20(2)31-34(4,50-31)27(49-32(43)21(3)38-28(41)12-13-37-5)17-29(42)40(6)23-15-22(14-19)16-24(46-7)30(23)36/h9-11,15-16,20-21,25-27,31,37,45H,12-14,17-18H2,1-8H3,(H,38,41)(H,39,44)/b11-9-,19-10-/t20-,21+,25-,26-,27-,31+,34+,35+/m0/s1
Pharmaceutical Properties	Molecule Weight	721.248	Polar area	177.29
	Complexity	50	xlogp Value	2.7818
	Heavy Count	50	Rot Bonds	8
	Hbond acc	11	Hbond Donor	4

Each Antibody-drug Conjugate Related to This Payload

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

EGFRvIII-16 [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					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.00% (Day 25)	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	ADCs were dosed at 1 and 5 mg/kg in a single dose and once weekly for 3 weeks.
In Vivo Model	MMT CDX model
In Vitro Model	Malignant neoplasms of the mouse mammary gland	MMT-060562 cells		CVCL_4241

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					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.30 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Astrocytoma	U-251MG cells		CVCL_0021
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.30 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Malignant neoplasms of the mouse mammary gland	MMT-060562 cells		CVCL_4241
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Normal	HEK293 cells		CVCL_0045

PSMA-16 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.50 nM	Positive PSMA expression (PSMA+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782

PRLR-16 [Investigative]

ADC Info

Revealed Based on the Cell Line Data

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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00 nM	Positive PRLR expression (PRLR+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

References

Ref 1	Antibody drug conjugates of cleavable amino-alkyl and aryl maytansinoids. Bioorg Med Chem. 2018 May 15;26(9):2271-2279. doi: 10.1016/j.bmc.2018.02.025. Epub 2018 Feb 21.