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SGN-2FF Sale

目录号 : GC33031

SGN‐2FF (2-fluorofucose) is an orally bioavailable small‐molecule inhibitor of fucosyltransferase that demonstrated encouraging preclinical antitumor activity in mouse models.

SGN-2FF Chemical Structure

Cas No.:2089647-47-0

规格 价格 库存 购买数量
5mg
¥1,620.00
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10mM (in 1mL Water)
¥1,782.00
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25mg
¥5,184.00
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50mg
¥8,280.00
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100mg
¥13,275.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

SGN‐2FF (2-fluorofucose) is an orally bioavailable small‐molecule inhibitor of fucosyltransferase that demonstrated encouraging preclinical antitumor activity in mouse models.

SGN‐2FF can fully inhibit the fucosylation of the h1F6 mAb at the lowest screening concentration in CHO cells treated with SGN‐2FF. The functional effect of inhibiting fucosylation of LS174T cells with SGN‐2FF is apparent from its diminished adherence to E-selectin–coated plates.[2]

In mice, SGN‐2FF inhibits fucosylation of endogenously produced antibodies, tumor xenograft membranes, and neutrophil adhesion glycans. SGN‐2FF treatment affords complete protection from tumor engraftment in a syngeneic tumor vaccine model, inhibits neutrophil extravasation, and delays the outgrowth of tumor xenografts in immune-deficient mice. [2]

[1] Khanh T Do, et al. Oncologist. 2021 Nov;26(11):925-e1918. [2] Nicole M Okeley, et al. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5404-9.

Chemical Properties

Cas No. 2089647-47-0 SDF
Canonical SMILES F[C@H]1[C@@H]([C@@H]([C@H](C)OC1O)O)O
分子式 C6H11FO4 分子量 166.15
溶解度 Water : 36.67 mg/mL (220.70 mM) 储存条件 Store at -20°C,protect from light
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 6.0187 mL 30.0933 mL 60.1866 mL
5 mM 1.2037 mL 6.0187 mL 12.0373 mL
10 mM 0.6019 mL 3.0093 mL 6.0187 mL
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Research Update

First-In-Human, First-In-Class, Phase I Trial of the Fucosylation Inhibitor SGN-2FF in Patients with Advanced Solid Tumors

Oncologist 2021 Nov;26(11):925-e1918.PMID:34288257DOI:PMC8571760

Lessons learned: Inhibition of glycoprotein fucosylation, as monotherapy and in combination with immune checkpoint blockade, is a promising therapeutic strategy for treating a broad range of cancers. In this first-in-human, first-in-class, phase I study in advanced solid tumors, SGN-2FF demonstrated dose-proportional pharmacokinetics, evidence of pharmacodynamic target inhibition of glycoprotein fucosylation, and preliminary antitumor activity. SGN-2FF was associated with thromboembolic events that led to study termination. Background: We conducted a first-in-human, first-in-class, phase I study of SGN-2FF, a potent small-molecule inhibitor of glycoprotein fucosylation, in patients with advanced solid tumors. Methods: The study consisted of four parts: SGN-2FF monotherapy dose-escalation (part A) and expansion (part B), and SGN-2FF + pembrolizumab dose-escalation (part C) and expansion (part D). The objectives were to evaluate safety and tolerability, maximum tolerated dose (MTD), pharmacokinetics (PK), pharmacodynamics (PD), and antitumor activity of SGN-2FF monotherapy and SGN-2FF + pembrolizumab. Results: Forty-six patients were enrolled (part A, n = 33; part B, n = 6; part C, n = 7; part D did not enroll any patients). During part A (n = 32) exploring 1-15 g once daily (QD) and 2-5 g twice daily (b.i.d.), grade 3 dose-limiting toxicities were diarrhea (2 g and 15 g QD) and increased lipase (2 g QD). The MTD was 10 g daily. In part A, common toxicities were grades 1-2 diarrhea, fatigue, and nausea (each 47%); thromboembolic events (grades 2-5) occurred in 5 of 32 patients (16%). Safety measures included concurrent prophylactic anticoagulation with low-molecular weight heparin (LMWH). In part C, despite the safety measures implemented, a thromboembolic event occurred in one of seven patients (14%) during the SGN-2FF lead-in period. Of 28 evaluable patients in part A, 1 patient with advanced head and neck squamous cell carcinoma achieved Response Evaluation Criteria in Solid Tumors (RECIST) v1.1 complete response (CR) and 10 (36%) had RECIST v1.1 stable disease, including 1 patient with advanced triple-negative breast cancer with 51% tumor burden reduction. SGN-2FF administration led to dose-proportional increases in exposure and PD reduction in protein fucosylation. Conclusion: SGN-2FF demonstrated proof-of-mechanism and preliminary antitumor activity but was associated with thromboembolic events leading to study termination.