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Merck

SML1540

Sigma-Aldrich

SBI-0206965

≥98% (HPLC)

别名:

2-((5-溴-2-((3,4,5-三甲氧基苯基)氨基)嘧啶-4-基)氧)-N-甲基苯甲酰胺

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About This Item

经验公式(希尔记法):
C21H21BrN4O5
分子量:
489.32
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 20 mg/mL, clear

儲存溫度

−20°C

SMILES 字串

BrC1=C(OC2=C(C(NC)=O)C=CC=C2)N=C(NC3=CC(OC)=C(OC)C(OC)=C3)N=C1

InChI

1S/C21H21BrN4O5/c1-23-19(27)13-7-5-6-8-15(13)31-20-14(22)11-24-21(26-20)25-12-9-16(28-2)18(30-4)17(10-12)29-3/h5-11H,1-4H3,(H,23,27)(H,24,25,26)

InChI 密鑰

NEXGBSJERNQRSV-UHFFFAOYSA-N

應用

SBI-0206965已用于研究其对镉转化的前列腺上皮细胞生长的影响。

生化/生理作用

SBI-0206965 是丝氨酸/苏氨酸自噬起始激酶 ULK1 和 ULK2 的强效选择性抑制剂,对 ULK1 具有选择性。 SBI-0206965对于ULK1的IC50值为108 nM,而对于ULK2为711 nM。 肿瘤细胞需要自噬来清除错误折叠的蛋白质或受损的细胞器。SBI-0206965可抑制mTOR抑制诱导的细胞自噬。 mTOR信号通常在许多肿瘤中过度活跃,并能驱动增殖,所以mTOR抑制剂作为抗癌药物正在被研究。 然而,mTOR抑制也会导致激活依赖于ulk1的自噬生存反应,而mTOR抑制剂的大多数结果最多只能起到细胞抑制作用。 SBI-0206965协同mTOR抑制诱导细胞凋亡和死亡。
由于大多数肿瘤细胞通过自噬机制存活,因此抑制自噬诱导物Unc-51(丝氨酸/苏氨酸蛋白激酶)样自噬激活激酶(ULK1和ULK2)可能在癌症治疗中有用。

象形圖

Exclamation mark

訊號詞

Warning

危險聲明

危險分類

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

標靶器官

Respiratory system

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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