Motesanib
Motesanib Basic information
- Product Name:
- Motesanib
- Synonyms:
-
- CS-1108
- AMG 706; AMG-706
- N-(3,3-diMethylindolin-6-yl){2-[(4-pyridylMethyl)-aMino](3-pyridyl)}-carboxaMide
- 3-PyridinecarboxaMide, N-(2,3-dihydro-3,3-diMethyl-1H-indol-6-yl)-2-[(4-pyridinylMethyl)aMino]-
- Motesanib Base
- AMG-706(Motesanib)
- Motesanib (AMG-706) Base)
- motesanib
- CAS:
- 453562-69-1
- MF:
- C22H23N5O
- MW:
- 373.45
- Product Categories:
-
- API
- Inhibitors
- Antineoplastic
- Mol File:
- 453562-69-1.mol
Motesanib Chemical Properties
- Melting point:
- 147-150°C
- Boiling point:
- 517.3±50.0 °C(Predicted)
- Density
- 1.251
- storage temp.
- Refrigerator
- solubility
- DMSO (Slightly), Methanol (Slightly)
- form
- White powder solid.
- pka
- 11.75±0.40(Predicted)
- color
- Pale Yellow
- InChI
- InChI=1S/C22H23N5O/c1-22(2)14-26-19-12-16(5-6-18(19)22)27-21(28)17-4-3-9-24-20(17)25-13-15-7-10-23-11-8-15/h3-12,26H,13-14H2,1-2H3,(H,24,25)(H,27,28)
- InChIKey
- RAHBGWKEPAQNFF-UHFFFAOYSA-N
- SMILES
- C1(NCC2C=CN=CC=2)=NC=CC=C1C(NC1=CC2=C(C=C1)C(C)(C)CN2)=O
Motesanib Usage And Synthesis
Chemical Properties
Pale Yellow Solid
Uses
Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3, PDGFR, c-Kit and Ret with IC50 of 2 nM/3 nM/6 nM, 84 nM, 8 nM and 59 nM, respectively.
Uses
Motesanib is an oral angiogenesis inhibitor, demonstrates clinical efficacy in advanced thymoma.
Definition
ChEBI: Motesanib is a pyridinecarboxamide.
in vivo
Motesanib (100 mg/kg) significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib twice daily or once daily potently inhibits, in a dose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ED50 of 2.1 mg/kg and 4.9 mg/kg, respectively. Motesanib induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells[1]. Motesanib in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models[2]. Motesanib treatment also induces significant dose-dependent reductions in tumor growth and blood vessel density of MCF-7, MDA-MB-231, or Cal-51 xenografts, which can be markedly enhanced when combined with docetaxel or tamoxifen[3].
target
VEGFR1
IC 50
VEGFR1: 2 nM (IC50); VEGFR2: 3 nM (IC50); VEGFR3: 6 nM (IC50)
MotesanibSupplier
- Tel
- 15076683720
- klq@cw-bio.com
- Tel
- 18210857532; 18210857532
- jkinfo@jkchemical.com
- Tel
- 021-20221225 13917446399
- zwchem@163.com
- Tel
- +86-21-20908456
- sales@BioChemBest.com
- Tel
- 1-(800)-881-8210
- inquiries@lgmpharma.com
Motesanib(453562-69-1)Related Product Information
- Xylene
- Imiquimod
- Dacthal
- Dimethyl fumarate
- N,N-Dimethylformamide
- Dimethyl carbonate
- Dimethyl sulfoxide
- Dimethyl sulfate
- Dimethyl phthalate
- Dimethyl ether
- ETHANE
- 2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
- N-[4-[5-(1,3-BENZODIOXOL-5-YL)-3-METHOXY-1H-1,2,4-TRIAZOL-1-YL]PHENYL]-2-(PHENYLTHIO)ACETAMIDE
- Compound 23
- ERK Inhibitor
- 6-HYDROXY-2,5,7,8-TETRAMETHYLCHROMAN-2-CARBOXYLIC ACID
- Motesanib