Bosutinib(TINIBS )
Bosutinib
CAS: 380843-75-4
Molecular Formula: C26H29Cl2N5O3
Bosutinib(TINIBS ) - Names and Identifiers
| Name | Bosutinib |
| Synonyms | CS-311 Bsutinib Bosutinib Bosutinib(TINIBS ) SKI 606 - Bosutinib Bosutinib ( SKI-606 ) Bosutinib for research 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinoline-3-carbonitrile 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile 3-Quinolinecarbonitrile, 4-[(2,4-dichloro-5-Methoxyphenyl)aMino]-6-Methoxy-7-[3-(4-Methyl-1-piperazinyl)propoxy]- |
| CAS | 380843-75-4 |
| EINECS | 700-455-1 |
| InChI | InChI=1/C26H29Cl2N5O3/c1-32-6-8-33(9-7-32)5-4-10-36-25-13-21-18(11-24(25)35-3)26(17(15-29)16-30-21)31-22-14-23(34-2)20(28)12-19(22)27/h11-14,16H,4-10H2,1-3H3,(H,30,31) |
| InChIKey | PICKMQXYAMDEPF-UHFFFAOYSA-N |
Bosutinib(TINIBS ) - Physico-chemical Properties
| Molecular Formula | C26H29Cl2N5O3 |
| Molar Mass | 530.45 |
| Density | 1.36 |
| Melting Point | 116-120 ºC |
| Boling Point | 649.7±55.0 °C(Predicted) |
| Flash Point | 346.7°C |
| Solubility | Soluble in DMSO, not in water |
| Vapor Presure | 0-0Pa at 20℃ |
| Appearance | Solid |
| Color | off-white to light brown |
| pKa | 7.63±0.10(Predicted) |
| Storage Condition | room temp |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| Refractive Index | 1.651 |
| In vitro study | Bosutinib has a higher selectivity for Src than non-Src family kinases, with an IC50 of 1.2 nM, and effectively inhibits Src-dependent cell proliferation, with an IC50 of 100 nM. Bosutinib significantly inhibited the proliferation of Bcr-Abl-positive leukemia cell lines KU812, K562, and MEG-01 but not Molt-4, HL-60, Ramos, and other leukemia cell lines, with IC50 of 5 nM, 20 nM, respectively, and 20 nM, more effective than STI-571. Similar to STI-571, Bosutinib acts on Abl-MLV transforming fibers and has proliferative activity with an IC50 of 90 nM. At concentrations of 50 nM, 10-25 nM, and 200 nM, respectively, Bosutinib excised Bcr-Abl and STAT5 in CML cells and v-Abl tyrosine phosphorylation expressed in fibers, this results in inhibition of phosphorylation of Bcr-Abl downstream signaling Lyn/Hck. Although it can not inhibit the proliferation and survival of breast cancer cells, it can significantly reduce the movement and invasion of breast cancer cells, IC50 is 250 nM, and improve the intercellular adhesion and membrane localization of β-catenin. |
| In vivo study | Bosutinib was effective in nude mice bearing Src-transformed fiber xenografts and HT29 xenografts at a dose of 60 mg/kg per day, with T/C values of 18% and 30%, respectively. Oral administration of Bosutinib to mice for 5 days significantly inhibited the growth of K562 tumors in a dose-dependent manner. Large tumors were eradicated at a dose of 100 mg/kg, treatment at a dose of 150 mg/kg removed tumors with no toxicity. Compared with the effect on HT29 transplanted tumor, Bosutinib at a dose of 75 mg/kg, twice a day, could inhibit tumor growth in nude mice bearing Colo205 transplanted tumor, there was no higher effect after increasing the dose, but the 50 mg/kg dose had no effect. |
Bosutinib(TINIBS ) - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36 - Irritating to the eyes |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
| WGK Germany | 3 |
| HS Code | 29335990 |
Bosutinib(TINIBS ) - Introduction
Bosutinib is a double inhibitor of Src/Abl with IC50 of 1.2 nM and 1 nM, respectively.
Last Update：2022-10-16 17:25:00
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Email: r@reformchem.com
Mobile: +86-17551318830
QQ: 3785839865
Product Name: Bosutinib Request for quotation
CAS: 380843-75-4
Tel: 17505222756
Email: pules.cn@gmail.com
Mobile: +86-17551318830
Wechat: 17505222756
CAS: 380843-75-4
Tel: 17505222756
Email: pules.cn@gmail.com
Mobile: +86-17551318830
Wechat: 17505222756
Multiple SpecificationsSpot supply
Product Name: Bosutinib Visit Supplier Webpage Request for quotationCAS: 380843-75-4
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: Bosutinib (SKI-606) Visit Supplier Webpage Request for quotationCAS: 380843-75-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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