Skip to the beginning of the images gallery

Dovitinib lactate - 99%, high purity , CAS No.692737-80-7

COA

Grade & Purity:

≥99%

Cas Number: 692737-80-7
Molecular Weight: 482.52
PubChem CID: 135431668

In stock

Item Number

D651722

Grouped product items
SKU	Size	Availability	Price
D651722-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$60.90
D651722-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$96.90
D651722-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$288.90
D651722-100mg	100mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$480.90
D651722-200mg	200mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$840.90
D651722-500mg	500mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,560.90

View related series

c-Kit (81) FGFR (112) FLT3 (103) PDGFR (109) Protein Tyrosine Kinase/RTK (1314) Receptor Tyrosine Kinase (1260) VEGFR (187)

Basic Description

Synonyms	BCP04112 \| Triptorelin (USAN/INN) \| TKI258 \| 4-AMINO-5-FLUORO-3-(6-(4-METHYLPIPERAZIN-1-YL)-1H-BENZO-[D]IMIDAZOL-2-YL)QUINOLIN-2(1H)-ONE 2-HYDROXYPROPANOATE \| 4-Amino-5-fluoro-3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one 2-hyd
Specifications & Purity	≥99%
Biochemical and Physiological Mechanisms	Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC 50 s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3 , c-Kit , FGFR1/3 , VEGFR1/2/3 and PDGFRα/β , respectively.
Storage Temp	Store at 2-8°C,Desiccated
Shipped In	Wet ice This product requires cold chain shipping. Ground and other economy services are not available.
Product Description	Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC 50 s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3 , c-Kit , FGFR1/3 , VEGFR1/2/3 and PDGFRα/β , respectively In Vitro Dovitinib potently inhibits the FGF-stimulated growth of WT and F384L-FGFR3-expressing B9 cells with IC 50 values of 25 nM. B9-MINV cells are resistant to the inhibitory activity of Dovitinib at concentrations up to 1 μM. Dovitinib inhibits cell proliferation of KMS11 (FGFR3-Y373C), OPM2 (FGFR3-K650E), and KMS18 (FGFR3-G384D) cells with IC 50 of values of 90 nM (KMS11 and OPM2) and 550 nM, respectively. Treatment of SK-HEP1 cells with dovitinib results in G2/M cell cycle arrest, inhibition of colony formation in soft agar and blockade of bFGF-induced cell migration. Dovitinib inhibits basal expression and FGF-induced phosphorylation of FGFR-1, FRS2-α and ERK1/2. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Dovitinib (10 mg/kg, 30 mg/kg, 60 mg/kg, p.o.) shows significant antitumor effect in the KMS11-bearing mice model, and the growth inhibition is 48%, 78.5%, and 94% in the 10 mg/kg, 30 mg/kg, and 60 mg/kg treatment arms, respectively, compared with the placebo-treated mice . Dovitinib demonstrates significant antitumor and antimetastatic activities in HCC xenograft models. Dovitinib potently inhibits tumor growth of six HCC lines. Inhibition of angiogenesis correlates with inactivation of FGFR/PDGFR-β/VEGFR-2 signaling pathways. Dovitinib also causes dephosphorylation of retinoblastoma, upregulation of p-histone H2A-X and p27, and downregulation of p-cdk-2 and cyclin B1, which results in a reduction in cellular proliferation and the induction of tumor cell apoptosis. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Assay To determine IC 50 for SK-HEP1 cells, cells are plated at a density of 2×10 4 cells per dish. After 48 h, cells are treated with 0, 0.01, 0.1, 1, 5, 10, 50, 100 μM dovitinib in DMEM containing 1% FBS for 24 h. Cell viability is determined with Cell Proliferation Assay. IC 50 is calculated by nonlinear regression analysis using GraphPad Prism software. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal administration Mice: Six HCC lines (06-0606, 26-0808A, 26-1004, 25-0705A, 5-1318, 21-0208) are used to establish tumors in male SCID mice. or dose-esponse experiments, mice bearing the 06-0606 xenografts re orally given vehicle (5% dextrose) or two doses of dovitinib (50 and 75 mg/kg) daily for 14 days. For time-dependent inhibition of dovitinib targets, mice bearing 06-0606 tumors are given orally 200 μL of either vehicle (n=6) or 50 mg/kg/day of dovitinib (n=10) . aladdin has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:FLT3 1 nM (IC 50 ) c-Kit 2 nM (IC 50 ) FGFR1 8 nM (IC 50 ) FGFR3 9 nM (IC 50 ) VEGFR1 1 nM (IC 50 ) VEGFR3 8 nM (IC 50 ) VEGFR2 13 nM (IC 50 ) PDGFRα 27 nM (IC 50 ) PDGFRβ 210 nM (IC 50 )

