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• 产品描述： Amuvatinib is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.

• 靶点： Apoptosis;c-Kit;c-Met/HGFR;c-RET;DNA/RNA Synthesis;FLT;PDGFR

• 体外研究： 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

• 体内研究： 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

• 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)

• 动物实验： Animal Models: Mice (athymic nude) xenograft models of HT-29, A549, and SB-CL2 cells Dosages: 10 mg/kg–75 mg/kg (i.p.) or 50 mg/kg–200 mg/kg (p.o.) Administration: Oral gavage (qd5 × 3 weeks) or intraperitoneal injection (qd5 × 2 weeks)

• 参考文献：
  1. Welsh JW, et al. The c-Met receptor tyrosine kinase inhibitor MP470 radiosensitizes glioblastoma cells. Radiat Oncol, 2009, 4, 69. 2. Qi W, et al. MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer. BMC Cancer, 2009, 9, 142. 3. Mahadevan D, et al. A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors. Oncogene, 2007, 26(27), 3909-3919. 4. Han H W, Hahn S, Jeong H Y, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent[J]. Scientific reports. 2018 Oct 8;8(1):14969. 5. Hurley LH, et al. World Patent, WO/2005/037825.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.235 ml	11.173 ml	22.345 ml
  5 mM	0.447 ml	2.235 ml	4.469 ml
  10 mM	0.223 ml	1.117 ml	2.235 ml
  50 mM	0.045 ml	0.223 ml	0.447 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *