Allitinib (AST-1306)

製品コードS2185 別名:AST-6

Allitinib (AST-1306)化学構造

分子量(MW):621.08

AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.

サイズ 価格(税別)  
JPY 111220.00
JPY 44820.00
JPY 61420.00

カスタマーフィードバック(1)

  • Reversal effect of AST-1306 on the sensitivity of NCI-H460/MX20 cells to mitoxantrone. The figure showes the survival curves of cells at different concentrations of mitoxantrone with or without AST-1306. Cell viability was determined by MTT Assay. NCI-H460 is lung cancer cell line while NCI-H460/MX20 is ABCG2 overexpressing drug (mitoxantrone) selected cell line.

    Allitinib (AST-1306) purchased from Selleck.

製品安全説明書

EGFR阻害剤の選択性比較

生物活性

製品説明 AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.
ターゲット
EGFR [1]
(Cell-free assay)
ErbB4 [1]
(Cell-free assay)
ErbB2 [1]
(Cell-free assay)
EGFR (T790M/L858R) [1]
(Cell-free assay)
0.5 nM 0.8 nM 3.0 nM 12 nM
体外試験

AST-1306 also ErB2 and EGFR T790M/L858R double mutant. AST-1306 is approximately 500-fold more potent than lapatinib and more than 3000-fold selective for ErbB family kinases over other kinase families including PDGFR, KDR and c-Met. AST-1306 might covalently bind to specific amino acid residues of EGFR and ErbB2. AST-1306 acts in a concentration dependent manner to significantly inhibit the growth of HIH3T3-EGFR T790M/L858R cells. AST-1306 effectively suppresses EGFR phosphorylation in HIH3T3-EGFR T790M/L858R cells. Moreover, AST-1306 blocks the growth of NCI-H1975 cells that harbor the EGFR T790M/L858R mutation in a concentration-dependent manner. AST-1306 blocks phosphorylation of EGFR and downstream pathways as well. In addition, AST-1306 dose-dependently and markedly inhibits EGF-induced EGFR phosphorylation in A549 cells. AST-1306 inhibits the phosphorylation of EGFR and ErbB2, and downstream signaling in human cancer cells including A549 cells, Calu-3 cells and SK-OV-3 cells. [1]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A431 cells  MlXFVJJwdGmoZYLheIlwdiCjc4PhfS=> NV7qRY5NPzJiaB?= MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF2M{GgZ4VtdHNib4\ldk1mgHC{ZYPzbY5oKEWJRmKg[4Vv\SCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvOiEQvF2= NFyxWFAzOjJ{N{KxOC=>
NCI-H1975 cells MVTQdo9tcW[ncnH0bY9vKGG|c3H5 NFzHelE4OiCq NVexTnVXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNib4\ldk1mgHC{ZYPzbY5oKEWJRmKgcZV1[W62IHflcoUh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlch|ryP MlTxNlIzOjd{MUS=
A549 cells NX3NXHpjWHKxbHnm[ZJifGmxbjDhd5NigQ>? MoLpO|IhcA>? NXK1dVhZSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJI93\XJvZYjwdoV{e2mwZzDFS2ZTKGenbnWgZYZ1\XJiN{KgbJJ{KGK7IGPSRkBie3OjeTygTWM2OD14Lkig{txO MXeyNlIzPzJzNB?=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 Twice daily oral administration of AST-1306 gives rise to a dramatic prevention of tumor growth in SK-OV-3 and Calu-3 xenograft models. In SK-OV-3 models, tumors nearly disappears after treatment with AST-1306 for 7 days. In contrast, AST-1306 only slightly inhibits the growth of tumor in HO-8910 and A549 xenograft models. Therefore, the antitumor efficacy of AST-1306 is greater in ErbB2-overexpressing tumor models than in models expressing low levels of ErbB2. AST-1306 is well tolerated. Lapatinib displays antitumor activity in these ErbB2-overexpressing tumor models, but AST-1306 is more efficacious than lapatinib in the SK-OV-3 xenograft tumor model when given at the same dose and schedule. In addition, oral administration of AST-1306 twice daily for 3 weeks dramatically suppresses the growth of tumor in the FVB-2/Nneu models. After treatment for 11 days, tumors almost completely disappears. The body weights of the mice reduces by less than 20% during treatment. [1]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

Tyrosine kinase assays:

