GDC-0810 (ARN-810) - CAS 1365888-06-7
Catalog number: 1365888-06-7
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Estrogen Receptor/ERR
GDC-0810, also known as ARN-810 and RG6046, an orally bioavailable Selective Estrogen Receptor Degrader (SERD) that demonstrates robust activity in tamoxifen-resistant breast cancer xenografts.
Solid powder
GDC0810; GDC 0810; GDC-0810; ARN810; ARN 810; ARN-810; RG6046; RG-6046; RG 6046.
Soluble in DMSO, not in water
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf Life:
2 years if stored properly
Canonical SMILES:
1.Novel Selective Estrogen Receptor Downregulators (SERDs) Developed against Treatment-Resistant Breast Cancer.
Xiong R;Zhao J;Gutgesell LM;Wang Y;Lee S;Karumudi B;Zhao H;Lu Y;Tonetti DA;Thatcher GR J Med Chem. 2017 Feb 23;60(4):1325-1342. doi: 10.1021/acs.jmedchem.6b01355. Epub 2017 Feb 10.
Resistance to the selective estrogen receptor modulator tamoxifen and to aromatase inhibitors that lower circulating estradiol occurs in up to 50% of patients, generally leading to an endocrine-independent ER+ phenotype. Selective ER downregulators (SERDs) are able to ablate ER and thus, theoretically, to prevent survival of both endocrine-dependent and -independent ER+ tumors. The clinical SERD fulvestrant is hampered by intramuscular administration and undesirable pharmacokinetics. Novel SERDs were designed using the 6-OH-benzothiophene (BT) scaffold common to arzoxifene and raloxifene. Treatment-resistant (TR) ER+ cell lines (MCF-7:5C and MCF-7:TAM1) were used for optimization, followed by validation in the parent endocrine-dependent cell line (MCF-7:WS8), in 2D and 3D cultures, using ERα in-cell westerns, ERE-luciferase, and cell viability assays, with 2 (GDC-0810/ARN-810) used for comparison. Two BT SERDs with superior in vitro activity to 2 were studied for bioavailability and shown to cause regression of a TR, endocrine-independent ER+ xenograft superior to that with 2.
2.Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts.
Lai A;Kahraman M;Govek S;Nagasawa J;Bonnefous C;Julien J;Douglas K;Sensintaffar J;Lu N;Lee KJ;Aparicio A;Kaufman J;Qian J;Shao G;Prudente R;Moon MJ;Joseph JD;Darimont B;Brigham D;Grillot K;Heyman R;Rix PJ;Hager JH;Smith ND J Med Chem. 2015 Jun 25;58(12):4888-904. doi: 10.1021/acs.jmedchem.5b00054. Epub 2015 May 22.
Approximately 80% of breast cancers are estrogen receptor alpha (ER-α) positive, and although women typically initially respond well to antihormonal therapies such as tamoxifen and aromatase inhibitors, resistance often emerges. Although a variety of resistance mechanism may be at play in this state, there is evidence that in many cases the ER still plays a central role, including mutations in the ER leading to constitutively active receptor. Fulvestrant is a steroid-based, selective estrogen receptor degrader (SERD) that both antagonizes and degrades ER-α and is active in patients who have progressed on antihormonal agents. However, fulvestrant suffers from poor pharmaceutical properties and must be administered by intramuscular injections that limit the total amount of drug that can be administered and hence lead to the potential for incomplete receptor blockade. We describe the identification and characterization of a series of small-molecule, orally bioavailable SERDs which are potent antagonists and degraders of ER-α and in which the ER-α degrading properties were prospectively optimized. The lead compound 11l (GDC-0810 or ARN-810) demonstrates robust activity in models of tamoxifen-sensitive and tamoxifen-resistant breast cancer, and is currently in clinical trials in women with locally advanced or metastatic estrogen receptor-positive breast cancer.
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CAS 1365888-06-7 GDC-0810 (ARN-810)

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