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
- Superclass Organoheterocyclic compounds
  - Class Diazinanes
    - Subclass Piperazines

Kingdom	Organic compounds
Superclass	Organoheterocyclic compounds
Class	Diazinanes
Subclass	Piperazines
Intermediate Tree Nodes	Not available
Direct Parent	N-arylpiperazines
Alternative Parents	Hydroquinolones Haloquinolines 4-aminoquinolines Hydroquinolines Benzimidazoles Dialkylarylamines Pyridinones N-methylpiperazines Aminopyridines and derivatives Benzenoids Aryl fluorides Alpha hydroxy acids and derivatives Vinylogous amides Imidazoles Heteroaromatic compounds Trialkylamines Secondary alcohols Lactams Monocarboxylic acids and derivatives Carboxylic acids Azacyclic compounds Primary amines Organopnictogen compounds Organofluorides Organic oxides Hydrocarbon derivatives Carbonyl compounds
Molecular Framework	Not available
Substituents	N-arylpiperazine - 4-aminoquinoline - Haloquinoline - Dihydroquinolone - Aminoquinoline - Quinoline - Dihydroquinoline - Benzimidazole - Dialkylarylamine - Tertiary aliphatic/aromatic amine - N-alkylpiperazine - N-methylpiperazine - Pyridinone - Aminopyridine - Benzenoid - Pyridine - Hydroxy acid - Aryl halide - Aryl fluoride - Alpha-hydroxy acid - Heteroaromatic compound - Vinylogous amide - Imidazole - Azole - Tertiary aliphatic amine - Tertiary amine - Secondary alcohol - Lactam - Azacycle - Monocarboxylic acid or derivatives - Carboxylic acid - Carboxylic acid derivative - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Primary amine - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Carbonyl group - Amine - Alcohol - Aromatic heteropolycyclic compound
Description	This compound belongs to the class of organic compounds known as n-arylpiperazines. These are organic compounds containing a piperazine ring where the nitrogen ring atom carries an aryl group.
External Descriptors	Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61. DOI: 10.1186/s13321-016-0174-y

Names and Identifiers

IUPAC Name	4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one;2-hydroxypropanoic acid
INCHI	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)
InChIKey	ZRHDKBOBHHFLBW-UHFFFAOYSA-N
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
Isomeric 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
PubChem CID	135431668
Molecular Weight	482.52

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	DMSO : ≥ 30 mg/mL (62.17 mM)
Molecular Weight	482.500 g/mol
XLogP3
Hydrogen Bond Donor Count	5
Hydrogen Bond Acceptor Count	9
Rotatable Bond Count	3
Exact Mass	482.208 Da
Monoisotopic Mass	482.208 Da
Topological Polar Surface Area	148.000 Å²
Heavy Atom Count	35
Formal Charge	0
Complexity	737.000
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	1
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
The total count of all stereochemical bonds	0
Covalently-Bonded Unit Count	2

Solution Calculators

Molarity Calculator

Determine the necessary mass, volume, or concentration for preparing a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions, always use the batch-specific molecular weight of the product found on the vial label and the Certificate of Analysis (available online).

Dilution Calculator

Determine the dilution needed to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator enables you to quickly determine the volume of a reagent needed to reconstitute your vial. Just enter the mass of the reagent and the target concentration, and the calculator will do the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration