AST 1306 (p-Toluenesulfonic acid)
AST-1306 TsOH
CAS: 1050500-29-2
Molecular Formula: C31H26ClFN4O5S
AST 1306 (p-Toluenesulfonic acid) - Names and Identifiers
AST 1306 (p-Toluenesulfonic acid) - Physico-chemical Properties
| Molecular Formula | C31H26ClFN4O5S |
| Molar Mass | 621.0783432 |
| Solubility | Soluble in DMSO (124 mg/mL), water (<1 mg/mL), and ethanol (<1 mg/mL). |
| Storage Condition | 2-8℃ |
| Use | A potent and selective inhibitor of EGFR phosphorylation. |
| In vitro study | AST-1306 selective inhibition of EGFR and ErbB2 tyrosine kinase activity. AST-1306 also potently inhibited the T790M/L858R double mutant EGFR with an IC50 of 12 nM. AST-1306 the effect was more than 500 times higher than that of Lapatinib. Acting on ErbB family kinases AST-1306 is more than 3000-fold more selective than acting on other kinase families including PDGFR, KDR and c-Met. AST-1306 may be covalently bound to EGFR and ErbB2 amino acid residues. AST-1306 significantly inhibited the growth of HIH3T3-EGFR T790M/L858R cells in a concentration-dependent manner. AST-1306 effect on HIH3T3-EGFR T790M/L858R cells, effectively inhibit EGFR phosphorylation. Furthermore, AST-1306 inhibited the growth of NCI-H1975 of cells harboring the EGFR T790M/L858R mutation in a concentration-dependent manner. AST-1306 inhibit the phosphorylation of EGFR and its downstream pathway. Furthermore, AST-1306 significantly inhibited EGF-induced EGFR phosphorylation in A549 cells in a dose-dependent manner. AST-1306 acts on human cancer cells including A549 cells, Calu-3 cells and SK-OV-3 cells, and inhibits phosphorylation of EGFR and ErbB2 and their downstream signals. |
| In vivo study | AST-1306 daily oral treatment of SK-OV-3 and Calu-3 xenograft models significantly inhibited tumor growth. AST-1306 treatment SK-OV-3 model, 7 days later, the tumor almost completely disappeared. In contrast, AST-1306 inhibited tumor growth only slightly in HO-8910 and A549 xenografts. Therefore, AST-1306 acts on a tumor model overexpressing ErbB2, and the effect is much higher than that of a tumor expressing a low level of erbb2. AST-1306, the drug resistance was very good. Lapatinib has anti-cancer activity in a tumor model overexpressing ErbB2, but at the same dose and feeding arrangement, SK-OV-3 is more effective than Lapatinib in a AST-1306 transplanted tumor model. In addition, AST-1306 oral treatment FVB-2/N |
AST 1306 (p-Toluenesulfonic acid) - Introduction
AST-1306 is a new and irreversible EGFR and ErbB2 inhibitor. IC50 is 0.5 nM and 3 nM respectively. It is also effective for mutant EGFR T790M/L858R, and is more effective for cells overexpressing ErbB2. It is 3000 times more selective for ErbB family than for other kinases.
