BAY-985
- CAS号:2409479-29-2
- 英文名:BAY-985
- 中文名:BAY-985
- CBNumber:CB55839640
- 分子式:C27H30F3N9O
- 分子量:553.58
- MOL File:2409479-29-2.mol
- 沸点 :753.3±70.0 °C(Predicted)
- 密度 :1.373±0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO: 50 mg/mL (90.32 mM)
- 形态 :A solid
- 酸度系数(pKa) :10.06±0.10(Predicted)
- 颜色 :Light yellow to yellow
BAY-985性质、用途与生产工艺
- 生物活性 BAY-985是一种有效、高选择性的TBK1/IKKε抑制剂。 BAY-985对TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay)和IKKε (IC50 = 2 nM)具有高效力，在机械性细胞phosphorylation of interferon regulatory factor 3(pIRF3)分析中也具有高效力(IC50 = 74 nM)，并且对SK-MEL-2细胞具有抗增殖作用(IC50 = 900 nM)。
-
靶点
Target Value TBK1
(in low ATP assay)2 nM IKKε
(Cell-free assay)2 nM TBK1
(in high ATP assay)30 nM pIRF3
(Cell-free assay)74 nM -
体外研究
BAY-985 inhibits FLT3, RSK4, DRAK1, and ULK1 with IC 50 s of 123, 276, 311, and 7930 nM, respectively.
BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 (IRF3) with an IC 50 of 74 nM.
BAY-985 is active in cellular mechanistic assay and shows anti-proliferative activity in a few cancer cell lines with IC 50 s of 900 and 7260 nM for SK-MEL2 (NRAS and TP53 mutated) and ACHN (CDKN2A mutated) cells, respectively.Cell Proliferation Assay
Cell Line: ACHN and SK-MEL-2 cell lines Concentration: Incubation Time: 96 hours Result: Inhibited proliferation in SK-MEL2 and ACHN cells with IC 50 s of 900 and 7260 nM, respectively. -
体内研究
BAY-985 (200 mg/kg; p.o.; b.i.d.; 111 days) results in weak antitumor efficacy.
BAY-985 shows high clearance (CL b = 4.0 L/h/kg, ca. 95% hepatic extraction), large volume of distribution at steady state (V ss =2.9 L/kg) and a short terminal half-life (t 1/2 =0.79 h).Animal Model: Female NMRI nude mice bearing SK-MEL-2 human melanoma xenograft model Dosage: 200 mg/kg Administration: Applied p.o.; twice daily (b.i.d.) continuously 111 days Result: Treatment resulted in weak antitumor efficacy with a T/C tumor weight ratio of 0.6.
The treatment was well tolerated, with a maximum body weight loss of less than 10%.
- 更新日期：2024/08/19
- 产品编号：HY-133117
- 产品名称：BAY-985
- CAS编号：
- 包装：1 mg
- 价格：1714元
- 更新日期：2024/08/19
- 产品编号：S8935
- 产品名称：BAY-985 BAY-985
- CAS编号：2409479-29-2
- 包装：5mg
- 价格：4668.48元
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：+1-781-999-5354 +1-00000000000
- 电子邮件：marketing@targetmol.com
- 国家：美国
- 产品数：19892
- 优势度：58
- 公司名称：Aladdin Scientific
- 联系电话：+1-+1(833)-552-7181
- 电子邮件：sales@aladdinsci.com
- 国家：美国
- 产品数：57511
- 优势度：58
- 公司名称：CAYMAN
- 联系电话：--
- 电子邮件：cayman@caymanchem.com
- 国家：美国
- 产品数：6618
- 优势度：81
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
