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Purity: ≥98%
Bosutinib (formerly also known as SKI-606; trade name Bosulif) is a novel, quinolone-based, and potent dual Src/Abl kinase inhibitor with potential antitumor activity. It inhibits Src and Abl with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib was approved by the US FDA and EU European Medicines Agency on September 4, 2012 and 27 March 2013 respectively for treating Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) in adult patients.
| ln Vitro |
Bosutinib (SKI-606), with IC50 values in the low nanomolar range, is an effective inhibitor of Bcr-Abl in a number of chronic myelogenous leukemia cell lines[2].
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| ln Vivo |
In nude mice, busutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) has anti-human KU812 xenograft action. Against syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts, bosutinib (150 mg/kg; once day, five days weekly) has activity[2].
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: The leukemic Bcr-Abl+ cell lines (KCL22, K562, KU812, and Lama84) Tested Concentrations: 0.1 μmol/L Incubation Duration: 72 h Experimental Results: Inhibited several human CML derived cell lines with IC50 values ranging from 1 to 20 nmol/L |
| Animal Protocol |
Animal/Disease Models: KU812CM L xenograft model[2]
Doses: 75 mg/kg twice (two times) daily or 150 mg/kg one time/day Route of Administration: Bosutinib (po (oral gavage); 75 mg/kg twice (two times) daily or 150 mg/kg one time/day) Experimental Results: Had the therapeutic activity and produced a dose- and schedule-dependent weight loss. Animal/Disease Models: Syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts[2] Doses: 150 mg/kg Route of Administration: Bosutinib (150 mg/kg; one time/day, 5 days weekly) Experimental Results: diminished the rate of tumor growth and prolonged event-free survival of mice. |
| References |
[1]. Jorge E Cortes, et al. Bosutinib versus imatinib in newly diagnosed chronic-phase chronic myeloid leukemia: results from the BELA trial. J Clin Oncol. 2012 Oct 1;30(28):3486-92.
[2]. Miriam Puttini, et al. In vitro and in vivo activity of SKI-606, a novel Src-Abl inhibitor, against imatinib-resistant Bcr-Abl+ neoplastic cells. Cancer Res. 2006 Dec 1;66(23):11314-22. |
| Molecular Formula |
C26H29CL2N5O3
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|---|---|
| Molecular Weight |
530.45
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| CAS # |
380843-75-4
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| Related CAS # |
Bosutinib hydrate;918639-08-4;Bosutinib-d8;Bosutinib isomer;1391063-17-4
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| SMILES |
N#CC1=C(NC2=CC(OC)=C(Cl)C=C2Cl)C3=CC(OC)=C(OCCCN4CCN(C)CC4)C=C3N=C1
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| InChi Key |
UBPYILGKFZZVDX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/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)
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| Chemical Name |
4-(2,4-dichloro-5-methoxyphenylamino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile
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| Synonyms |
Bosutinib; SKI606; SKI 606; SK-I606; trade name: Bosulif.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8852 mL | 9.4260 mL | 18.8519 mL | |
| 5 mM | 0.3770 mL | 1.8852 mL | 3.7704 mL | |
| 10 mM | 0.1885 mL | 0.9426 mL | 1.8852 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
SKI-606 is a potent inhibitor of CML cell proliferation and survival.Cancer Res.2003 Jan 15;63(2):375-81. |
SKI-606 inhibits tyrosine phosphorylation of cellular proteins and Bcr-Abl in CML cells.Cancer Res.2003 Jan 15;63(2):375-81. |
SKI-606 is an Abl kinase inhibitor.Cancer Res.2003 Jan 15;63(2):375-81. |
Comparison of inhibition of Bcr-Abl tyrosine phosphorylation and v-Abl phosphorylation by SKI-606.Cancer Res.2003 Jan 15;63(2):375-81. |
SKI-606 inhibits downstream signaling from Bcr-Abl.Cancer Res.2003 Jan 15;63(2):375-81. |
SKI-606 reduces phosphorylation of Tyr397 in Lyn.Cancer Res.2003 Jan 15;63(2):375-81. |
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