Last Update：2022-10-16 17:41:16
AST 1306 (p-Toluenesulfonic acid) - Reference Information
| Effect | Alitinib (AST-1306) is a structural analog of lapatinib, a new quinazoline anti-tumor drug, and a small molecule epidermal growth factor receptor tyrosine kinase inhibitor, which selectively acts on EGFR/ErbB2/ErbB4 receptors. Compared with the first substitute for Ni, ailitinib toluenesulfonate is an irreversible inhibitor of EGFR/ErbB2/ErbB4 triple tyrosine kinase, which is more effective than the first generation, and may be resistant to the first substitute for Ni. Patients produce curative effect. |
| anticancer drug | eritinib (AST-6) is a structural analog of lapatinib and is a new anti-tumor drug of quinazoline, which produces anti-tumor effect by inhibiting epidermal growth factor receptor tyrosine kinase. Alitinib is an innovative oral anti-tumor drug obtained by Alis's choice of epidermal growth factor receptor (EGFR, ErbB2) family and its signaling pathway as a target for anti-tumor drug development. Alitinib has highly effective tumor inhibitory activity and extremely high safety, and is intended to be used in the treatment of malignant solid tumors in clinical practice. Its comprehensive preclinical studies have shown that oral administration of eritinib is safe, its molecular mechanism of anti-tumor effect is clear, and it has a high degree of specificity and specificity. It has obvious inhibitory effects on EGFR/ErbB1 and ErbB2 tyrosine kinases, and has significant effects on ovarian cancer, breast cancer, non-small cell lung cancer and other solid malignant tumors. Its toxicity is far lower than that of traditional cytotoxic anti-tumor drugs, which can be taken orally and can be used for a long time. |
| drug effect | the drug selectively inhibits EGFR/ErbB2/ErbB4 receptor kinase at the molecular level, cell level and animal tests, has a strong anti-tumor growth effect, and has an effect on inhibiting the growth of T790M cells resistant to the first substitute. |
| biological activity | Allitinib (AST-1306, AST-6) is a new and irreversible EGFR and ErbB2 inhibitor with IC50 of 0.5 nM and 3 nM respectively. it is also effective for mutant EGFR T790M/L858R and is more effective for cells overexpressing ErbB2, the ErbB family is 3000 times more selective than other kinases. |
| target | TargetValue EGFR (Cell-Free Assay) 0.5 nM ErbB4 (Cell-Free Assay) 0.8 nM ErbB2 (Cell-Free Assay) 3.0 nM EGFR (T790M/L858R) (Cell-Free Assay) 12 nM |
| Target | Value |
| EGFR (Cell-free assay) | 0.5 nM |
| ErbB4 (Cell-free assay) | 0.8 nM |
| ErbB2 (Cell-free assay) | 3.0 nM |
| EGFR (T790M/L858R) (Cell-free assay) | 12 nM |
| in vitro study | AST-1306 selectively inhibit EGFR and ErbB2 tyrosine kinase activity. AST-1306 also effectively inhibited T790M/L858R double mutant EGFR with IC50 of 12 nM. The AST-1306 effect is more than 500 times higher than the Lapatinib. The selectivity of AST-1306 acting on ErbB family kinases is more than 3000 times higher than that of other kinase families including PDGFR, KDR and c-Met. AST-1306 may be covalently bound to EGFR and ErbB2 amino acid residues. AST-1306 significantly inhibited the growth of HIH3T3-EGFR T790M/L858R cells in a concentration-dependent manner. AST-1306 acts on HIH3T3-EGFR T790M/L858R cells and effectively inhibits EGFR phosphorylation. Moreover, AST-1306 inhibit the growth of NCI-H1975 cells containing EGFR T790M/L858R mutation, this effect is concentration-dependent. AST-1306 inhibits phosphorylation of EGFR and its downstream pathways. In addition, AST-1306 acts on A549 cells to significantly inhibit EGF-induced EGFR phosphorylation, which is dose-dependent. AST-1306 acts on human cancer cells including A549 cells, Calu-3 cells and SK-OV-3 cells, inhibiting EGFR and ErbB2 and their downstream signal phosphorylation. |
| in vivo study | AST-1306 treat SK-OV-3 and Calu-3 transplanted tumor models orally every day, significantly inhibiting tumor growth. After 7 days, the tumor almost completely disappeared after AST-1306 treatment of the SK-OV-3 model. On the contrary, AST-1306 act on HO-8910 and A549 transplanted tumors and only slightly inhibit tumor growth. Therefore, the effect of AST-1306 on tumor models that overexpress ErbB2 is much higher than that of tumors that express low levels of ErbB2. AST-1306 resistance is good. Lapatinib acting on tumor models overexpressing ErbB2 has anti-cancer activity, but acting on SK-OV-3 transplanted tumor models according to the same dose and feeding arrangement AST-1306 better than Lapatinib. In addition, AST-1306 oral treatment of FVB-2/N |
Last Update：2024-04-09 21:01:54
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Product Name: AST-1306 TsOH Visit Supplier Webpage Request for quotation
CAS: 1050500-29-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1050500-29-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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