貨號	規(guī)格	價格	上海	北京	武漢	南京
S81002-5mg	99.9%	￥564.40 S81002-5mg ￥564.40 現貨	4 4	-	-	-
S81002-10mg	99.9%	￥1088.00 S81002-10mg ￥1088.00 現貨	7 7	-	-	-
S81002-25mg	99.9%	￥2176.00 S81002-25mg ￥2176.00 現貨	6 6	-	-	-
S81002-100mg	≥99%	￥4692.00 S81002-100mg ￥4692.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

Amuvatinib is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.

產品描述：

Amuvatinib is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.

靶點：

Apoptosis;c-Kit;c-Met/HGFR;c-RET;DNA/RNA Synthesis;FLT;PDGFR;Apoptosis;?FLT;?c-Met/HGFR;?c-RET;?DNA/RNASynthesis;?PDGFR;?c-Kit

體外研究：

通過腹腔注射10 mg/kg-75 mg/kg或通過口服50 mg/kg-200 mg/kg MP-470,可以抑制攜帶HT-29,A549和SB-CL2細胞的小鼠移植瘤模型中腫瘤生長.20 mg/kg MP-470和厄洛替尼聯用明顯抑制攜帶LNCaP移植瘤的小鼠中的腫瘤生長

體內研究：

1 μM MP-470抑制MDA-MB-231細胞中AXL的酪氨酸磷酸化。10 μM MP-470使LNCaP細胞的細胞周期在G1期停滯,且降低Akt和ERK1/2磷酸化。10 μM MP-470抑制SF767細胞中c-Met磷酸化,且使細胞對輻射敏感。10 μM MP-470和輻射聯用,抑制GSK-3β活性,誘導凋亡,且可能通過抑制Rad51而破壞dsDNA b斷裂修復。MP-470鹽酸鹽有效抑制OVCAR-3,A549,NCI-H647,DMS-153和 DMS-114細胞增殖,IC50為0.9 μM–7.86 μM。MP-470對MiaPaCa-2,PANC-1和GIST882細胞具有毒性,IC50為1.6 μM 到3.0 μM。MP-470作用于LNCaP和PC-3,而不是DU145細胞,具有毒性,IC50分別為4 μM和8 μM,且在10 μM時誘導細胞凋亡

細胞實驗：

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)

動物實驗：

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)

參考文獻：

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

保存條件：

-20℃

配置溶液濃度參考：

	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

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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Amuvatinib (MP-470)