Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Amuvatinib (MP470) 是一种多靶点酪氨酸激酶抑制剂,对突变 c-Kit,PDGFRα,Flt3,c-Met 和 c-Ret 具有活性。它还是一种 DNA 修复抑制剂,靶向蛋白 DNA 修复 RAD51,从而破坏 DNA 损伤修复,具有抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 397 | 现货 | ||
2 mg | ¥ 625 | 现货 | ||
5 mg | ¥ 919 | 现货 | ||
10 mg | ¥ 1,498 | 现货 | ||
25 mg | ¥ 2,760 | 现货 | ||
50 mg | ¥ 3,710 | 现货 | ||
100 mg | ¥ 5,340 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 897 | 现货 |
产品描述 | Amuvatinib (MP470) is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity. |
靶点活性 | c-Kit (D816H):10 nM, PDGFRα (V561D):40 nM, FLT3 (D835Y):81 nM |
体外活性 | 通过腹腔注射10 mg/kg-75 mg/kg或通过口服50 mg/kg-200 mg/kg MP-470,可以抑制携带HT-29,A549和SB-CL2细胞的小鼠移植瘤模型中肿瘤生长.20 mg/kg MP-470和厄洛替尼联用明显抑制携带LNCaP移植瘤的小鼠中的肿瘤生长. |
体内活性 | 1 μM MP-470抑制MDA-MB-231细胞中AXL的酪氨酸磷酸化。10 μM MP-470使LNCaP细胞的细胞周期在G1期停滞,且降低Akt和ERK1/2磷酸化。10 μM MP-470抑制SF767细胞中c-Met磷酸化,且使细胞对辐射敏感。10 μM MP-470和辐射联用,抑制GSK-3β活性,诱导凋亡,且可能通过抑制Rad51而破坏dsDNA b断裂修复。MP-470盐酸盐有效抑制OVCAR-3,A549,NCI-H647,DMS-153和 DMS-114细胞增殖,IC50为0.9 μM–7.86 μM。MP-470对MiaPaCa-2,PANC-1和GIST882细胞具有毒性,IC50为1.6 μM 到3.0 μM。MP-470作用于LNCaP和PC-3,而不是DU145细胞,具有毒性,IC50分别为4 μM和8 μM,且在10 μM时诱导细胞凋亡。 |
激酶实验 | Kinase inhibition assay of c-Kit and PDGFRα: For the testing of inhibitory activity against c-Kit and PDGFRα, enzymes are incubated with varying concentrations of MP-470 and radiolabeled γ-32P-ATP. After 30 min, the reaction mixtures are electrophoresed on an acrylamide gel and autophosphorylation, quantitated by the amount of radioactivity incorporated into the enzyme, is assayed. |
细胞实验 | Cells are plated at a density of 2 × 103 to 1 × 104 cells per well in 100 μL medium on day 0 in 96-well Falcon microtitier plates. On day 1, ten μL of serial dilutions of MP-470 are added to the plates in quadruplicates. After incubation for 4 days, the cells are fixed with 10% Trichloroacetic acid solution. Subsequently, they are labeled with 0.04% Sulforhodamine B (SRB) in 1% acetic acid. After multiple washes to remove the excess dye, 100 μL of 50 mM Tris solution is added to each well in order to dissolve the dye. The absorbance of each well is read on a plate reader at 570 nm. Date are expressed as the percentage of survival of control calculated from the absorbance corrected for background absorbance. The surviving percent of cells is determined by dividing the mean absorbance values of the monoclonal antibody by mean absorbance values of the control and multiplying by 100.(Only for Reference) |
别名 | MP470, HPK 56 |
分子量 | 447.51 |
分子式 | C23H21N5O3S |
CAS No. | 850879-09-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (67 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.2346 mL | 11.1729 mL | 22.3459 mL | 55.8647 mL |
5 mM | 0.4469 mL | 2.2346 mL | 4.4692 mL | 11.1729 mL | |
10 mM | 0.2235 mL | 1.1173 mL | 2.2346 mL | 5.5865 mL | |
20 mM | 0.1117 mL | 0.5586 mL | 1.1173 mL | 2.7932 mL | |
50 mM | 0.0447 mL | 0.2235 mL | 0.4469 mL | 1.1173 mL |
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。
Amuvatinib 850879-09-3 Angiogenesis Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Tyrosine Kinase/Adaptors FLT c-Met/HGFR c-RET DNA/RNA Synthesis PDGFR c-Kit HPK56 MP 470 MP-470 HPK-56 Fms like tyrosine kinase 3 Cluster of differentiation antigen 135 RET FLT3 CD117 CD135 Platelet-derived growth factor receptor SCFR MP470 Inhibitor RAD51 HPK 56 inhibit inhibitor