Regorafenib (BAY-734506) Monohydrate

Dangerous Goods

CAS number：1019206-88-2 molecular formula：C21H15ClF4N4O3.H2O

overview

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physicochemical properties

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Production methods and uses

MSDS

overview

compound introduction

Information Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM forVEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E)respectively. Targets PDGFRβ (Cell-free); RET (Cell-free); Raf-1 (Cell-free); murine VEGFR2 (Cell-free); KIT (Cell-free) 29421, 1.5 nM; 2.5 nM; 4.2 nM; 7 nM In vitro Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppress PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibited the mutant receptors KIT K642E and RET C634W , with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF 165 -stimulated HUVECs, with an IC50 of approximately 3 nM. Regorafenib prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively. Regorafenib targets both tumor cell proliferation and tumor vasculature through inhibition of receptors of tyrosine kinases (VEGFR, KIT, RET, FGFR, and PDGFR) and serine/threonine kinases (Raf and p38MAPK). Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner. In vivo Regorafenib reveals potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages in breast MDA-MB-231 and renal 786-O carcinoma models. Regorafenib prevents not only the growth of syngeneic primary 4T1 breast tumors growing orthotopically in the fat pad, but also suppresses the formation of tumor metastasis in the lung. Cell Research(from reference) Cell lines：GIST 882 and TT cells Concentrations：5 nM-10 μM Incubation Time：96 h

Specs

Chinese alias	-
English alias	D10137 \| AC-25914 \| MFCD17170366 \| 4-{4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide monohydrate \| Q27137075 \| 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-
CAS number	1019206-88-2	molecular formula	C21H15ClF4N4O3.H2O
molecular weight	500.83 g/mol	Exact mass	10mM in DMSO
PSA	93.400 Å²	logp	4.174

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Safety information

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GHS08 , GHS09

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Hazard Statement：

H410: 对水生生物有剧毒并具有长期持续影响 H372: 通过长时间或反复暴露对器官造成损害 H360FD: 可能损害生育能力；可能会伤害未出生的孩子 H362: 可能对母乳喂养的孩子造成伤害

Statement of Preventive Measures：

P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P391: 收集溢出物 P263: 避免在怀孕期间/哺乳期间接触。 P203: 使用前，获取、阅读并遵守所有安全说明。 P318: 如果暴露或担心，请就医。 P319: 如果你感到不适，请寻求医疗帮助。