货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T29295-1ml	10mM in DMSO	￥1300.00 T29295-1ml ￥1300.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T29295-1ml

10mM in DMSO

￥1300.00

货期：3-5天

产品描述：

(R)-GNE-140是选择性的LDHA 和 LDHB抑制剂，IC50分别为3 nM和5 nM。(R)-GNE-140的效力是其S型异构体的18倍

靶点：

LDHA(Cell-free assay):3 nM; LDHB(Cell-free assay):5 nM

体外研究：

(R)-GNE-140 inhibits proliferation in 37 of 347 cancer cell lines tested at a potency cut off of 5 μM. (R)-GNE-140 exhibits inhibition with two chondrosarcoma (bone) cancer cell lines that harbored IDH1 mutations (IC50 = 0.8μM).(R)-GNE-140 has submicromolar MiaPaca2 potency and inhibits proliferation in 11% of cancer cell lines in a broad panel.

体内研究：

(R)-GNE-140 presents a low Clp, and also had high bioavailability when dosed orally at 5 mg/kg to mice. At higher oral doses, ranging from 50 to 200 mg/kg, (R)-GNE-140 displays greater in vivo exposure

细胞实验：

Cell lines: 105KC,JJ012,143B,G84,1321N1,ONS-76,G22,G140,G96,HCC1143,CAL-120,Hs 578T,SISO,SKG-II,HCT-15,KYSE-520,KMRC-1,SNU-475,SNU-423,HT-1080,NCI-H1437,NCI-H1339,LXF-289,MCAS,PA-1,Hs 38.T,59M,MIA PaCa-2,SW 1990,PSN1,GR-M,Hs 746T,MKN-74,S-117,FTC-238,B-CPAP,HEC-265 cell lines Concentrations: 6 pt dose titration scheme Incubation Time: 72 h Method: Cells are plated using optimal seeding densities in 384-well plates using RPMI, 5% FBS, 100 ug/ml penicillin, 100 units/ml streptomycin. Optimal seeding densities are established for each cell line in order to reach 75-80% confluence at the end of the assay. The following day, cells are treated with (R)-GNE-140 using a 6 pt dose titration scheme. After 72 hours, cell viability is assessed using the CellTiter-Glo® Luminescence Cell Viability assay. Absolute inhibitory concentration (IC) values are calculated using four-parameter logistic curve fitting.

动物实验：

Animal Models: Female CD-1 mice Dosages: IV: 1.0 mg/kg; Oral: 5,50,100,200 mg/kg Administration: IV / Oral

参考文献：

1. Purkey, Hans E. , et al. Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice. ACS Med Chem Lett. 2016 Aug 26;7(10):896-901. eCollection 2016 Oct 13.

溶解性：

Soluble in DMSO

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.004 ml	10.019 ml	20.038 ml
5 mM	0.401 ml	2.004 ml	4.008 ml
10 mM	0.2 ml	1.002 ml	2.004 ml
50 mM	0.04 ml	0.2 ml	0.401 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

CS-2624

(R)-GNE-140 ；GNE140

参考文献

质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)