UNC0379 TFA

目录号: PL15001
UNC0379 TFA 是一个选择性的底物竞争性的赖氨酸甲基转移酶 SETD8 (KMT5A) 抑制剂,IC50 值为 7.3 μM,KD 值 of 18.3 μM。UNC0379 TFA 可用于炎症癌症的研究,如肺纤维化,卵巢癌,神经母细胞瘤。
CAS No. :1620401-83-3
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中文名称
UNC0379 TFA
英文名称
UNC0379 TFA
英文别名
UNC0379 (trifluoroacetate);UNC-0379 trifluoroacetate;6,7-Dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)-pentyl)quinazolin-4-amine trifluoroacetate salt;UNC0379 TFA;UNC0379 trifluoroacetate;UNC0379 trifluoroacetate salt;UNC0379 (TFA);6,7-Dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine x2,2,2-trifluoroacetate;6,7-dimethoxy-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amine;2,2,2-trifluoroacetic acid
Cas No.
1620401-83-3
分子式
C25H36F3N5O4
分子量
527.58
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述
UNC0379 TFA 是一个选择性的底物竞争性的赖氨酸甲基转移酶 SETD8 (KMT5A) 抑制剂,IC50 值为 7.3 μM,KD 值 of 18.3 μM。UNC0379 TFA 可用于炎症癌症的研究,如肺纤维化,卵巢癌,神经母细胞瘤。
产品详情
UNC0379 TFA 是一个选择性的底物竞争性的赖氨酸甲基转移酶 SETD8 (KMT5A) 抑制剂,IC50 值为 7.3 μM,KD 值 of 18.3 μM。UNC0379 TFA 可用于炎症癌症的研究,如肺纤维化,卵巢癌,神经母细胞瘤。
生物活性
UNC0379 TFA is a selective, substrate-competitive inhibitor of lysine methyltransferase SETD8 (KMT5A) with an IC 50 of 7.3 μM, K D value of 18.3 μM. UNC0379 TFA can be used in the research of inflammation and cancers, such as pulmonary fibrosis, ovarian cancer, neuroblastoma.
性状
Solid
IC50 & Target[1][2]
SETD8 (KMT5A)
体外研究(In Vitro)
UNC0379 TFA (1-10 μM, 9 days) inhibits HGSOC cells proliferation.
UNC0379 TFA (10 μM, 96 h) increases in the proportion of sub-G1 phase cells in HGSOC cells.
UNC0379 TFA (10 μM, 48 h) induces myofibroblast de-differentiation and inhibits additional fibroblast to myofibroblast differentiation.
has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
UNC0379 TFA (intratracheal administration, 1 mg/kg/day, 1 mg/kg/day, on day7, 8, and 9) ameliorates the lung fibrosis in Bleomycin (BLM)-induced lung fibrosis mouse. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Ma A, et al. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.
[2]. Miku Wada, et al. Epigenetic Modifier SETD8 as a Therapeutic Target for High-Grade Serous Ovarian Cancer. Biomolecules. 2020 Dec 16;10(12):1686.
溶解度数据
In Vitro: H2O : 100 mg/mL (189.54 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. Ma A, et al. Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.
[2]. Miku Wada, et al. Epigenetic Modifier SETD8 as a Therapeutic Target for High-Grade Serous Ovarian Cancer. Biomolecules. 2020 Dec 16;10(12):1686.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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