Amuvatinib
作者：齊岳
發布時間：2023-08-22
09:22:11
點擊數：
產品名稱：Amuvatinib
產品描述：
| 產品描述 | Amuvatinib is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity. |
| 靶點活性 | c-Kit (D816H):10 nM, PDGFRα (V561D):40 nM, FLT3 (D835Y):81 nM |
| 體外活性 | 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移植瘤的小鼠中的生長. |
| 體內活性 | 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。 |
| 激酶實驗 | 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. |
| 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) |
| 別名 | HPK 56, MP470 |
| 分子量 | 447.51 |
| 分子式 | C23H21N5O3S |
| CAS No. | 850879-09-3 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 30 mg/mL (67 mM)
Ethanol: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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