[CAS NO. 1612888-66-0] Alofanib (RPT835)
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PRODUCTS SPECIFICATIONS [1612888-66-0]
Store
Catalog
SLK-S8754
Brand
Selleck
CAS
1612888-66-0
DESCRIPTION [1612888-66-0]
Overview
| MDL | MFCD30747921 |
|---|---|
| Molecular Weight | 413.40 |
| Molecular Formula | C19H15N3O6S |
| SMILES | O=C(O)C1=CC=CC(S(=O)(NC2=CC(C3=CC=CN=C3)=C(C)C=C2[N+]([O-])=O)=O)=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4190 mL | 12.0948 mL | 24.1896 mL |
| 5 mM | 0.4838 mL | 2.4190 mL | 4.8379 mL |
| 10 mM | 0.2419 mL | 1.2095 mL | 2.4190 mL |
| 50 mM | 0.0484 mL | 0.2419 mL | 0.4838 mL |
Description
Alofanib (RPT835) is a novel selective allosteric inhibitor of and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells. It has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels in either cell lines and no effects on FGF2-FGFR2 binding.
Targets
| FGFR2 [1] (Cell-free assay) |
In vitro
Alofanib induces mainly apoptosis with cleavage of caspase 3, PARP and Bcl-2 in SKOV3 cell line. Cytotoxic effect of compound on ovarian cancer cells is low. Alofanib inhibits phosphorylation of FRS2α with the IC50 values of 7 and 9 nmol/l in cancer cells expressing different FGFR2 isoforms. In a panel of four cell lines representing several tumour types (triple-negative breast cancer,melanoma, and ovarian cancer), alofanib inhibits FGF-mediated proliferation with 50% growth inhibition (GI50) values of 16-370 nmol/l. Alofanib dose dependently inhibits the proliferation and migration of human and mouse endothelial cells (GI50: 11-58 nmol/l) compared with brivanib and bevacizumab.
References
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