LY2409881
(Synonyms: IKK2抑制剂（LY2409881）) 目录号 : GC10093
A selective IKK2 inhibitor
Cas No.:946518-60-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
LY2409881 is a potent and selective inhibitor of IKK2 with IC50 value of 30 nM [1].
IκB kinase β (IKK2) is an enzyme that serves as a subunit of IκB kinase, which is involved in the cytokine-activated immune responses. IKK2 activates nuclear factor kappa-B kinase (NF-κB).
LY2409881 is a selective IKK2 inhibitor and exhibited >10-fold selectivity over other common kinases and IKK1. In the ovarian cancer cell line SKOV3, LY2409881 showed moderate cytotoxicity. While coadministration of LY2409881 and TNFɑ significantly induced cells death, which suggested LY2409881 inhibited NF-κB mediated antiapoptotic signals in a TNFɑ-dependent way. In the DLBCL cell line LY10, LY2409881 (10 μM) inhibited TNFɑ-dependent phosphorylation of IκB. In the DLBCL cell line SUDHL2, LY2409881 (10 μM) inhibited the nuclear signals of p50 and NF-κB. Also, LY2409881 induced apoptosis in a concentration-dependent way [1].
In SCID-beige mice bearing LY10 cell-derived tumors, LY2409881 (50, 100 and 200 mg/kg) significantly inhibited tumor growth [1].
Reference:
[1]. Deng C, Lipstein M, Rodriguez R, et al. The novel IKK2 inhibitor LY2409881 potently synergizes with histone deacetylase inhibitors in preclinical models of lymphoma through the downregulation of NF-κB. Clin Cancer Res, 2015, 21(1): 134-145.
Cell experiment: | OCI-Ly1, OCI-Ly7, and Su-DHL4 are GCB DLBCL cell lines; OCI-Ly3, OCI-Ly10, HBL1, and Su-DHL2 are ABC DLBCL lines. These cell lines are grown in Iscove Modified Dulbecco Medium with 10% FCS. Fresh medium is added every 2 to 3 days, and the cells are kept at a cell concentration of 0.1 to 1×106/mL. Cytotoxicity is evaluated using the CellTiter-Glo Reagent. Experiments are carried out in 96-well plates, with each treatment in triplicate. Samples are taken at typically 24, 48, and 72 hours after treatment. Cytotoxicity is expressed by the decreasing percentage of live cells in each treatment (LY2409881; 0.01, 0.1, 1 and 10 μM) relative to the untreated control from the same experiment, as a function of time. IC50 for each cell line is calculated using the CalcuSyn Version 2.0 software[1]. |
Animal experiment: | Mice[1]Mouse experiments are carried out. Five- to 7-week-old SCID beige mice are injected with 107 Ly10 cells mixed in Matrigel in the posterior flank subcutaneously. When the tumors approach 150 mm3, the mice are divided into four groups of 8 mice: (i) control group, which receive 5% dextrose in water; (ii) LY2409881 at 50 mg/kg in D5W; (iii) LY2409881 at 100 mg/kg in D5W; and (iv) LY2409881 at 200 mg/kg in D5W. LY2409881 or D5W is administered intraperitoneally on day 1 and 4 of every week for 4 weeks. The data are expressed as average tumor volume (mm3) per group as a function of time. Tumor volume is calculated. |
References: [1]. Deng C, et al. The novel IKK2 inhibitor LY2409881 potently synergizes with histone deacetylase inhibitors in preclinical models of lymphoma through the downregulation of NF-κB. Clin Cancer Res. 2015 Jan 1;21(1):134-45. | |
| Cas No. | 946518-60-1 | SDF | |
| 别名 | IKK2抑制剂（LY2409881） | ||
| 化学名 | 2-(5-chloro-2-((3-(4-methylpiperazin-1-yl)propyl)amino)pyrimidin-4-yl)-N-cyclopropylbenzo[b]thiophene-4-carboxamide | ||
| Canonical SMILES | ClC1=CN=C(NCCCN2CCN(C)CC2)N=C1C3=CC4=C(S3)C=CC=C4C(NC5CC5)=O | ||
| 分子式 | C24H32Cl4N6OS | 分子量 | 594.43 |
| 溶解度 | ≥ 59.4mg/mL in DMSO with ultrasonic | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6823 mL | 8.4114 mL | 16.8228 mL |
| 5 mM | 0.3365 mL | 1.6823 mL | 3.3646 mL |
| 10 mM | 0.1682 mL | 0.8411 mL | 1.6823 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet