Vemurafenib-d5(Synonyms: 维罗非尼 d5)

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Vemurafenib-d5 (Synonyms: 维罗非尼 d5)

Vemurafenib-d5 (PLX4032-d5) 是 Vemurafenib 的氘代物。Vemurafenib (PLX4032; RG7204; RO5185426) 是首创的，有效的 B-RAF 选择性抑制剂，能够抑制 RAFV600E 和 c-RAF-1 的活性，IC50 分别为 31 nM 和 48 nM。Vemurafenib 可以诱导细胞自噬 (autophagy)。

Vemurafenib-d5(Synonyms: 维罗非尼 d5)

Vemurafenib-d5 Chemical Structure

CAS No. : 1365986-90-8

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生物活性

Vemurafenib-d5 (PLX4032-d5) is the deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

494.95

Formula

C23H13D5ClF2N3O3S
CAS 号

1365986-90-8
中文名称

维罗非尼 d5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Bollag G, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature, 2010, 467(7315), 596-599.

    [3]. Yang H, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res, 2010, 70(13), 5518-5527.

    [4]. Prahallad A, et al. Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature, 2012, 483(7387), 100-103.

    [5]. Shelledy L, et al. Vemurafenib: First-in-Class BRAF-Mutated Inhibitor for the Treatment of Unresectable or MetastaticMelanoma. J Adv Pract Oncol. 2015 Jul-Aug;6(4):361-5.

    [6]. Wang W, et al. Targeting Autophagy Sensitizes BRAF-Mutant Thyroid Cancer to Vemurafenib.J Clin Endocrinol Metab. 2017 Feb 1;102(2):634-643.

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