CS-69
Saracatinib
CAS: 379231-04-6
Molecular Formula: C27H32ClN5O5
CS-69 - Names and Identifiers
CS-69 - Physico-chemical Properties
| Molecular Formula | C27H32ClN5O5 |
| Molar Mass | 542.03 |
| Density | 1.348 |
| Melting Point | 84-89°C |
| Boling Point | 671.2±55.0 °C(Predicted) |
| Flash Point | 359.759°C |
| Solubility | Soluble in DMSO (50 mg/ml) and ethanol (54 mg/mL with warming) |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | solid |
| Color | White |
| pKa | 7.55±0.10(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| Refractive Index | 1.641 |
| Use | A diverse Src inhibitor. |
| In vitro study | Saracatinib also potently inhibits other Src tyrosine kinase family members, including c-Yes, Fyn, Lyn, Blk, Fgr, and Lck, with an IC50 of 4 to 10 nM. Saracatinib effectively inhibited SrcY530F mutated NIH 3T3 cells with an IC50 of 80 nM. In NBT-II bladder cancer cells, Saracatinib significantly blocked the invasion of HT1080 cells through the three-dimensional collagen matrix and completely inhibited EGF-induced cell dispersal. Saracatinib acts on DU145 and PC3 cells and effectively inhibits Src activation by inhibiting Y419 phosphorylation. Saracatinib inhibited the growth of prostate cancer cells including PC3, DU145, CWR22Rv1, and LNCaP, whereas Saracatinib showed low activity on LAPC-4, PZ-HPV7, and RWPE-1 cells. Saracatinib stops the cell cycle at the G1/S stage, but does not break caspase 3. Saracatinib also significantly inhibited the movement of DU145 and PC3 in The Boyden chamber. Saracatinib potently and persistently inhibits Akt and enhances the sensitivity of A549 and Calu-6 cells to radiation treatment. Saracatinib inhibits osteoblasts in activity, resorption, and composition. Saracatinib also reversibly blocked the movement of osteoblast precursors. |
| In vivo study | Saracatinib showed a strong tumor growth inhibition rate in Src3T3 allografts, and Saracatinib caused an appropriate delay in the growth of Calu-6, MDA-MB-231, AsPc-1 and BT474C xenografts. Saracatinib was treated with 25mg Saracatinib per kilogram of mouse body weight per day, and the results showed strong anticancer activity. |
CS-69 - Introduction
Saracatinib (AZD0530) is a potent Src inhibitor with an IC50 of 2.7 nM, which is also active against c-Yes, Fyn, Lyn, Blk, Fgr and Lck, etc., but has low activity against Abl and EGFR (L858R and L861Q). Phase 2/3.
Last Update：2022-10-16 17:24:59
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Product Name: Saracatinib (AZD0530) Visit Supplier Webpage Request for quotationCAS: 379231-04-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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Spot supply
Product Name: Saracatinib (AZD0530) Visit Supplier Webpage Request for quotationCAS: 379231-04-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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