| 名稱(chēng) | Amuvatinib |
| 描述 | Amuvatinib (MP470) is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity. |
| 細(xì)胞實(shí)驗(yàn) | 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) |
| 激酶實(shí)驗(yàn) | 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. |
| 體外活性 | 通過(guò)腹腔注射10 mg/kg-75 mg/kg或通過(guò)口服50 mg/kg-200 mg/kg MP-470,可以抑制攜帶HT-29,A549和SB-CL2細(xì)胞的小鼠移植瘤模型中腫瘤生長(zhǎng).20 mg/kg MP-470和厄洛替尼聯(lián)用明顯抑制攜帶LNCaP移植瘤的小鼠中的腫瘤生長(zhǎng). |
| 體內(nèi)活性 | 1 μM MP-470抑制MDA-MB-231細(xì)胞中AXL的酪氨酸磷酸化。10 μM MP-470使LNCaP細(xì)胞的細(xì)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(xì)胞中c-Met磷酸化,且使細(xì)胞對(duì)輻射敏感。10 μM MP-470和輻射聯(lián)用,抑制GSK-3β活性,誘導(dǎo)凋亡,且可能通過(guò)抑制Rad51而破壞dsDNA b斷裂修復(fù)。MP-470鹽酸鹽有效抑制OVCAR-3,A549,NCI-H647,DMS-153和 DMS-114細(xì)胞增殖,IC50為0.9 μM–7.86 μM。MP-470對(duì)MiaPaCa-2,PANC-1和GIST882細(xì)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(xì)胞,具有毒性,IC50分別為4 μM和8 μM,且在10 μM時(shí)誘導(dǎo)細(xì)胞凋亡。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 1 mg/ml, Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| 關(guān)鍵字 | HPK56 | c-Kit | MP 470 | MP-470 | HPK-56 | c-Met/HGFR | Apoptosis | Fms like tyrosine kinase 3 | Cluster of differentiation antigen 135 | RET | FLT3 | CD117 | CD135 | Platelet-derived growth factor receptor | PDGFR | SCFR | Amuvatinib | Inhibitor | RAD51 | inhibit |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Thymidine | Sodium 4-phenylbutyrate |
| 相關(guān)庫(kù) | 抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 抗癌活性化合物庫(kù) | 已知活性化合物庫(kù) | 激酶抑制劑庫(kù) | 抗衰老化合物庫(kù) | 酪氨酸激酶分子庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌臨床化合物庫(kù) | 抗癌藥物庫(kù) |