1466546-45-1
Chemical Structure
NMS-P528
- CAS No.: 1466546-45-1
- Formula:C27H28ClN3O3S
- Molecular Weight:510.05
InChIKey: DLGMWIQPGAEPPC-GOSISDBHSA-N
SMILES: ClC[C@@H](C1=C2C=C(O)C3=C1C(C)=CS3)CN2C(C(N4)=CC5=C4C=CC(OCCN6CCCC6)=C5)=O
Biological Activity: NMS-P528 is a DNA minor groove alkylating agent and ADC payload. NMS-P528 undergoes intramolecular cyclization to form reactive electrophilic derivatives, which in turn induce DNA damage, cell cycle arrest, and Apoptosis. NMS-P528 shows no significant anti-tumor activity as a free payload in a HER2-negative Raji lymphoma mouse xenograft model. NMS-P528 serves as the cytotoxic payload for the antibody-drug conjugate EV20/NMS-P945. NMS-P528 can be used in research related to breast cancer, gastric cancer, colon adenocarcinoma, Burkitt's lymphoma, neuroblastoma, pancreatic cancer, prostate cancer, head and neck cancer, ovarian cancer, and melanoma[1][2][3].
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NMS-P528 | NMS-P528 is a DNA minor groove alkylating agent and ADC payload. NMS-P528 undergoes intramolecular cyclization to form reactive electrophilic derivatives, which in turn induce DNA damage, cell cycle arrest, and Apoptosis. NMS-P528 shows no significant anti-tumor activity as a free payload in a HER2-negative Raji lymphoma mouse xenograft model. NMS-P528 serves as the cytotoxic payload for the antibody-drug conjugate EV20/NMS-P945. NMS-P528 can be used in research related to breast cancer, gastric cancer, colon adenocarcinoma, Burkitt's lymphoma, neuroblastoma, pancreatic cancer, prostate cancer, head and neck cancer, ovarian cancer, and melanoma. | |||||||||||||||||||||
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- [1]. Valsasina B, et al. Novel Thienoduocarmycin-Trastuzumab ADC Demonstrates Strong Antitumor Efficacy with Favorable Safety Profile in Preclinical Studies. Molecular cancer therapeutics. 2023 Dec 01;22(12):1465-1478. [Content Brief]
- [2]. Sano R, et al. An antibody-drug conjugate directed to the ALK receptor demonstrates efficacy in preclinical models of neuroblastoma. Science translational medicine. 2019 Mar 13;11(483):eaau9732. [Content Brief]
- [3]. Capone E, et al. EV20/NMS-P945, a Novel Thienoindole Based Antibody-Drug Conjugate Targeting HER-3 for Solid Tumors. Pharmaceutics. 2021 Apr 02;13(4):483. [Content Brief]
Keywords
