WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H200760
CAS#: 915769-50-5 (lactate)
Description: Dovitinib, also known as TKI-258 or CHIR-258, is an orally bioavailable FGFR3 inhibitor, which strongly binds to fibroblast growth factor receptor 3 (FGFR3) and inhibits its phosphorylation, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell death. In addition, this agent may inhibit other members of the RTK superfamily, including the vascular endothelial growth factor receptor; fibroblast growth factor receptor 1; platelet-derived growth factor receptor type 3; FMS-like tyrosine kinase 3; stem cell factor receptor (c-KIT); and colony-stimulating factor receptor 1; this may result in an additional reduction in cellular proliferation and angiogenesis, and the induction of tumor cell apoptosis.
Hodoodo Cat#: H200760
Name: Dovitinib lactate
CAS#: 915769-50-5 (lactate)
Chemical Formula: C24H27FN6O4
Exact Mass: 0.00
Molecular Weight: 482.516
Elemental Analysis: C, 59.74; H, 5.64; F, 3.94; N, 17.42; O, 13.26
Related CAS #: 915769-50-5 (lactate) 405169-16-6 (free base)
Synonym: TKI258; TKI-258; TKI 258; CHIR258; CHIR-258; CHIR 258; Dovitinib lactate
IUPAC/Chemical Name: 4-Amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]-2(1H)-quinolinone 2-hydroxypropanoate
InChi Key: ZRHDKBOBHHFLBW-UHFFFAOYSA-N
InChi Code: InChI=1S/C21H21FN6O.C3H6O3/c1-27-7-9-28(10-8-27)12-5-6-14-16(11-12)25-20(24-14)18-19(23)17-13(22)3-2-4-15(17)26-21(18)29;1-2(4)3(5)6/h2-6,11H,7-10H2,1H3,(H,24,25)(H3,23,26,29);2,4H,1H3,(H,5,6)
SMILES Code: O=C1NC2=C(C(F)=CC=C2)C(N)=C1C3=NC4=CC=C(N5CCN(C)CC5)C=C4N3.CC(O)C(O)=O
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
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The following data is based on the product molecular weight 482.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
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9: Thanasupawat T, Natarajan S, Rommel A, Glogowska A, Bergen H, Krcek J, Pitz M, Beiko J, Krawitz S, Verma IM, Ghavami S, Klonisch T, Hombach-Klonisch S. Dovitinib enhances temozolomide efficacy in glioblastoma cells. Mol Oncol. 2017 Aug;11(8):1078-1098. doi: 10.1002/1878-0261.12076. Epub 2017 Jun 5. PubMed PMID: 28500786; PubMed Central PMCID: PMC5537714.
10: Lee Y, Jung JI, Park KY, Kim SA, Kim J. Synergistic inhibition effect of TNIK inhibitor KY-05009 and receptor tyrosine kinase inhibitor dovitinib on IL-6-induced proliferation and Wnt signaling pathway in human multiple myeloma cells. Oncotarget. 2017 Jun 20;8(25):41091-41101. doi: 10.18632/oncotarget.17056. PubMed PMID: 28467797; PubMed Central PMCID: PMC5522218.
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12: Dillon PM, Petroni GR, Horton BJ, Moskaluk CA, Fracasso PM, Douvas MG, Varhegyi N, Zaja-Milatovic S, Thomas CY. A Phase II Study of Dovitinib in Patients with Recurrent or Metastatic Adenoid Cystic Carcinoma. Clin Cancer Res. 2017 Aug 1;23(15):4138-4145. doi: 10.1158/1078-0432.CCR-16-2942. Epub 2017 Apr 4. PubMed PMID: 28377480; PubMed Central PMCID: PMC5540767.
13: Yadav SS, Li J, Stockert JA, Herzog B, O'Connor J, Garzon-Manco L, Parsons R, Tewari AK, Yadav KK. Induction of Neuroendocrine Differentiation in Prostate Cancer Cells by Dovitinib (TKI-258) and its Therapeutic Implications. Transl Oncol. 2017 Jun;10(3):357-366. doi: 10.1016/j.tranon.2017.01.011. Epub 2017 Mar 24. PubMed PMID: 28342996; PubMed Central PMCID: PMC5369368.
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18: Lim SH, Sun JM, Choi YL, Kim HR, Ahn S, Lee JY, Lee SH, Ahn JS, Park K, Kim JH, Cho BC, Ahn MJ. Efficacy and safety of dovitinib in pretreated patients with advanced squamous non-small cell lung cancer with FGFR1 amplification: A single-arm, phase 2 study. Cancer. 2016 Oct;122(19):3024-31. doi: 10.1002/cncr.30135. Epub 2016 Jun 17. PubMed PMID: 27315356.
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