DOVITINIB (TKI-258, CHIR-258) DOVITINIB
Dovitinib
CAS: 405169-16-6
Molecular Formula: C21H21FN6O
DOVITINIB (TKI-258, CHIR-258) DOVITINIB - Names and Identifiers
DOVITINIB (TKI-258, CHIR-258) DOVITINIB - Physico-chemical Properties
| Molecular Formula | C21H21FN6O |
| Molar Mass | 392.43 |
| Density | 1.386 |
| Solubility | Soluble in DMSO (up to 30 mg/ml). |
| Appearance | solid |
| Color | Yellow-green |
| pKa | 9.44±0.70(Predicted) |
| Storage Condition | -20° |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Use | Dovitinib (TKI-258, CHIR-258) is a multi-target RTK inhibitor, which has the strongest effect on type III (FLT3/c-Kit), IC50 is 1 nM/2 nM, and also acts on class IV (FGFR1/3) and class V (VEGFR1-4) RTKs,IC50 is 8-13 nM, but it has weak effect on InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2. |
| In vitro study | Dovitinib potently inhibits FGFR1/3 and VEFFR1-2 with an IC50 of 8-13 nM. Dovitinib had little effect on inhibition of InsR, EGFR, c-Met, EphrinA2, Tie2, IGFR1, and HER2. The growth of Dovitinib on FGF-stimulated wild-type B9 cells and F384L mutant B9 cells showed strong cytotoxicity with an IC50 of 25 nM. However, Dovitinib showed low cytotoxicity on MINV mutant B9 cells. Dovitinib inhibits the phosphorylation of downstream ERK1/2. When Dovitinib acts on MV4;11 (FLT-3 ITD mutant), it shows higher anti-malignant cell proliferation ability than when it acts on RS4;11 (FLT-3 wild type). On the other hand, Dovitinib also selectively inhibits the FGFR1 oncogene ligand 2-fgfr-positive KG1 and KG1A cell lines, which have the FGFR1 oncogene ligand 2-FGFR1 polymerizing gene. In addition, Dovitinib inhibits primary cell growth in 8p11 Myeloproliferative syndrome (EMS) patients. |
| In vivo study | In the KMS-11 transplantation mouse model, 60 mg Dovitinib per kilogram of mouse body weight led to the decline of FGFR3, resulting in a tumor growth inhibition rate of 94%. In SCID-NOD mice, Dovitinib showed potent anticancer activity against MV4;11 tumors. Dovitinib also effectively inhibits KMS-11 tumors that activate fgfr3. |
DOVITINIB (TKI-258, CHIR-258) DOVITINIB - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.548 ml | 12.741 ml | 25.482 ml |
| 5 mM | 0.51 ml | 2.548 ml | 5.096 ml |
| 10 mM | 0.255 ml | 1.274 ml | 2.548 ml |
| 5 mM | 0.051 ml | 0.255 ml | 0.51 ml |
Last Update：2024-01-02 23:10:35
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View History
DOVITINIB (TKI-258, CHIR-258) DOVITINIB
124569-76-2
L-ARGINYL-L-ARGININE 7-AMIDO-4-METHYLCOUMARIN TRIHYDROCHLORIDE
4-羟基-6-甲基-2-吡喃酮
4-氨基-2-硝基吡啶
2-Hydroxy-6-methylpyridine-3-boronic Acid
(2-METHYL-3-NITRO-PHENYL)-ACETYL CHLORIDE
Ethylene glycol, propylene glycol, isophthalic acid, tall oil fattyacids, pentaerythritol, glycerol polymer
2-(3-(三氟甲氧基)苯基)丙基-2-胺盐酸盐
2-氨基-4-噻唑乙酸乙酯
124569-76-2
L-ARGINYL-L-ARGININE 7-AMIDO-4-METHYLCOUMARIN TRIHYDROCHLORIDE
4-羟基-6-甲基-2-吡喃酮
4-氨基-2-硝基吡啶
2-Hydroxy-6-methylpyridine-3-boronic Acid
(2-METHYL-3-NITRO-PHENYL)-ACETYL CHLORIDE
Ethylene glycol, propylene glycol, isophthalic acid, tall oil fattyacids, pentaerythritol, glycerol polymer
2-(3-(三氟甲氧基)苯基)丙基-2-胺盐酸盐
2-氨基-4-噻唑乙酸乙酯