Bosutinib
Cat.No:IB0740 Solarbio
CAS:380843-75-4
Molecular Formula:C26H29Cl2N5O3
Molecular Weight:530.45
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥99%
Appearance:White to yellow Solid
Qty:
Size:
{{cart_num}}
My Cart>
Small Molecule Compounds >
Inhibitors & Antagonists & Agonists >
Protein Tyrosine Kinase/PTK >
BosutinibCAS:380843-75-4
Molecular Formula:C26H29Cl2N5O3
Molecular Weight:530.45
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥99%
Appearance:White to yellow Solid
Qty:
Size:
CAS | 380843-75-4 |
Name | Bosutinib |
Molecular Formula | C26H29Cl2N5O3 |
Molecular Weight | 530.45 |
Solubility | Soluble in DMSO |
Purity | ≥99% |
Appearance | White to yellow Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC | EINECS 700-455-1 |
MDL | MFCD07367846 |
SMILES | CN1CCN(CC1)CCCOC2=C(C=C3C(NC4=CC(OC)=C(C=C4Cl)Cl)=C(C=NC3=C2)C#N)OC |
Target Point | Src;Abl |
Passage | Protein Tyrosine Kinase/RTK |
Background | Bosutinib is a dual inhibitor of Src/Abl. |
Biological Activity | Bosutinib(SKI-606) is a dual Src/Abl inhibitor with IC50s of 1.2 nM and 1 nM, respectively.[1] |
IC50 | Src: 1.2nM;Abl: 1nM[1] |
In Vitro | SKI-606(bosutinib),a selective Src family kinase inhibitor,on human cancer cells derived from breast cancer patients to assess its potential for breast cancer treatment. The results show that SKI-606 caused a decrease in cell motility and invasion of breast cancer cell lines with an IC50 of f250 nmol/L,which was also the IC50 for inhibition of cellular Src kinase activity in intact tumor cells. These changes were accompanied by an increase in cell-to-cell adhesion and membrane localization of B-catenin. Analysis of downstream effectors of Src revealed that SKI-606 inhibits the phosphorylation of focal adhesion kinase(FAK),proline-rich tyrosine kinase 2(Pyk2),and Crk-associated substrate(p130Cas),with an IC50 similar to inhibition of cellular Src kinase. SKI-606 inhibits signaling pathways involved in controlling tumor cell motility and invasion,suggesting that SKI-606 is a promising therapeutic for breast cancer.[2] SKI-606,a potent inhibitor of Src and Abl kinases. SKI-606 inhibited Src autophosphorylation with an IC(50)of approximately 0.25 micromol/L in HT29 cells. Phosphorylation of Tyr(925)of focal adhesion kinase,a Src substrate,was reduced by similar concentrations of inhibitor. [3] |
In Vivo | On oral administration to nude mice at the lowest efficacious dose,peak plasma concentrations of approximately 3 micromol/L,an oral bioavailability of 18%,and a t(1/2)of 8.6 hours were observed. SKI-606 was orally active in s.c. colon tumor xenograft models and caused substantial reductions in Src autophosphorylation on Tyr(418)in HT29 and Colo205 tumors. SKI-606 inhibited HT29 tumor growth on once daily administration,whereas twice daily administration was necessary to inhibit Colo205,HCT116,and DLD1 tumor growth. [3] |
Cell Experiment | Briefly,f5,000 cells were seeded in each well of a 96-well plate and allowed to adhere before the addition of 0.01% DMSO or 0.1,0.3,and 1 umol/L of SKI-606. After 2to 6 d of incubation at 37℃ in 5% CO2,MTS reagent was added to each well for 30 min and absorbance measured at 490 nm.[2] |
Animal Experiment | In HT29 xenograft studies,SKI-606 was given by oral gavage once daily to mice with tumors ranging from 200 to 300mg. A dose-dependent antitumor response was observed in those mice given doses of 25 to 150 mg/kg over a 21-day period(P < 0.003 in Student’s two-tailed t test in the group that received the 25 mg/kg/d). Although the once daily 25 mg/kg dose was not consistently active,the higher doses were reproducibly effective. No deaths occurred and no weight loss was observed in animals given SKI-606 at 150 mg/kg. [3] |
Data Literature Source | [1]. Boschelli DH,et al. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J Med Chem,2001,44(23),3965-3977. [2]. Vultur A,et al. SKI-606 (bosutinib),a novel Src kinase inhibitor,suppresses migration and invasion of human breast cancer cells. Mol Cancer Ther,2008,7(5),1185-1194. [3]. Golas JM,et al. SKI-606,a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models. Cancer Res,2005,65(12),5358-5364. |
Unit | Bottle |
Specification | 10mg 20mg 100mg |
Bosutinib是 Src/Abl 的双抑制剂。
Remark:These protocols are for reference only. Solarbio does not independently validate these methods.
Note:
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
Sorry, there is no more information.
Sorry, there is no more information.