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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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| MS4322
MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. |
| xStAx-VHLL TFA
xStAx-VHLL TFA, a PROTAC, sustains β-catenin degradation and manifested strong inhibition of Wnt signaling. xStAx-VHLL TFA promotes β-catenin ubiquitination. |
| (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level. |
| MTX-23
MTX-23 is an AR-based PROTAC. MTX-23 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. MTX-23 induces apoptosis. |
| YD23
YD23 is a SMARCA2 PROTAC. |
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