Home
Services
Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassay Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
Polymers & Contract Manufacturing
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services
Products
Small Molecule Inhibitors and Antagonist
Bioactive Compounds and Agonist
Primary Antibodies
Catalog Peptides
Amino Acids Derivatives
Reagents
Fluorescent dyes
Intermediates
PCR
Proteasomes and Enzymes
Enzyme substrate
Nucleotides
Promotions
Customer Support
About Us
Site Map
Contact Us
Small Molecule Inhibitors and Antagonist
Anti-virus
Cell Cycle
DMPK/Tox
Endocrinology
Epigenetics
GPCR/G-protein
Mitogen-activated Protein Kinases (MAPK)
PI3K/Akt/mTOR
Proteases/Proteasome
Protein Tyrosine Kinases (PTK)
Stem Cells
TGF-Beta/Smad
Transporter
Others
Cat. No. Name Size Price Add Cart
KI0437Dovitinib Dilactic acid (TKI258 Dilactic acid)10 mg$272
Dovitinib Dilactic acid (TKI258 Dilactic acid)25 mg$432
Dovitinib Dilactic acid (TKI258 Dilactic acid)50 mg$752

Chemical Characteristic

Product NameDovitinib Dilactic acid (TKI258 Dilactic acid)
SynonymsTKI258 dilactic acid, CHIR258
CAS No.852433-84-2
Molecular Weight 572.59
FormulaC21H21FN6O.2C3H6O3
Chemical Name(3Z)-4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1,3-dihydrobenzimidazol-2-ylidene]quinolin-2-one;2-hydroxypropanoic acid
SmilesC(=O)(C(C)O)O [nH]1c(=O)c(c(c2c(cccc12)F)N)c1nc2c([nH]1)cc(cc2)N1CCN(CC1)C C(=O)(C(C)O)O
Chemical Structure

Biological activities

Dovitinib is a highly potent inhibitor of vascular endothelial growth factor receptor (VEGFR) 1, VEGFR2, VEGFR3, platelet-derived growth factor receptor (PDGFR) β, and fibroblast growth factor growth (FGFR)1, FGFR2, and FGFR3 (fibroblast growth factor receptors 1, 2, and 3). Dovitinib potently inhibits FGFR3 with an IC50 of 5 nM. Dovitinib inhibits members of the class III receptor tyrosine kinases (RTKs) including FLT3, c-Kit, CSF-1R, and PDGFRα/β with IC50 values of 1 to 210 nM. Additionally, dovitinib potently prevents class IV (FGFR1 and 3) and class V (VEGFR1-4) RTKs with IC50 values of 8 to 13 nM.[1] Dovitinib inhibits PDGFRβ and FGFR 1, 2 with IC50 of 12, 8 and 40 nM, respectively.[2] Dovitinib sensitizes resistant hepatocellular carcinoma (HCC) cells to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)- and tigatuzumab-induced apoptosis. The combination of dovitinib and tigatuzumab restores the sensitivity of HCC cells to TRAIL- and tigatuzumab-induced apoptosis. Dovitinib down-regulates phospho-STAT3 (Tyr705) (p-STAT3) and subsequently decreases the protein levels of STAT3-regulated proteins, Mcl-1, survivin and cylcin D1, in TRAIL-treated HCC cells.[3] Dovitinib markedly suppresses ccRCC tumorgraft growth, resulting in a greater prevention of tumor growth than both sunitinib and sirolimus. Moreover, dovitinib prevents the development of paraneoplastic hypercalcemia in mice. Dovitinib is more effective than sunitinib or sirolimus in RCC tumorgrafts in mice. [4] The terminal elimination t1/2 of dovitinib in plasma in mice is ∼3 hours. Plasma dovitinib concentrations increases with dose across the dose range evaluated. Plasma Cmax values elevate from 163 ng/mL (10 mg/kg) to 742 ng/mL (30 mg/kg) to 1,560 ng/mL (100 mg/kg).[5]

Protocols

Dovitinib solution is formulated in water and is given orally on either daily.[5]

References

[1] Trudel S, et al. CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood. 2005, 105(7): 2941-2948.
[2] Wang X, et al. Population Pharmacokinetic/Pharmacodynamic Modeling to Assist Dosing Schedule Selection for Dovitinib. Clin Pharmacol. 2012.
[3] Chen KF, et al. Dovitinib sensitizes hepatocellular carcinoma cells to TRAIL and tigatuzumab, a novel anti-DR5 antibody, through SHP-1-dependent inhibition of STAT3. Biochem Pharmacol. 2012, 83(6): 769-777.
[4] Sivanand S, et al. A validated tumorgraft model reveals activity of dovitinib against renal cell carcinoma. Sci Transl Med. 2012, 4(137): 137ra75.
[5] Lee SH, et al. In vivo target modulation and biological activity of CHIR-258, a multitargeted growth factor receptor kinase inhibitor, in colon cancer models. Clin Cancer Res. 2005, 11(10): 3633-41.

Please click here to fill online order form, and we will make sure to supply you product with detail information. This process usually takes between 24 to 48 hours, depending on products stock avaliability. All inquires and subsequent projects are handled in the strictest confidence and will be backed by a confidentiality agreement if required.
KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
About
KareBayTM Biochem
Sitemap
Blog
Custom Services
Organic Synthesis
Peptide Synthesis
Antibody Production
Protein Expression
Bioconjugation Service
Immunoassry Service
Molecular Biology Services
Oligonucleotides Synthesis
RNA Synthesis Service
cGMP Peptide Synthesis Services
cGMP Organic Synthesis Services
Biochemical Products
Small Molecule Inhibitors
Bioactive Compounds
Primary Antibodies
Peptides
Amino Acids
Reagents
Fluorescent dyes
Intermediates
PCR
Contact Us
KareBayTM Biochem, Inc.
11 Deer Park Drive, Suite 102A
Monmouth Junction, NJ 08852
Telephone
: 732-823-1545

Fax
: 732-823-1349
product@karebaybio.com
service@karebaybio.com
support@karebaybio.com
Follow Us
Follow Karebay on LinkedinFollow IMAGING on Twitter Google+ Facebook