ARV-766 free base · Synonyms: Luxdegalutamide

ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader.

For research use only. Not for human or veterinary use.

Target PROTACs Androgen Receptor

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

ARV-766 structure

CAS No.: 2750830-09-0

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 425.00	BP-02047-50mg	In stock	Get quote
100 mg	USD 725.00	BP-02047-100mg	In stock	Get quote
250 mg	USD 1,225.00	BP-02047-250mg	In stock	Get quote
500 mg	USD 1,885.00	BP-02047-500mg	In stock	Get quote
1 g	Inquire	BP-02047-1g	In stock	Inquire

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Description

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.

Biological activity

Luxdegalutamide (0.03-30 μM, 48 h) induces the expression of CYP3A4 and CYP2C8 mRNA instead of CYP1A2, 2B6, and 2C9 mRNA, with little effect on cytochrome P450 (CYP) and transporter mediated drug interactions (DDI) Luxdegalutamide exhibits anti-tumor activity in mouse LNCaP and VCaP xenograft models

Identifiers

SMILES: CC(C)([C@@H](C1(C)C)NC(C2=CC=C(N3CCC(CC3)CN4CCN(C5=CC(F)=C(C=C5)C(N[C@@H]6C(NC(CC6)=O)=O)=O)CC4)C=C2)=O)[C@@H]1OC7=CC(OC)=C(C=C7)C#N
InChIKey: RDPPBRKNBBXPNZ-FMPIRMQTSA-N

Specifications

MW (average): 807.9520
Formula: C₄₅H₅₄FN₇O₆
CAS No.: 2750830-09-0
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Solid -20℃ 2 years; In solvent -20℃ 1 month; sealed storage, away from moisture

Solubility

Soluble in DMSO : 100 mg/mL

Documents

References

[1]. Petrylak D P, et al. A phase 2 expansion study of ARV-766, a PROTAC androgen receptor (AR) degrader, in metastatic castration-resistant prostate cancer (mCRPC)[J]. 2023.

Same target

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Same research area

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