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SKLB 610 - 98%, high purity , CAS No.1125780-41-7

    Grade & Purity:
  • ≥98%
In stock
Item Number
S413502
Grouped product items
SKU Size
Availability
Price Qty
S413502-5mg
5mg
3
$193.90
S413502-10mg
10mg
2
$343.90
S413502-25mg
25mg
2
$735.90
S413502-50mg
50mg
2
$1,201.90
S413502-100mg
100mg
2
$1,716.90

VEGFR2 Selective Inhibitors

Basic Description

Synonyms SKLB 610 | N-Methyl-4-[4-[3-(trifluoromethyl)benzamido]phenoxy]-2-picolinamide
Specifications & Purity ≥98%
Biochemical and Physiological Mechanisms SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

Information

SKLB-610 is a multi-target inhibitor of thetyrosine kinases. It is most potent againstVEGFR2and exhibits slightly weaker inhibitor ofFGFR2 and PDGFR.


Targets

VEGFR2 ; FGFR2 ; PDGFR ; PDGFR ; FGFR2


In vitro

SKLB610 shows selective inhibition of VEGF-stimulated human umbilical vein endothelial cells (HUVECs) proliferation, and this proliferation inhibitory effect is associated with decreased phosphorylation of VEGFR2 and p42/44 mitogen-activated protein kinase (p42/44 MAPK). SKLB610 inhibits a panel of human cancer cells proliferation in a concentration-dependent manner and human nonsmall cell lung cancer cell line A549 and human colorectal cancer cell line HCT116 are most sensitive to SKLB610 treatment. At concentration of 10μM, SKLB610 inhibits 65% FGFR2 activity and 55% PDGFRE activity, respectively. Relative to PDGFR2 and FGFR2 SKLB610 has more selective inhibition of VEGFR2 which shows 97% inhibition of VEGFR2 activity at 10μM in vitro. No inhibition of enzyme activity is detected when 10μM of SKLB610 is examined against PI3K, EGFR, Aurora-A, CDK2/cyclinE and CDK6/cyclinD3.


In vivo

chronic intraperitoneally administration of SKLB610 at dose of 50mg/kg/d results in significant inhibition in the growth of established human A549 and HCT116 tumor xenografts in nude mice without exhibit toxicity.

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Benzenoids
Class Benzene and substituted derivatives
Subclass Anilides
Intermediate Tree Nodes Aromatic anilides
Direct Parent Benzanilides
Alternative Parents Diarylethers  Trifluoromethylbenzenes  Benzamides  Pyridinecarboxamides  2-heteroaryl carboxamides  Benzoyl derivatives  Phenoxy compounds  Phenol ethers  Heteroaromatic compounds  Secondary carboxylic acid amides  Azacyclic compounds  Hydrocarbon derivatives  Alkyl fluorides  Organic oxides  Organofluorides  Organonitrogen compounds  
Molecular Framework Aromatic heteromonocyclic compounds
Substituents Benzanilide - Diaryl ether - Trifluoromethylbenzene - Benzamide - Benzoic acid or derivatives - Pyridinecarboxamide - Pyridine carboxylic acid or derivatives - 2-heteroaryl carboxamide - Phenoxy compound - Benzoyl - Phenol ether - Pyridine - Heteroaromatic compound - Secondary carboxylic acid amide - Carboxamide group - Organoheterocyclic compound - Azacycle - Carboxylic acid derivative - Ether - Alkyl fluoride - Organohalogen compound - Organofluoride - Hydrocarbon derivative - Organonitrogen compound - Organooxygen compound - Organic oxide - Organic oxygen compound - Organic nitrogen compound - Alkyl halide - Aromatic heteromonocyclic compound
Description This compound belongs to the class of organic compounds known as benzanilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with a benzene ring. They have the general structure RNC(=O)R', where R,R'= benzene.
External Descriptors Not available

Product Properties

ALogP 3.603
HBD Count 2
Rotatable Bond 6

Associated Targets(Human)

KDR Tclin Vascular endothelial growth factor receptor 2 (20924 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MCF7 (126967 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 504770032
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504770032
IUPAC Name N-methyl-4-[4-[[3-(trifluoromethyl)benzoyl]amino]phenoxy]pyridine-2-carboxamide
INCHI InChI=1S/C21H16F3N3O3/c1-25-20(29)18-12-17(9-10-26-18)30-16-7-5-15(6-8-16)27-19(28)13-3-2-4-14(11-13)21(22,23)24/h2-12H,1H3,(H,25,29)(H,27,28)
InChIKey WACDHHMEVMSODJ-UHFFFAOYSA-N
Smiles CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)C3=CC(=CC=C3)C(F)(F)F
Isomeric SMILES CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)C3=CC(=CC=C3)C(F)(F)F
PubChem CID 25230662
Molecular Weight 415.37

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

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

Find and download the COA for your product by matching the lot number on the packaging.

5 results found

Lot Number Certificate Type Date Item
H2203708 Certificate of Analysis May 12, 2025 S413502
H2203709 Certificate of Analysis May 12, 2025 S413502
H2203707 Certificate of Analysis May 12, 2025 S413502
H2203710 Certificate of Analysis May 12, 2025 S413502
H2203706 Certificate of Analysis May 12, 2025 S413502

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 83 mg/mL (199.82 mM); Ethanol: 27 mg/mL (65.0 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility 83
DMSO(mM) Max Solubility 199.821845583456
Water(mg / mL) Max Solubility <1
Molecular Weight 415.400 g/mol
XLogP3 3.700
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 5
Exact Mass 415.114 Da
Monoisotopic Mass 415.114 Da
Topological Polar Surface Area 80.300 Ų
Heavy Atom Count 30
Formal Charge 0
Complexity 594.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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