Dovitinib dilactic acid | CAS#852433-84-2 | VEGF kinase inhibitor

MedKoo Cat#: 581837 | Name: Dovitinib dilactic acid

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively.

Chemical Structure

Dovitinib dilactic acid

CAS#852433-84-2 (dilactic acid)

Theoretical Analysis

MedKoo Cat#: 581837

Name: Dovitinib dilactic acid

CAS#: 852433-84-2 (dilactic acid)

Chemical Formula: C24H27FN6O4

Exact Mass: 482.2078

Molecular Weight: 482.52

Elemental Analysis: C, 59.74; H, 5.64; F, 3.94; N, 17.42; O, 13.26

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 450.00	2 Weeks
25mg	USD 850.00	2 Weeks

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Related CAS #

915769-50-5 (lactate hydrate) 405169-16-6 (free base) 852433-84-2 (dilactic acid)

Synonym

TKI258; TKI-258; TKI 258; CHIR258; CHIR-258; CHIR 258; Dovitinib Dilactic acid;

IUPAC/Chemical Name

4-amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one bis(2-hydroxypropanoate)

InChi Key

XXLPVQZYQCGXOV-UHFFFAOYSA-N

InChi Code

InChI=1S/C21H21FN6O.2C3H6O3/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;2*1-2(4)3(5)6/h2-6,11H,7-10H2,1H3,(H,24,25)(H3,23,26,29);2*2,4H,1H3,(H,5,6)

SMILES Code

CC(C(=O)O)O.CC(C(=O)O)O.CN1CCN(CC1)C2=CC3=C(C=C2)N=C(N3)C4=C(C5=C(C=CC=C5F)NC4=O)N

Appearance

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

Shelf Life

>3 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

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor.

In vitro activity:

Treatment of CH157MN and IOMM-Lee cells with Dovitinib suppressed multiple angiokinases-mainly FGFRs, leading to suppression of downstream signaling by RAS-RAF-MAPK molecules and PI3K-AKT molecules which are involved in cell proliferation, cell survival, and tumor invasion. Furthermore, Dovitinib induced apoptosis via downregulation of survival proteins (Bcl-XL), and over-expression of apoptotic factors (Bax and caspase-3) regardless of CHEK2 and NF2 mutation status. Reference: Cancer Invest. 2020 Jul;38(6):349-355. https://pubmed.ncbi.nlm.nih.gov/32441531/

In vivo activity:

The effects of an FGFR inhibitor, dovitinib dilactic acid (TKI258) on tumor growth and tumor-induced bone changes were evaluated. Cancer-induced bone lesions were smaller in dovitinib-treated mice as evaluated by X-ray imaging. Peripheral quantitative computed tomography imaging showed higher total and cortical bone mineral content and cortical bone mineral density in dovitinib-treated mice, suggesting better preserved bone mass. Reference: J Bone Oncol. 2019 Mar 19;16:100232. https://pubmed.ncbi.nlm.nih.gov/30956945/

Preparing Stock Solutions

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:

1. Das A, Martinez Santos JL, Alshareef M, Porto GBF, Infinger LK, Vandergrift WA 3rd, Lindhorst SM, Varma AK, Patel SJ, Cachia D. In Vitro Effect of Dovitinib (TKI258), a Multi-Target Angiokinase Inhibitor on Aggressive Meningioma Cells. Cancer Invest. 2020 Jul;38(6):349-355. doi: 10.1080/07357907.2020.1773844. Epub 2020 Jun 8. PMID: 32441531. 2. AlRabiah H, Kadi AA, Aljohar HI, Attwa MW, Al-Shakliah NS, Attia SM, Mostafa GA. A New Validated HPLC-MS/MS Method for Quantification and Pharmacokinetic Evaluation of Dovitinib, a Multi-Kinase Inhibitor, in Mouse Plasma. Drug Des Devel Ther. 2020 Jan 28;14:407-415. doi: 10.2147/DDDT.S223573. PMID: 32095071; PMCID: PMC6995292. 3. Kähkönen TE, Tuomela JM, Grönroos TJ, Halleen JM, Ivaska KK, Härkönen PL. Dovitinib dilactic acid reduces tumor growth and tumor-induced bone changes in an experimental breast cancer bone growth model. J Bone Oncol. 2019 Mar 19;16:100232. doi: 10.1016/j.jbo.2019.100232. PMID: 30956945; PMCID: PMC6434100. 4. 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. PMID: 28342996; PMCID: PMC5369368.

In vitro protocol:

In vivo protocol:

1. Kähkönen TE, Tuomela JM, Grönroos TJ, Halleen JM, Ivaska KK, Härkönen PL. Dovitinib dilactic acid reduces tumor growth and tumor-induced bone changes in an experimental breast cancer bone growth model. J Bone Oncol. 2019 Mar 19;16:100232. doi: 10.1016/j.jbo.2019.100232. PMID: 30956945; PMCID: PMC6434100. 2. 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. PMID: 28342996; PMCID: PMC5369368.

1: Kähkönen TE, Tuomela JM, Grönroos TJ, Halleen JM, Ivaska KK, Härkönen PL. Dovitinib dilactic acid reduces tumor growth and tumor-induced bone changes in an experimental breast cancer bone growth model. J Bone Oncol. 2019 Mar 19;16:100232. doi: 10.1016/j.jbo.2019.100232. PMID: 30956945; PMCID: PMC6434100. 2: Sohn SH, Sul HJ, Kim B, Kim BJ, Kim HS, Zang DY. TRK inhibitors block NFKB and induce NRF2 in TRK fusion-positive colon cancer. J Cancer. 2021 Aug 28;12(21):6356-6362. doi: 10.7150/jca.60845. PMID: 34659525; PMCID: PMC8489125.