EC-0225

EC-0225, a folate conjugate of two agents- one a potent microtubule inhibiting agent, and the second a DNA alkylating agent. EC-0225 inhibits the growth of folate receptor (FR) -positive KB cells with an IC50 of ~1 nM. EC-0225 can be selectively delivered to advanced FR-positive tumors without causing overt toxicity, such as lung carcinoma[1].

Product Specifications

CAS Number

[926626-77-9]

UNSPSC

12352005

Target

DNA Alkylator/Crosslinker; Folate Receptor (FR) ; Microtubule/Tubulin

Related Pathways

Cell Cycle/DNA Damage; Cytoskeleton

Field of Research

Cancer

Smiles

O[C@@]1(CC)C[C@]2([H])C[C@@](C3=C(OC)C=C4C([C@@]5(CC6)[C@@]([C@](C(NNC(OCCSSC[C@H](C(O)=O)CC([C@@H](NC([C@H](NC([C@H](CC(O)=O)NC([C@H](CC)NC(CC[C@@H](C)NC(C7=CC=C(NCC8=CNC(C9=N8)=NC(N)=CC9=O)C=C7)=O)=O)=O)=O)CC(O)=O)=O)CNC(CCSSCCNC%10=C(C)C(C%11=C(C[C@@]%12(OC)N%11C[C@H]%13[C@@H]%12N%13)C%10=O)=O)=O)=O)=O)=O)(O)[C@H](O)[C@@]%14(CC)[C@]5([H])N6CC=C%14)([H])N4C)=C3)(C(OC)=O)C%15=C(CC[N@@](C2)C1)C%16=CC=CC=C%16N%15

Molecular Formula

C103H130N20O26S4

Molecular Weight

2192.51

References & Citations

[1]Joseph A. Reddy, et al. Folate receptor targeted anti-tumor activity of EC-0225, a folate-targeted dual drug conjugate Free. Cancer Res (2006) 66 (8_Supplement) : 135.