CB-839
货号：
IC2470
品牌：
Jinpan
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产品简介
| 有效期 | 2年 |
| 描述 | 是一种有效的，选择性的 glutaminase 抑制剂。 |
| MDL | MFCD28167826 |
| CAS | 1439399-58-2 |
| 分子式 | C26H24F3N7O3S |
| 分子量 | 571.57 |
| 储存条件 | 2-8℃ |
| 纯度 | ≥98% |
| 外观（性状） | Solid |
| 单位 | 瓶 |
| 生物活性 | CB-839 (Telaglenastat) 是一种有效的，选择性的，口服生物可利用的 glutaminase 抑制剂，对重组人GAC的 IC50 为 24 nM。CB-839(Telaglenastat)可诱导自噬并具有抗肿瘤活性。[1] |
| In Vitro | CB-839表现出时间依赖性和缓慢可逆的动力学特性。与rHu-GAC预培养1小时后，CB-839抑制谷氨酰胺酶的IC50值<50 nmol> |
| In Vivo | 在小鼠TNBC模型中，单剂CB-839 (200 mg/kg, p.o.)抑制相对于载体对照61%的肿瘤生长。在小鼠JIMT-1异种移植模型中，CB-839单独用药(200 mg/kg, p.o.)导致相对载体对照54%的肿瘤生长抑制(TGI)，CB-839 (200 mg/kg, p.o.)和paclitaxel (10 mg/kg, p.o.)联合用药很大程度上抑制肿瘤的再生长，相对于载体对照，引起100%的肿瘤生长抑制(TGI)。[1] |
| SMILES | O=C(NC1=NN=C(CCCCC2=NN=C(NC(CC3=CC=CC(OC(F)(F)F)=C3)=O)C=C2)S1)CC4=NC=CC=C4 |
| 靶点 | Glutaminase |
| 动物实验 | CB-839 and metabolite levels were measured in tumors and tissues excised from female Scid/Bg mice (Charles River Laboratories; age 6–9 weeks, 17–23 g) implanted with HCC1806 cells in the mammary fat pad (2.5 x 106 cells/mouse; tumor volume~500 mm3 at time of dosing) 4 hours after oral administration of 200 mg/kg CB-839 or vehicle. The vehicle consisted of 25% (w/v) hydroxypropyl-b-cyclodextrin (HPBCD) in 10 mmol/L citrate, pH 2. CB-839 was formulated as a solution at 20 mg/mL (w/v) in vehicle; the dose volume for all groups was 10 mL/kg.[1] |
| 细胞实验 | For viability assays, all cell lines were treated with CB-839 at the indicated concentrations for 72 hoursin duplicate wells and analyzed for antiproliferative effects using Cell Titer Glo. [1] |
| 数据来源文献 | [1]. Gross MI, Demo SD, Dennison JB, Chen L, Chernov-Rogan T, Goyal B, Janes JR, Laidig GJ, Lewis ER, Li J, Mackinnon AL, Parlati F, Rodriguez ML, Shwonek PJ, Sjogren EB, Stanton TF, Wang T, Yang J, Zhao F, Bennett MK. Antitumor activity of the glutaminase inhibitor CB-839 in triple-negative breast cancer. Mol Cancer Ther. 2014 Apr;13(4):890-901. |
| 规格 | 5mg 10mg |