AST-1306

Catalog No.S2185 Synonyms: AST-6

AST-1306 Chemical Structure

Molecular Weight(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.

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In DMSO USD 670 In stock
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USD 370 In stock
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1 Customer Review

  • 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.

    AST-1306 purchased from Selleck.

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Biological Activity

Description 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.
Targets
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
In vitro

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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A431 cells  MkHQVJJwdGmoZYLheIlwdiCjc4PhfS=> NX7tSW4zPzJiaB?= MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF2M{GgZ4VtdHNib4\ldk1mgHC{ZYPzbY5oKEWJRmKg[4Vv\SCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvOiEQvF2= NVSzdnFvOjJ{MkeyNVQ>
NCI-H1975 cells NHzoT4tRem:uaX\ldoF1cW:wIHHzd4F6 Mkf1O|IhcA>? NUnOW5BTSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNib4\ldk1mgHC{ZYPzbY5oKEWJRmKgcZV1[W62IHflcoUh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlch|ryP NVj4cpAyOjJ{MkeyNVQ>
A549 cells MXnQdo9tcW[ncnH0bY9vKGG|c3H5 NHy0O3M4OiCq MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNib4\ldk1mgHC{ZYPzbY5oKEWJRmKg[4Vv\SCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVYvQCEQvF2= M33UUFIzOjJ5MkG0

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Kinase Assay:[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.
Cell Research:[1]
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  • Cell lines: Calu-3 and A-549 cell lines
  • Concentrations: 0.001-1 μM
  • Incubation Time: 72 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Nude mice bearing SK-OV-3 xenograft tumors and SK-OV-3FVB-2/Nneu transgenic mouse
  • Formulation: 0.5% hydroxypropyl methylcellulose (HPMC), grinding with agate morta
  • Dosages: 25 mg/kg, 50 mg/kg and 100 mg/kg
  • Administration: p.o., twice daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 124 mg/mL (199.65 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
0.5% hydroxyethyl cellulose
30 mg/mL

* 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.

Chemical Information

Molecular Weight 621.08
Formula

C24H18ClFN4O2,C7H8O3S

CAS No. 1050500-29-2
Storage powder
Synonyms AST-6

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID