bs-6980C

DATASHEET

Formulation Powder

Storage: Store in dry, dark place at -20C for 1 year.

Product Information:

Molecular Weight: 889.8

Formula: C48 H43 Cl2 F N6 O6

CAS Number: 2136247-12-4

InChi Key: ZLGNYFOIDAVMHY-MPKOGUQCSA-N

InChi: InChI=1S/C48H43Cl2FN6O6/c49-29-16-19-34-36(25-29)54-46(63)48(34)39(32-12-8-13-35(50)40(32)51)41(56-47(48)22-4-2-5-23-47)44(61)53-30-17-14-28(15-18-30)42(59)52-24-6-1-3-9-27-10-7-11-31-33(27)26-57(45(31)62)37-20-21-38(58)55-43(37)60/h7-8,10-19,25,37,39,41,56H,1-2,4-6,20-24,26H2,(H,52,59)(H,53,61)(H,54,63)(H,55,58,60)/t37?,39-,41+,48+/m0/s1

Smiles: O=C1NC2=CC(Cl)=CC=C2[C@]21[C@H]([C@@H](NC12CCCCC1)C(=O)NC1C=CC(=CC=1)C(=O)NCCCC#CC1C=CC=C2C=1CN(C1CCC(=O)NC1=O)C2=O)C1C=CC=C(Cl)C=1F

Purity: 98.0

Solubility: Soluble in DMSO

Appearance: Solid Power.

Shelf Life: 1.0 years

Description:

MD-224 is a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression. MD-224 effectively induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells. It achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells and also low nanomolar IC50 values in a panel of leukemia cell lines. MD-224 achieves complete and durable tumor regression in vivo in the RS4;11 xenograft tumor model in mice at well-tolerated dose schedules. MD-224 is thus a highly potent and efficacious MDM2 degrader and warrants extensive evaluations as a new class of anticancer agent.