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ODM-203 - 10mM in DMSO, high purity , CAS No.1430723-35-5

    Grade & Purity:
  • 10mM in DMSO
In stock
Item Number
O421589
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O421589-1ml
1ml
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$241.90

FGFR1 Selective Inhibitors

Basic Description

Synonyms ODM-203 | 1430723-35-5 | ODM203 | Y7HJ4D4CRT | N-[3-(2,4-difluorophenyl)-5-[5-(1-methylpyrazol-4-yl)benzimidazol-1-yl]phenyl]cyclopropanesulfonamide | N-(2',4'-Difluoro-5-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)-[1,1'-biphenyl]-3-yl)cyclopropanesulfo
Specifications & Purity 10mM in DMSO
Biochemical and Physiological Mechanisms ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively.
Storage Temp Store at -80°C
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Product Description

Information

ODM-203 is a selective inhibitor ofFGFRandVEGFRwith ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively.

Targets

VEGFR3 (Cell-free assay); FGFR3 (Cell-free assay); VEGFR2 (Cell-free assay); FGFR1 (Cell-free assay); FGFR2 (Cell-free assay) 32053,5 nM; 6 n

In vitro

In cellular assays, ODM-203 inhibits VEGFR-induced tube formation (IC50 33 nmol/L) with similar potency as it inhibits proliferation in FGFR-dependent cell lines such as H1581,SNU16,and RT4 cells (IC50 50-150 nmol/L).

In vivo

ODM-203 shows strong antitumor activity in both FGFR-dependent xenograft models and in an angiogenic xenograft model at similar well-tolerated doses.

Cell Research(from reference)

Cell lines:H1581,SNU16,and RT4 cells 

Concentrations:up to 3 μmol/L 

Incubation Time:96 h 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Benzimidazoles
Subclass Phenylbenzimidazoles
Intermediate Tree Nodes Not available
Direct Parent Phenylbenzimidazoles
Alternative Parents Biphenyls and derivatives  Phenylimidazoles  Sulfanilides  Fluorobenzenes  Aryl fluorides  Organosulfonamides  N-substituted imidazoles  Organic sulfonamides  Heteroaromatic compounds  Aminosulfonyl compounds  Pyrazoles  Azacyclic compounds  Hydrocarbon derivatives  Organic oxides  Organofluorides  Organonitrogen compounds  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Phenylbenzimidazole - Biphenyl - 1-phenylimidazole - Sulfanilide - Fluorobenzene - Halobenzene - Benzenoid - Organosulfonic acid amide - Organic sulfonic acid amide - Aryl halide - Monocyclic benzene moiety - Aryl fluoride - N-substituted imidazole - Aminosulfonyl compound - Sulfonyl - Organosulfonic acid or derivatives - Organic sulfonic acid or derivatives - Heteroaromatic compound - Pyrazole - Azole - Imidazole - Azacycle - Hydrocarbon derivative - Organohalogen compound - Organofluoride - Organic nitrogen compound - Organonitrogen compound - Organosulfur compound - Organic oxygen compound - Organic oxide - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as phenylbenzimidazoles. These are compounds containing a phenylbenzimidazole skeleton, which consists of a benzimidazole moiety where its imidazole ring is attached to a phenyl group.
External Descriptors Not available

Product Properties

ALogP 4.626
hba_count 4
HBD Count 1
Rotatable Bond 6

Associated Targets(Human)

FGFR1 Tclin Fibroblast growth factor receptor 1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FGFR2 Tclin Fibroblast growth factor receptor 2 (3405 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FGFR1 Tclin Fibroblast growth factor receptor 1 (9149 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FLT1 Tclin Vascular endothelial growth factor receptor 1 (6262 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
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
FLT4 Tclin Vascular endothelial growth factor receptor 3 (3216 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RT-4 (268 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Fgfr4 Fibroblast growth factor receptor 4 (138 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 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

IUPAC Name N-[3-(2,4-difluorophenyl)-5-[5-(1-methylpyrazol-4-yl)benzimidazol-1-yl]phenyl]cyclopropanesulfonamide
INCHI InChI=1S/C26H21F2N5O2S/c1-32-14-18(13-30-32)16-2-7-26-25(10-16)29-15-33(26)21-9-17(23-6-3-19(27)11-24(23)28)8-20(12-21)31-36(34,35)22-4-5-22/h2-3,6-15,22,31H,4-5H2,1H3
InChIKey ZJFCBQXPTQSTCZ-UHFFFAOYSA-N
Smiles CN1C=C(C=N1)C2=CC3=C(C=C2)N(C=N3)C4=CC(=CC(=C4)NS(=O)(=O)C5CC5)C6=C(C=C(C=C6)F)F
Isomeric SMILES CN1C=C(C=N1)C2=CC3=C(C=C2)N(C=N3)C4=CC(=CC(=C4)NS(=O)(=O)C5CC5)C6=C(C=C(C=C6)F)F
Molecular Weight 505.54
Reaxy-Rn 24250974
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24250974&ln=

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

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

Chemical and Physical Properties

DMSO(mg / mL) Max Solubility 100
DMSO(mM) Max Solubility 197.808284210943
Water(mg / mL) Max Solubility <1
Molecular Weight 505.500 g/mol
XLogP3 4.400
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 6
Exact Mass 505.138 Da
Monoisotopic Mass 505.138 Da
Topological Polar Surface Area 90.200 Ų
Heavy Atom Count 36
Formal Charge 0
Complexity 886.000
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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