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Sunitinib

CAT: 0013-GTR19162010-04Size: 500 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19162010-04Size:500 mg
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Description
A multi-targeted RTK inhibitor that targets VEGFR2 (Flk-1) and PDGFRβ with Ki of 8 nM and 9 nM respectively; displays >10-fold higher selectivity over FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and Src; also inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM; regresses FLT3-ITD tumors in the subcutaneous tumor xenograft model.Gastric Cancer Approved (In Vitro) :Sunitinib Malate is also a good inhibitor of KIT and FLT-3. In RS4;11 cells (FLT3-WT), treatment with Sunitinib (SU11248) inhibits FLT3-WT phosphorylation in a dose-dependent manner with IC50 of approximately 250 nM. In MV4;11 cells that express FLT3-ITD, Sunitinib inhibits FLT3-ITD phosphorylation in a dose-dependent manner with an IC50 of 50 nM following a 2-hour treatment.In biochemical assays, Sunitinib (SU11248) exhibits competitive inhibition (with regard to ATP) against Flk-1 and PDGFRβ with Ki values of 9 nM and 8 nM, respectively. Sunitinib is also a competitive, albeit less potent, inhibitor of FGFR1 tyrosine kinase activity, with a Ki value of 0.83 μM. In addition to these three structurally related split kinase domain RTKs, the activity of Sunitinib has also been evaluated against a broad panel of additional tyrosine and serine/threonine kinases. In these biochemical assays, the IC50 values for Sunitinib are generally at least 10-fold higher than those for Flk-1 and PDGFR (e.g., IC50values of: >10 μM for EGFR and Cdk2; 4 μM for Met; 2.4 μM for IGFR-1; 0.8 μM for Abl; and 0.6 μM for Src) . (In Vivo) :Sunitinib Malate has very good oral bioavailability, is highly efficacious in a number of preclinical tumor models, and is well tolerated at efficacious doses. Sunitinib (80 mg/kg/day) inhibits the growth of established SF763T and Colo205 tumor xenografts in athymic mice. Sunitinib (SU11248) treatment effectively inhibits the growth of established tumor xenografts.
CAS Number
557795-19-4
Product Name Alternative
SU 11248 | SU-11248
Field of Research
Pharmacology & Drug Discovery
Purity
>98% (HPLC)
Solubility
DMSO: 25 mg/mL
Smiles
CCN (CC) CCNC (=O) C1=C (NC (=C1C) /C=C\2/C3=C (C=CC (=C3) F) NC2=O) C
Molecular Formula
C22H27FN4O2
Molecular Weight
398.4738
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1H-Pyrrole-3-carboxamide, N-[2- (diethylamino) ethyl]-5-[ (Z) - (5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene) methyl]-2,4-dimethyl-

Chemical Information

Sunitinib

Sunitinib is a member of pyrroles and a monocarboxylic acid amide. It has a role as an antineoplastic agent, an angiogenesis inhibitor, an immunomodulator, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, a neuroprotective agent and a vascular endothelial growth factor receptor antagonist. It is functionally related to a 3-methyleneoxindole.

CAS Number557795-19-4
PubChem CID5329102
IUPAC NameN-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
Molecular FormulaC22H27FN4O2
Molecular Weight398.5
XLogP2.6
Topological Polar Surface Area77.2
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count4
Rotatable Bond Count7
Heavy Atom Count29
Formal Charge0
Complexity636
SMILES
CCN(CC)CCNC(=O)C1=C(NC(=C1C)/C=C\2/C3=C(C=CC(=C3)F)NC2=O)C
InChI
InChI=1S/C22H27FN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
InChIKey
WINHZLLDWRZWRT-ATVHPVEESA-N
Chemical Structure
2D Structure
2D structure of Sunitinib
CAS: 557795-19-4
CID: 5329102
Formula: C22H27FN4O2
MW: 398.5
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight398.5
XLogP32.6
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count4
Rotatable Bond Count7
Exact Mass398.21180428
Monoisotopic Mass398.21180428
Topological Polar Surface Area77.2 Ų
Heavy Atom Count29
Formal Charge0
Complexity636
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count1
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

Alternative Products

CatalogName
B1045-500Sunitinib
A8255-2000Sunitinib malate
CS-O-10804Sunitinib-d4

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