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| SKU | Size | Availability |
Price | Qty |
|---|---|---|---|---|
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S413502-5mg
|
5mg |
3
|
$193.90
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S413502-10mg
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10mg |
2
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$343.90
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S413502-25mg
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25mg |
2
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$735.90
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S413502-50mg
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50mg |
2
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$1,201.90
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|
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S413502-100mg
|
100mg |
2
|
$1,716.90
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|
VEGFR2 Selective Inhibitors
| 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. |
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 |
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| ALogP | 3.603 |
|---|---|
| HBD Count | 2 |
| Rotatable Bond | 6 |
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
|---|
| 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 |
Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Date | Item |
|---|---|---|---|
| Certificate of Analysis | May 12, 2025 | S413502 | |
| Certificate of Analysis | May 12, 2025 | S413502 | |
| Certificate of Analysis | May 12, 2025 | S413502 | |
| Certificate of Analysis | May 12, 2025 | S413502 | |
| Certificate of Analysis | May 12, 2025 | S413502 |
| 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 |