Name: EC1167 hydrochloride
Brand: BOC Sciences
Rating: 5 (1 reviews)

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IUPAC Name

(2S)-2-[[(1S)-1-carboxy-5-[[4-[2-[[(2S)-3-carboxy-1-[[(2S)-3-carboxy-1-[[(1R)-1-carboxy-2-sulfanylethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-2-oxoethyl]phenyl]methylcarbamoylamino]pentyl]carbamoylamino]pentanedioic acid;hydrochloride

Canonical SMILES

C1=CC(=CC=C1CC(=O)NC(CC(=O)O)C(=O)NC(CC(=O)O)C(=O)NC(CS)C(=O)O)CNC(=O)NCCCCC(C(=O)O)NC(=O)NC(CCC(=O)O)C(=O)O.Cl

InChI

InChI=1S/C33H45N7O17S.ClH/c41-23(36-20(12-25(44)45)27(48)37-21(13-26(46)47)28(49)38-22(15-58)31(54)55)11-16-4-6-17(7-5-16)14-35-32(56)34-10-2-1-3-18(29(50)51)39-33(57)40-19(30(52)53)8-9-24(42)43;/h4-7,18-22,58H,1-3,8-15H2,(H,36,41)(H,37,48)(H,38,49)(H,42,43)(H,44,45)(H,46,47)(H,50,51)(H,52,53)(H,54,55)(H2,34,35,56)(H2,39,40,57);1H/t18-,19-,20-,21-,22-;/m0./s1

InChIKey

OIRSWDXVPXXSCP-QXJGFYJDSA-N

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EC1167 hydrochloride is a small molecule widely recognized in the realm of pharmaceutical research, particularly as a linker in drug conjugates for targeted cancer therapy. This compound serves as a critical component in the design and development of EC1169, a prostate-specific membrane antigen (PSMA) targeting-tubulysin conjugate. Such conjugates are essential in advancing targeted therapy approaches, providing a mechanism to deliver potent cytotoxic agents directly to cancer cells, thereby minimizing the adverse effects commonly seen with traditional chemotherapy. This targeted approach is particularly promising for treating metastatic, castration-resistant prostate cancer (MCRPC), a challenging form of cancer that necessitates innovative therapeutic strategies.

The significance of EC1167 hydrochloride in drug discovery extends beyond its role as a mere chemical linker. It exemplifies the trend towards precision medicine, where treatments are tailored to the specific genetic makeup and characteristics of cancer cells. By utilizing this linker, researchers can engineer the conjugate EC1169 to bind selectively to PSMA, a protein abundantly expressed on the surface of prostate cancer cells, but limited in other tissues. This specificity not only enhances the efficacy of the treatment by ensuring that the cytotoxin is delivered precisely where it is needed, but it also reduces systemic toxicity, a common issue with non-targeted chemotherapeutic agents.

In the broader landscape of pharmaceutical development, EC1167 hydrochloride represents a critical leap forward in the synthesis of antibody-drug conjugates (ADCs) and other drug conjugates. These conjugates are pivotal in modern oncology, offering a synergistic approach to cancer treatment by combining the targeting capabilities of antibodies or ligands with the potent cell-killing effects of cytotoxic drugs. EC1167 hydrochloride enhances the stability and efficacy of these conjugates, ensuring that they remain intact until they reach their target, thereby optimizing therapeutic outcomes. The development and application of such linkers underscore the collaborative nature of medicinal chemistry and oncology, as researchers integrate chemical synthesis with biological insights to develop safer and more effective cancer therapies.

As research progresses, the potential applications of EC1167 hydrochloride could expand into other domains of targeted therapy, including other cancer types that express specific surface antigens recognizable by engineered drug conjugates. The safety profile and targeted delivery capabilities of drug conjugates employing EC1167 hydrochloride as a linker may also lend themselves to personalized medicine approaches, where treatments are crafted to meet the unique needs of individual patients. This versatility highlights the importance of chemical linkers in the future of drug design, emphasizing their role in realizing the full potential of targeted therapies in combating cancer.