Powder: -20°C for 3 years | In solvent: -80°C for 1 year
dTAGV-1 TFA is a highly effective and specific compound that targets mutant FKBP12 F36V fusion proteins for degradation. It possesses potent activity in inducing the degradation of the FKBP12 F36V -Nluc protein in living organisms.
产品描述 | dTAGV-1 TFA is a highly effective and specific compound that targets mutant FKBP12 F36V fusion proteins for degradation. It possesses potent activity in inducing the degradation of the FKBP12 F36V -Nluc protein in living organisms. |
体外活性 | dTAGV-1 (0.1 nM-10 μM; 24 h) TFA induces potent degradation of FKBP12 F36V -Nluc with no effects on FKBP12 WT -Nluc in 293FT cells[1]. dTAGV-1 (125-2000 nM; 24 h) TFA co-treatment with THAL-SNS-032 leads to pronounced degradation of both LACZ-FKBP12 F36V and CDK9[1]. dTAGV-1 (500 nM; 1-24 h) TFA leads to rapid KRAS G12V and pERK1/2 degradation[1]. dTAGV-1 (50-5000 nM; 24 h) TFA enables EWS/FLI degradation in Ewing sarcoma[1]. |
体内活性 | dTAGV-1 (35 mg/kg; i.p. once daily for 4 days) TFA induces degradation of FKBP12 F36V -Nluc in mice[1]. dTAGV-1 (2-10 mg/kg; i.p.) TFA exhbits half-lives (T 1/2 =3.64 and 4.4 h), C max (595 and 2123 ng/mL) and great exposure (AUC inf =3136 and?18517 h?ng/mL) in mice[1]. dTAGV-1 (2 mg/kg; i.v.) TFA exhbits half-life (T 1/2 =3.02 h), C max (7780 ng/mL) and great exposure (AUC inf =3329 h?ng/mL) in mice[1]. Animal Model: 8-week-old immunocompromised female mice were transplanted with MV4;11 luc-FKBP12 F36V cells[1]Dosage: 35 mg/kg Administration: I.p. once daily for 4 days Result: Observed striking loss of bioluminescent signal 4?h after the first and three administrations. Degradation evident 28?h after the final administration. |
分子量 | 1361.58 |
分子式 | C70H91F3N6O16S |
CAS No. | 2624313-15-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
dTAGV-1 TFA 2624313-15-9 dTAGV1 TFA dTAGV 1 TFA Inhibitor inhibitor inhibit