Dovitinib (TKI258) LactateOral tyrosine kinase inhibitor (TKI) against FGFR1–3, VEGFR1–3, and platelet-derived growth factor receptor (PDGFR). CAS# 915769-50-5 |
- AZD4547
Catalog No.:BCC3711
CAS No.:1035270-39-3
- PD 173074
Catalog No.:BCC3662
CAS No.:219580-11-7
- TCS 359
Catalog No.:BCC1183
CAS No.:301305-73-7
- Sunitinib
Catalog No.:BCC4064
CAS No.:557795-19-4
- Amuvatinib (MP-470, HPK 56)
Catalog No.:BCC2258
CAS No.:850879-09-3
- TG101209
Catalog No.:BCC2198
CAS No.:936091-14-4
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 915769-50-5 | SDF | Download SDF |
| PubChem ID | 135611162 | Appearance | Powder |
| Formula | C24H27FN6O4 | M.Wt | 482.51 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | ≥168.2mg/ml in H2O | ||
| Chemical Name | 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one;2-hydroxypropanoic acid;hydrate | ||
| SMILES | 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.O | ||
| Standard InChIKey | QDPVYZNVVQQULH-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C21H21FN6O.C3H6O3.H2O/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);1H2 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
Dovitinib (TKI258) Lactate Dilution Calculator
Dovitinib (TKI258) Lactate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.0725 mL | 10.3625 mL | 20.725 mL | 41.4499 mL | 51.8124 mL |
| 5 mM | 0.4145 mL | 2.0725 mL | 4.145 mL | 8.29 mL | 10.3625 mL |
| 10 mM | 0.2072 mL | 1.0362 mL | 2.0725 mL | 4.145 mL | 5.1812 mL |
| 50 mM | 0.0414 mL | 0.2072 mL | 0.4145 mL | 0.829 mL | 1.0362 mL |
| 100 mM | 0.0207 mL | 0.1036 mL | 0.2072 mL | 0.4145 mL | 0.5181 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
Description:
IC50: ~10 nmol/L for FGFR1–3
Fibroblast growth factor receptor 1 (FGFR1) and FGFR2 amplifications are observed in approximately 10% of breast cancers and are related to poor outcomes. Dovitinib (TKI258) is an oral tyrosine kinase inhibitor (TKI) against FGFR1–3, VEGFR1–3, and platelet-derived growth factor receptor (PDGFR).
In vitro: Dovitinib decreased the concentrations of pFRS2 and pERK/MAPK in a dose-dependent manner in FGFR1 amplified and FGFR2 amplified cell lines. The IC50 for cell growth inhibition was 190 and 180 nmol/L in MDA-MB-134 and SUM52, respectively. Conversely, IC50 values were more than 2,000 nmol/L in the 11 breast cancer cell lines that had neither FGFR1 nor FGFR2 amplification [1].
In vivo: In vivo model (HBCx-2 breast cancer primary xenograft, with 8 FGFR1 gene copies), dovitinib prevented tumor growth at the 30 mg/kg dose and caused tumor regression at the 50 mg/kg dose. Similarly, dovitinib caused tumor regression in HBCx-3 xenografts when administered at a dose of 40 mg/kg daily until day 35 [1].
Clinical trial: Eighty-one patients were enrolled in the trial. Unconfirmed response or stable disease for over 6 months was observed in 5 and 1 patient(s) with FGFR1-amplified/HR-positive and FGFR1-nonamplified/HR-positive breast cancer. When qPCR-identified amplifications in FGFR1, FGFR2, or FGF3 were grouped to define an FGF pathway–amplified breast cancer in HR-positive patients, the mean reduction in target lesions was 21.1% compared with a 12.0% increase in patients that did not present with FGF pathway–amplified breast cancer [1].
Reference:
[1] André F, Bachelot T, Campone M, Dalenc F, Perez-Garcia JM, Hurvitz SA, Turner N, Rugo H, Smith JW, Deudon S, Shi M, Zhang Y, Kay A, Porta DG, Yovine A, Baselga J. Targeting FGFR with dovitinib (TKI258): preclinical and clinical data in breast cancer. Clin Cancer Res. 2013 Jul 1;19(13):3693-702.
- WAY 316606
Catalog No.:BCC2052
CAS No.:915759-45-4
- ABC294640
Catalog No.:BCC4192
CAS No.:915385-81-8
- Cot inhibitor-1
Catalog No.:BCC1496
CAS No.:915365-57-0
- Cot inhibitor-2
Catalog No.:BCC1497
CAS No.:915363-56-3
- Bakkenolide IIIa
Catalog No.:BCN7352
CAS No.:915289-60-0
- 3-[4-[(2-Chloro-5-iodophenyl)methyl]phenoxy]tetrahydro-furan
Catalog No.:BCC8601
CAS No.:915095-94-2
- MDV3100 (Enzalutamide)
Catalog No.:BCC1268
CAS No.:915087-33-1
- BEZ235 (NVP-BEZ235)
Catalog No.:BCC3655
CAS No.:915019-65-7
- Palomid 529
Catalog No.:BCC3905
CAS No.:914913-88-5
- INCB024360 analogue
Catalog No.:BCC1647
CAS No.:914471-09-3
- R788 disodium hexahydrate
Catalog No.:BCC5127
CAS No.:914295-16-2
- 9-Aminocamptothecin
Catalog No.:BCN2453
CAS No.:91421-43-1
- Momordicine I
Catalog No.:BCN3058
CAS No.:91590-76-0
- Benidipine HCl
Catalog No.:BCC4395
CAS No.:91599-74-5
- TCS 1102
Catalog No.:BCC4063
CAS No.:916141-36-1
- AC 55541
Catalog No.:BCC3951
CAS No.:916170-19-9
- Gopherenediol
Catalog No.:BCN6582
CAS No.:916236-79-8
- Acetylvirolin
Catalog No.:BCN7041
CAS No.:916264-22-7
- Clinodiside A
Catalog No.:BCN1048
CAS No.:916347-31-4
- Senkyunolide C
Catalog No.:BCC9141
CAS No.:91652-78-7
- Zingiberen newsaponin
Catalog No.:BCN2942
CAS No.:91653-50-8
- Coriatin
Catalog No.:BCN4457
CAS No.:91653-75-7
- Clematomandshurica saponin B
Catalog No.:BCN7810
CAS No.:916649-91-7
- Clematiunicinoside E
Catalog No.:BCN7809
CAS No.:916649-92-8
