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Vepdegestrant (ARV-471) is an oral estrogen receptor PROTAC protein degrader for breast cancer. Vepdegestrant (ARV-471) is a heterobifunctional molecule that promotes the interaction between estrogen receptor alpha and intracellular E3 ligase complexes. Vepdegestrant (ARV-471) causes ubiquitination and subsequent degradation of the estrogen receptor via the proteasome. Vepdegestrant (ARV-471) potently degrades ER-positive The ER in breast cancer cell lines is potently degraded by ARV-471 with a DC50 value of approximately 2 nM.
| Molecular Weight | 723.9 |
| Formula | C45H49N5O4 |
| CAS Number | 2229711-68-4 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage | -20°C, protect from light, dry, sealed |
[2] Diego Garcia Jimenez, et al. ADMET DMPK. Are we ready to design oral PROTACs®?
| Related PROTAC Products |
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| CR8
CR8 is a potent and selective inhibitor of cyclin dependent kinase (CDK1, 2, 5, 7, and 9). |
| ARV-393
ARV-393 is an orally active PROTAC degrader targeting BCL6 for studies related to diffuse large B-cell lymphoma. ARV-393 utilizes the ubiquitin-proteasome system to target the degradation of BCL6. |
| ARV-766
ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations. ARV-766 has the potential to be first- and best-in class PROTAC AR degrader in mCRPC. |
| Indisulam
Indisulam is a carbonic anhydrase inibitor and antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting CDK2, causing a blockade in the G1/S transition. |
| dBET6
dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity. |
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