The tyrosine kinase activities are determined in 96-well ELISA plates precoated with 20 μg/mL Poly (Glu,Tyr)4:1. First, 80 μL of 5 μM ATP solution diluted in kinase reaction buffer (50 mM HEPES pH 7.4, 20 mM MgCl2, 0.1 mM MnCl2, 0.2 mM Na3VO4, 1 mM DTT) is added to each well. Various concentrations of AST-1306 diluted in 10 μL of 1% DMSO (v/v) are then added to each reaction well, with 1% DMSO (v/v) used as the negative control. Subsequently, the kinase reaction is initiated by the addition of purified tyrosine kinase proteins diluted in 10 μL of kinase reaction buffer solution. Experiments at each concentration are performed in duplicate. After incubation for 60 min at 37 °C, the plate is washed three times with phosphate buffered saline (PBS) containing 0.1% Tween 20 (T-PBS). Next, 100 μL anti-phosphotyrosine antibody (PY99, 1:500 dilution) diluted in T-PBS containing 5 mg/mL BSA is added. After 30 min incubation at 37 °C, the plate is washed three times as before. Horseradish peroxidase-conjugated goat anti-mouse IgG (100 μL) diluted 1:2000 in T-PBS containing 5 mg/mL BSA is added. The plate is reincubated at 37 °C for 30 min, and then washed with PBS. Finally, 100 μL of a solution containing 0.03 % H2O2 and 2 mg/mL o-phenylenediamine in 0.1 M citrate buffer, pH 5.5, is added and samples are incubated at room temperature until color emerged. The reaction is terminated by the addition of 50 μL of 2 M H2SO4, and the plate is read using a multi-well spectrophotometer at 490 nm. The inhibition rate (%) is calculated using the following equation: [1-(A490 treated /A490 control)] ×100%. IC50 values are determined from the results of at least three independent tests and calculated by Logit method.
細胞試験: [1]
+ 展開
  • 細胞株: Calu-3 and A-549 cell lines
  • 濃度: 0.001-1 μM
  • 反応時間: 72 hours
  • 実験の流れ: Cell (including Calu-3, A-549 cell line et al.) proliferation is evaluated using the SRB (Sulforhodamine B) assay. Briefly, cells are seeded into 96-well plates and grown for 24 hours. The cells are then treated with increasing concentrations of AST-1306 and grown for a further 72 hours. The medium remains unchanged until the completion of the experiment. The cells are then fixed with 10% precooled trichloroacetic acid (TCA) for 1 hour at 4 °C and stained for 15 min at room temperature with 100 μL of 4 mg/mL SRB solution in 1% acetic acid. The SRB is then removed, and the cells are quickly rinsed five times with 1% acetic acid. After cells are air-dried, protein-bound dye is dissolved in 150 μL of 10 mM Tris base for 5 min and measured at 515 nm using a multiwell spectrophotometer. The inhibition rate on cell proliferation is calculated as (1 - A515 treated/A515 control) × 100%. The IC50 value is obtained by the Logit method and is determined from the results of at least 3 independent tests.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: Nude mice bearing SK-OV-3 xenograft tumors and SK-OV-3FVB-2/Nneu transgenic mouse
  • 製剤: 0.5% hydroxypropyl methylcellulose (HPMC), grinding with agate morta
  • 投薬量: 25 mg/kg, 50 mg/kg and 100 mg/kg
  • 投与方法: p.o., twice daily
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 124 mg/mL (199.65 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
0.5% hydroxyethyl cellulose
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 621.08
化学式

C24H18ClFN4O2,C7H8O3S

CAS No. 1050500-29-2
保管
in solvent
別名 AST-6

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

EGFRシグナル伝達経路

EGFR Inhibitors with Unique Features

相関EGFR製品

Tags: Allitinib (AST-1306)を買う | Allitinib (AST-1306) ic50 | Allitinib (AST-1306)供給者 | Allitinib (AST-1306)を購入する | Allitinib (AST-1306)費用 | Allitinib (AST-1306)生産者 | オーダーAllitinib (AST-1306) | Allitinib (AST-1306)化学構造 | Allitinib (AST-1306)分子量 | Allitinib (AST-1306)代理店
×

大阪市内で「G20サミット」が開催されることに伴い、大阪府内で大規模な交通規制が行われる影響で、6月26日(水)から7月1日(月)までの間、下記地域へ出荷が行えなくなります。
対象地域
大阪府(全域)、兵庫県(芦屋市、尼崎市、伊丹市、西宮市)
上記地域より西の地域につきましては納期の遅延が予想されます。
また、国際便も遅延が予想されているため国内在庫がない製品の納期が一週間程度遅れる可能性がございます。
ご不便をおかけいたしますが、宜しくお願い申し上げます。

×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID