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NCE Biomedical Co.,Ltd. |
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- Allitinib
-
- $48.00
-
2026-07-27
- CAS:897383-62-9
- Purity: 99.89%
- Supply Ability: 10g
- Allitinib
-
- $48.00
-
2026-07-27
- CAS:897383-62-9
- Purity: 99.89%
- Supply Ability: 10g
- AST-1306
-
- $9.80
-
2020-01-13
- CAS:897383-62-9
- Min. Order: 1g
- Purity: ≥99%
- Supply Ability: 100kg
|
| | AST-1306 Basic information |
| Product Name: | AST-1306 | | Synonyms: | AST-1306;ALS 1306;N-[4-[[3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl]amino]quinazolin-6-yl]acrylamide;N-[4-[[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-6-quinazolinyl]-2-propenamide;Allitinib (AST1306);Allitinib;CS-590;N-(4-(4-(3-fluorobenzyloxy)-3-chlorophenylamino)quinazolin-6-yl)acrylamide | | CAS: | 897383-62-9 | | MF: | C24H18ClFN4O2 | | MW: | 448.88 | | EINECS: | | | Product Categories: | | | Mol File: | 897383-62-9.mol |  |
| | AST-1306 Chemical Properties |
| Boiling point | 655℃ | | density | 1.395 | | Fp | 350℃ | | storage temp. | Store at -20°C | | solubility | ≥22.45 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | | form | solid | | pka | 12.16±0.43(Predicted) | | color | White to off-white | | InChIKey | MVZGYPSXNDCANY-UHFFFAOYSA-N | | SMILES | C(NC1C=CC2C(C=1)=C(NC1=CC=C(OCC3=CC=CC(F)=C3)C(Cl)=C1)N=CN=2)(=O)C=C |
| | AST-1306 Usage And Synthesis |
| Uses | AST-1306 is a novel irreversible inhibitor of EGFR and ErbB4 with IC50 of 0.5 nM and 0.8 nM, respectively. | | Uses | AST-1306 is a selective irreversible inhibitor of the epidermal growth factor receptor (EGFR) 1 and 2. Studies show that AST-1306 inhibited the enzymatic activities of wild-type EGF) and ErbB2 as well
as EGFR resistant mutant in both cell-free and cell-based systems. AST-1306 was more effective in inhibiting tumors with ErbB2-overexpressing cells than EGFR-overexpressing tumor. | | Definition | ChEBI: N-[4-[3-chloro-4-[(3-fluorophenyl)methoxy]anilino]-6-quinazolinyl]-2-propenamide is a member of quinazolines. | | Biological Activity | ast1306 is a novel inhibitor of egfr and her2 (ic50 = 0.5 nm and 3 nm respectively)egfr (epidermal growth factor receptor) is a cell-surface receptor tyrosine kinase. the receptor activation leads to dimerization and tyrosine autophosphorylation. it induces a cascade of downstream cellular responses such as modification in gene expression, cell proliferation and cytoskeletal rearrangement etc. her2 is a member of the epidermal growth factor and is associated with breast and ovarian cancers.ast1306 selectively blocked egfr and her2 kinase activities in a cell-free assay. the tyrosine kinase activity of egfr mutant t790m/l858r was also inhibited by ast1306 in intact cell and cell-free assays. in addition, ast1306 attenuated the egfr and her2 phosphorylation and downstream substrates. [1]in erbb2-overexpressing xenograft and fvb-2/nneu transgenic mouse model, ast1306 potently inhibited tumor growth. in sk-ov-3 xenograft model, ast1306 caused a quick and long-lasting (≥24h) inhibition of egfr and her2. [1] | | in vivo | AST1306 (AST-1306; p.o.; 25-100 mg/kg; twice daily; for 28 days) causes a dramatic suppression of tumor growth in SK-OV-3 and Calu-3 xenograft models[1]. | Animal Model: | Nude mice with SK-OV-3 and Calu-3 tumors[1] | | Dosage: | 25, 50, 100 mg/kg | | Administration: | p.o; twice daily; for 28 days | | Result: | Caused a dramatic suppression of tumor growth.
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| | IC 50 | EGFR: 0.5 nM (IC50); EGFRL858R/T790M: 12 nM (IC50); ErbB2: 3 nM (IC50); ErbB4: 0.8 nM (IC50) | | references | 1. xie h, lin l, tong l et al. ast1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo. plos one. 2011;6(7):e21487. |
| | AST-1306 Preparation Products And Raw materials |
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