R428 (BGB324)

目录号:S2841

R428 (BGB324) Chemical Structure

Molecular Weight(MW): 506.64

R428 (BGB324)是一种Axl抑制剂,IC50为14 nM,作用于Axl比作用于Abl选择性高100倍以上。作用于Axl选择性也比作用于Mer和Tyro3(高50到100倍)及InsR, EGFR, HER2,和PDGFRβ(高100倍以上)高。

规格 价格 库存 购买数量  
RMB 3027.37 现货
RMB 7120.16 现货
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客户使用该产品的4个实验数据:

  • Cetuximab-resistant cells are sensitive to therapeutic blockade of AXL activity with the AXL TKI R428. Cells were treated with vehicle (-) or indicated doses of R428 for 24 hours before harvesting whole-cell lysate and immunoblotting for the indicated proteins. α-Tubulin was used as a loading control.

    Cancer Res 2014 74(18), 5152-64. R428 (BGB324) purchased from Selleck.

    B) The processing of AXL is increased by an AXL kinase inhibitor. Panc-28 cells were incubated overnight with DMSO or 150 nM R428, a selective AXL kinase inhibitor, before examining by Western blot the levels of endogenous AXL-FL and AXL-CTF (C-20; left). Levels of AXL-CTF in DAPT-treated cells were quantified as described above and unpaired Student’s t test was employed for the analysis (right). Data are shown as means±SEM (n = 4). ***P<0.001.

    FASEB J, 2017, 31(4):1382-1397. R428 (BGB324) purchased from Selleck.

  • HCC827-ER cells were divided into four subgroups and treated with 15 μM Erlotinib, 1 μM R428 (a specific AXL inhibitor), 1 μM R428 + 15 μM Erlotinib, and DMEM as a control for 24 h, respectively. Cell viability (A) and apoptosis (B) in HCC827-ER were assessed by MTT and apoptosis assays, respectively. (*P<0.05 vs Control). Expression of the AXL, MAPK, AKT, Survivin and apoptosis pathway-related proteins were assessed by immunoblotting.

    Am J Transl Res, 2016, 8(11):4857-4868. R428 (BGB324) purchased from Selleck.

    Axl inhibitor promotes the apoptosis induced by ALK-TKIs. (A) After treated with crizotinib (100 nM), BGB324 (300 nM) or their combination for 48 h, cell apoptosis was determined by flow cytometry. (B) The induction of apoptosis by ceritinib (100 nM), BGB324 (300 nM) or their combination was examined. (C and D) Cells were treated with crizotinib (100 nM), BGB324 (300 nM) or their combination for 48 h, then whole-cell lysates were collected and the levels of indicated protein were analyzed by Western blot in (C) NB1643 and (D) SHSY5Y cells. *P < 0.05 for the indicated comparisons; ns, not significant.

    Biochem Bioph Res Co 2014 10.1016/j.bbrc.2014.10.126. R428 (BGB324) purchased from Selleck.

产品安全说明书

TAM Receptor抑制剂选择性比较

生物活性

产品描述 R428 (BGB324)是一种Axl抑制剂,IC50为14 nM,作用于Axl比作用于Abl选择性高100倍以上。作用于Axl选择性也比作用于Mer和Tyro3(高50到100倍)及InsR, EGFR, HER2,和PDGFRβ(高100倍以上)高。
靶点
Axl [1]
(Cell-free assay)
14 nM
体外研究

R428阻断Axl的催化和促癌活性。纳摩尔级R428抑制Axl活性并阻断Axl依赖的过程,包括Akt 磷酸化, 乳腺癌细胞入侵以及促炎细胞因子产生 [1] 。最近一项研究表明Axl 抑制剂R428 对原发性CLL B细胞处理24小时后平均IC50约为2.0μM,而类似条件下正常的B细胞, T细胞和自然杀伤细胞(NK) 在R428 (2.5 μM)浓度时没有明显的细胞死亡[2]

体内研究 药理学研究表明口服R428治疗后可以降低肿瘤中巨噬细胞集落刺激因子和上皮间质转化的转录调节因子Snail的表达,这种作用具有剂量依赖特性。R428在角膜微囊和肿瘤模型中抑制血管新生,这支持了之前的一项研究。在MDA-MB-231心内和4T1原位乳腺癌转移小鼠模型中,R428 治疗可以减轻癌细胞转移负担并延长生存期 (与对照组52天相比中位生存期大于80天,P<0.05) [1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

+ 展开

体外激酶分析:

在体外激酶放射性测量分析中进行R428的五点剂量滴定。同时利用荧光偏振法进行Axl, Mer和 Tyro3的分析。利用Z
细胞实验:

[1]

+ 展开
  • Cell lines: MDA-MB-231或者4T1细胞
  • Concentrations: 0.03, 0.3, 3 μM
  • Incubation Time: 3 小时
  • Method:

    在37 ℃条件下让MDA-MB-231或4T1细胞从基质胶沿着24孔Transwell培养板的8微米气孔迁移到20% FCS ,迁移时间16 到 24小时。将未迁移走的细胞和基质胶擦除掉。侵入的细胞用 4% 甲醛固定, 1% 结晶紫染色然后定量用于基于细胞的Axl分析。细胞先与R428预孵育3小时。 Transwell培养室上部和下部都加入 R428 。


    (Only for Reference)
动物实验:

[1]

+ 展开
  • Animal Models: 心脏内含有MDA-MB-231-luc-D3H2LN细胞的动物模型
  • Formulation: 0.5% 羟丙基甲基纤维素 + 0.1% 吐温80
  • Dosages: 125 mg/kg
  • Administration: 口服,一天两次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 6 mg/mL warmed (11.84 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+corn oil
1mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 506.64
化学式

C30H34N8

CAS号 1037624-75-1
稳定性 powder
in solvent
别名

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03649321 Not yet recruiting Cancer of Pancreas University of Texas Southwestern Medical Center|Triligent International|Translational Genomics Research Institute|BerGenBio ASA November 2018 Phase 1|Phase 2
NCT02872259 Recruiting Melanoma Haukeland University Hospital|BerGenBio ASA January 2017 Phase 1|Phase 2
NCT02922777 Recruiting Non-Small Cell Lung Carcinoma University of Texas Southwestern Medical Center|Texas Tech University Health Sciences Center|BerGenBio ASA November 2016 Phase 1
NCT02424617 Recruiting Non-Small Cell Lung Cancer BerGenBio ASA|Chiltern International Inc. March 2015 Phase 1|Phase 2
NCT02488408 Recruiting Acute Myeloid Leukemia|Myelodysplastic Syndromes BerGenBio ASA September 2014 Phase 1|Phase 2

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    Could you please let me know whether this compound is an enantiomer or it is in its racemic form?

  • 回答:

    Our S2841 R428 is S enantiomer, and its e.e. value (enantiomeric purity) >98%.

TAM Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID