Allitinib (AST-1306)

製品コードS2185 別名:AST-6

Allitinib (AST-1306)化学構造


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.

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  • 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.
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

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]

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?=


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]


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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]
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  • 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.
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  • 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

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
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。


分子量 621.08


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





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


  • 質量





開始濃度 x 開始体積 = 最終濃度 x 最終体積


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

  • C1



  • 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):




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


質量 濃度 体積 分子量



Handling Instructions


  • * 必須


EGFR Inhibitors with Unique Features


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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID