AZ 628 化学構造
分子量: 451.52



Quality Control & MSDS


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製品説明 AZ 628は力なチロシン・タンパク質阻害剤、 野生のタイプCRAFと BRAF V600Eに作用すると、 IC50 がそれぞれ 29 nM と 34 nMになる。
ターゲット wild-type CRAF BRAFV600E wild-type BRAF
IC50 29 nM 34 nM 100 nM [1]
In vitro試験 AZ628 prevents activation of number of tyrosine protein kinases including VEGFR2, DDR2, Lyn, Flt1, FMS and others. AZ628 suppresses anchorage-dependent and -independent growth, gives rise to cell cycle arrest, and induces apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation. The profile of AZ628 cross-reactivity suggests that similar to sorafenib, AZ628 may be antiangiogenic based on prevention of VEGFR2. [1] AZ628-resistant clones are approximately 100-fold more resistant to AZ628 than the parental cell line, exhibiting IC50 of approximately 10 μM, compared with 0.1 μM for the parental cell line. Effective suppression of p-ERK1/2 levels is observed in the M14 parental cell line following treatment with increasing concentrations of AZ628. AZ628-resistant clones express elevated CRAF. Elevated CRAF expression is a potential mechanism of acquired resistance to continuous AZ628 exposure, resulting in sustained activation of ERK1/2. p-ERK1/2 activity is not significantly inhibited by exposure to AZ628 in one of these three AZ628-insensitive cell lines (Wm1552C). Unlike in the AZ628-resistant M14 cells in which AZ628 fails to suppress the activation of ERK, AZ628 treatment efficiently attenuates ERK activation in the NRAS mutant melanoma cells.[2]
In vivo試験

プロトコル (参考用のみ)

細胞アッセイ: [1]

細胞株 M14 expressing the V600E BRAF mutation
濃度 0.01-10 μM
反応時間 Overnight
実験の流れ Approximately 0.5-2.5 × 105 M14 cells are seeded in 12 or 24 - well plates, respectively, in medium supplemented with 5% FBS. After overnight incubation, the cells are treated with various concentrations of AZ628. Fresh medium and drug is replaced every 2 days until the untreated control wells reached confluence. At this time-point, the media is removed and the cells are fixed in 4% formaldehyde in PBS for 20 minutes at room temperature. Cells are then washed twice with PBS and stained with a 1:5000 solution of the fluorescent nucleic acid stain Syto60. Quantitation of fluorescent signal intensity is carried out at 700 nm, using an Odyssey Infrared Imager. Each experiment is performed in quadruplicate and the results shown represent the average of the four values compared to untreated wells. Error bars represent standard deviation of the 4 values from the mean. High-throughput cell growth/viability assays are performed.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)



Download AZ 628 SDF
分子量 451.52


CAS No. 878739-06-1
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 90 mg/mL (199.32 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 3-(2-cyanopropan-2-yl)-N-(4-methyl-3-(3-methyl-4-oxo-3,4-dihydroquinazolin-6-ylamino)phenyl)benzamide

カスタマーフィードバック (2)

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Source Cancer Discov, 2013, 3(3), 350-62. AZ 628 purchased from Selleck
Method Immunoblotting
Cell Lines U2OS cells
Concentrations 0.2 uM
Incubation Time 16 h
Results Moreover, ERK phosphorylation was effectively suppressed (between 80–90%) by AZ628, even in the setting of NF1 knockdown but only by 65% in the presence of oncogenic KRAS.

Click to enlarge
Source Cell Death Dis, 2014, 5, e1278. AZ 628 purchased from Selleck
Method luminescent RIP3 assay
Cell Lines U2OS cells
Concentrations 0-100 uM
Incubation Time
Results The result showed that the six tested B-Raf inhibitors (dabrafenib, AZ628) inhibited the RIP3 activity with IC50s ranging from 0.25 to 14.52 uM.

文献中の引用 (5)



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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID