DC0-NH2

DC0-NH2 is an effector moiety for ADC and a simplified analog of DC1 with better stability. DC0-NH2 is about 1000-fold more cytotoxic than commonly used anticancer drugs (ex. Doxorubicin). DC0-NH2 can bind to the minor groove of DNA, followed by alkylation of adenine residues by its propabenzindole (CBI) component.

Product information

CAS Number: 615538-51-7

Molecular Weight: 550.01

Formula: C31H24ClN5O3

Chemical Name: 5-amino-N-{2-[(1S)-1-(chloromethyl)-5-hydroxy-1H, 2H, 3H-benzo[e]indole-3-carbonyl]-1H-indol-5-yl}-1H-indole-2-carboxamide

Smiles: NC1C=C2C=C(NC2=CC=1)C(=O)NC1C=C2C=C(NC2=CC=1)C(=O)N1C[C@@H](CCl)C2C3=CC=CC=C3C(O)=CC1=2

InChiKey: PANFWPQOVGEWSD-GOSISDBHSA-N

InChi: InChI=1S/C31H24ClN5O3/c32-14-18-15-37(27-13-28(38)21-3-1-2-4-22(21)29(18)27)31(40)26-12-17-10-20(6-8-24(17)36-26)34-30(39)25-11-16-9-19(33)5-7-23(16)35-25/h1-13,18,35-36,38H,14-15,33H2,(H,34,39)/t18-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

DC0-NH2 (0-3 nM; 72 hours), in the vitality test of breast cancer cell lines, has a high anti-proliferative effect on Ramos, Namalwa and HL60 / s cells, inhibits the proliferation of Namalwa and HL60 / s cells The IC50 values were 7 pM and 5 pM, respectively, and the inhibition range of COLO205 cells was within 100 pM.

References:

1. Zhao RY, et al. Synthesis and biological evaluation of antibody conjugates of phosphate prodrugs of cytotoxic DNA alkylators for the targeted treatment of cancer.J Med Chem. 2012 Jan 26;55(2):766-82.

Products are for research use only. Not for human use.