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名称
Roginolisib hemifumarate
别名
罗吉诺利布半富马酸盐
英文名称
Roginolisib hemifumarate
货号
R647769-5mg
包装规格
5mg
浓度
≥99%
储存温度
2-8°C储存,干燥
运输条件
冰袋运输
产品介绍
Roginolisib (MSC2360844) hemifumarate is a potent, orally active and selective PI3Kδ inhibitor, with an IC 50 of 145 nM. Roginolisib hemifumarate shows highly selective against a panel of 278 additional kinases In Vitro Roginolisib hemifumarate (0-10 μM; 1 hours) completely abolished BCR-induced pAkt in Ramos B cells in a concentration-dependent manner with IC 50 values of 280?nM. Roginolisib hemifumarate inhibits B cell proliferation in a concentration-dependent manner with an IC 50 of 48?nM. Roginolisib hemifumarate blocks BCR- and TCR-mediated responses in lymphocytes and TLR-induced IFNα by pDC in human primary cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: B cells Concentration: 0-10 μM Incubation Time: 1 hour Result: Inhibited B cell proliferation in a concentration-dependent manner with an IC 50 of 48 nM. In Vivo Roginolisib hemifumarate (6.6-66 mg/kg; daily from week 2 to 10) ameliorates disease manifestations in a murine SLE model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NZB/W F1 female mice Dosage: 6.6, 22, or 66 mg/kg Administration: Oral; starting at week 2 post ADV-IFNα delivery, once daily at 10 weeks Result: Significantly reduced proteinuria incidence and severity in a dose-dependent manner. Form:Solid IC50& Target:PI3Kδ 145 nM (IC 50 )
生化机理
Roginolisib (MSC2360844) hemifumarate 是一种强效、口服活性和选择性 PI3Kδ 抑制剂,IC 50 为 145 nM。Roginolisib hemifumarate 对其他 278 种激酶具有高度选择性。
CAS号
1621688-31-0
分子式
C26H27FN4O5S.1/2C4H4O4
分子量
584.62 g/mol
PubChem编号
77050629
Isomeric SMILES
C1COCCN1CC2=CC=C(C=C2)N3C4=C(CS(=O)(=O)C5=C4C=CC=C5F)C(=N3)C(=O)N6CCOCC6.C1COCCN1CC2=CC=C(C=C2)N3C4=C(CS(=O)(=O)C5=C4C=CC=C5F)C(=N3)C(=O)N6CCOCC6.C(=C/C(=O)O)\C(=O)O
Smiles
C1COCCN1CC2=CC=C(C=C2)N3C4=C(CS(=O)(=O)C5=C4C=CC=C5F)C(=N3)C(=O)N6CCOCC6.C1COCCN1CC2=CC=C(C=C2)N3C4=C(CS(=O)(=O)C5=C4C=CC=C5F)C(=N3)C(=O)N6CCOCC6.C(=C/C(=O)O)\C(=O)O
PubChem CID
77050629
溶解性
DMSO : 100 mg/mL (171.05 mM; Need ultrasonic)
危险属性
「暂无危险属性」
上下游信息
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技术文档
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Roginolisib hemifumarate 5mg
品牌:阿拉丁
货号:R647769-5mg
级别: ≥99%
货期:30天
已售 377 件
¥
3601
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¥
4321
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运费:0 元
规格:
5mg
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