Alofanib|RPT-835|cas 1612888-66-0|DC Chemicals

Cas No.:	1612888-66-0
Chemical Name:	Alofanib
Synonyms:	RPT835;Alofanib;3-(N-(4-methyl-2-nitro-5-(pyridin-3-yl)phenyl)sulfamoyl)benzoic acid;LQX7RFK8MZ;Alofanib [INN];Alofanib(RPT835);Benzoic acid, 3-(((4-methyl-2-nitro-5-(3-pyridinyl)phenyl)amino)sulfonyl)-;SB19665;AK668992;ES000835
SMILES:	O=[N+](C1=CC(C)=C(C2=CC=CN=C2)C=C1NS(=O)(C3=CC(C(O)=O)=CC=C3)=O)[O-]
Formula:	C₁₉H₁₅N₃O₆S
M.Wt:	413.4039
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer activities[1]. Antiangiogenic Activity[2].
In Vivo:	In a FGFR-driven human tumour xenograft model, oral administration of alofanib (30 mg/kg) is well tolerated and resulted in potent antitumour activity[1]. Treatment with alofanib ablated experimental FGF-induced angiogenesis in vivo[1].
In Vitro:	Alofanib inhibits phosphorylation of FRS2α with IC50s of 7 and 9 nM in cancer cells expressing different FGFR2 isoforms[1]. Alofanib (10-1000 nM) inhibits FGF-mediated proliferation in a panel of four cell lines representing several tumour types (triple-negative breast cancer, melanoma, and ovarian cancer with GI50s of 16-370 nM[1].
References:	[1]. Tsimafeyeu I, et al. Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models. Eur J Cancer. 2016 Jul;61:20-8. [2]. Khochenkov DA, et al. Antiangiogenic Activity of Alofanib, an Allosteric Inhibitor of Fibroblast Growth Factor Receptor 2. Bull Exp Biol Med. 2015 Nov;160(1):84-7.

Cat. No.	Product name	Field of application
DC28032	EMI1 (EGFR MaMTH Inhibitor 1)	EMI1 (EGFR MaMTH Inhibitor 1) is a novel EGFR ex19del/T790M/C797S inhibitor.EMI1, while potently reducing the interaction of EGFR triple mutant with Shc1 in our MaMTH-DS assay, did not behave as a TKI and displayed no inhibition of the kinase activity of EGFR triple-mutant protein invitro.EMI1 did, however, more strongly inhibit the viability and increase the caspase 3/7 activ-ity of PC9 EGFR ex19del/T790M/C797S triple-mutant cells than noncancerous human bronchial epithelial (HBE) cells, as well as potently reduce PC9 EGFR ex19del/T790M/C797S organ-oid viability.EMI1 had a similar inhibi-tory effect on microtubule plus-end growth in both EGFR-WT and EGFR-C797S triple-mutant cells at 50–100 nM concentration. At 1 µM concentration, EMI1 strongly depolymerized inter-phase microtubules, perturbed spindle formation and induced strong mitotic block in PC9 EGFR ex19del/T790M/C797S cells after 20 h of treatment. EMI1 inhibited interaction of both proteins with EGFR at a level similar to that observed with Shc1, indicating it is not a specific inhibitor of the EGFR-Shc1 PPI interface. Rather, the loss of interaction mediated by EMI1 appears to be due to a more general alteration in EGFR activity.EMI1 induced EGFR degradation, and inhibited the activation of EGFR, ERK, AKT and S6 in PC9-ex19del and PC9-ex19del/T790M cells.
DC42424	CPL304110	CPL304110 is a potent, orally active and selective of fibroblast growth factor receptors FGFR (1-3), with IC50 values of 0.75 nM, 0.5 nM, and 3.05 nM for FGFR (1-3), respectively.
DC11089	TAS-120 (Futibatinib)	TAS-120 is a highly potent and selective irreversible FGFR inhibitor, effective in tumors harboring various FGFR gene abnormalities.
DC10271	SUN11602	SUN11602 is a novel aniline compound, which mimics the neuroprotective mechanisms of basic fibroblast growth factor.
DC7508	SU 5402	SU5402（SU-5402; SU5402） is potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor. (IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively).
DC2054	PD-173074	PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM.
DC10068	PD166866	PD-166866 is a selective inhibitor of the FGF-1 receptor tyrosine kinase (FGFR1) with IC50 = 55 nM, and no effect on c-Src, PDGFR-b, EGFR or insulin receptor tyrosine kinases or MEK, PKC, and CDK4.
DC7019	LY-2874455	LY2874455 is a novel and potent FGF/FGFR inhibitor.
DC10033	H3B-6527	H3B-6527 is an orally bioavailable inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity.
DC9642	FIIN-3	FIIN-3 is a potent, selective, irreversible and the next-generation covalent FGFR inhibitor.