Dovitinib
CAS No. : 405169-16-6
(Synonyms: CHIR-258; TKI258)
| Size | Price | Stock |
|---|---|---|
| 5mg | $50 | In-stock |
| 10mg | $80 | In-stock |
| 25mg | $160 | In-stock |
| 50mg | $260 | In-stock |
| 100mg | $420 | In-stock |
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| Cat. No. : | HY-50905 |
| M.Wt: | 392.43 |
| Formula: | C21H21FN6O |
| Purity: | >98 % |
| Solubility: | DMSO : 23.33 mg/mL (ultrasonic;warming;heat to 60°C) |
Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity[1][2].
IC50 & Target: IC50: 1 nM (FLT3), 2 nM (c-Kit), 8 nM (FGFR1), 9 nM (FGFR3), 1 nM (VEGFR1), 13 nM (VEGFR2), 8 nM (VEGFR3), 27 nM (PDGFRα), 210 nM (PDGFRβ)[1]
In Vitro: Dovitinib (CHIR-258) shows more than 10-fold inhibition InsR (IC50=2 μM), EGFR1 (IC50=2 μM), c-Met (IC50>3 μM), EphrinA2 (EphA2; IC50=4 μM), Tie2 (IC50=4 μM), IGFR1 (IC50>10 μM), and HER2 (IC50>10 μM)[1].
Dovitinib (12.5-400 nM; 48 hours) potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC50 values of 25 nM[1].
Dovitinib (100, 500 nM; 96 hours) inhibits FGF-mediated ERK1/2 phosphorylation and induces apoptosis of FGFR3-expressing human myeloma cell lines[1].
Dovitinib (72 hours) inhibits cell proliferation of KMS11 (FGFR3-Y373C), OPM2 (FGFR3-K650E), and KMS18 (FGFR3-G384D) cells with IC50 of values of 90 nM (KMS11 and OPM2) and 550 nM, respectively[1].
Dovitinib (100 nM) augments Dexamethasone (0.5 μM) cytotoxicity in KMS11 cells[1].
Dovitinib significantly reduces the basal phosphorylation levels of FGFR-1, FGFR substrate 2α (FRS2-α) and ERK1/2 but not Akt in both SK-HEP1 and 21-0208 cells[2].
Dovitinib enhances the BMP-2-induced alkaline phosphatase (ALP) induction, which is a representative marker of osteoblast differentiation. Dovitinib also stimulates the translocation of phosphorylated Smad1/5/8 into the nucleus and phosphorylation of mitogen-activated protein kinases, including ERK1/2 and p38[3].
Dovitinib strongly inhibits both the interaction of TNIK with ATP (Ki, 13 nM) and the activation of Wnt signaling effectors such as β-catenin and TCF4. Dovitinib also induces caspase-dependent apoptosis in IM-9 cells without significant cytotoxicity in PBMCs[4].
In Vivo: Dovitinib (CHIR-258; 10-60 mg/kg/day; gavage; for 21 days) has a significant antitumor effect[1].
Dovitinib (50 and 75 mg/kg) results in 97% and 98% tumor growth inhibition, respectively, and the maximal efficacy is at 50 mg/kg[2].
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