RegoRafenib (BAY 73-4506) mesylate 是一种口服有效的多靶点受体酪氨酸激酶 (tyROSine kinase) 抑制剂，抑制VEGFR1/2/3，PDGFRβ，Kit，RET和Raf-1的IC50分别为 13/4.2/46，22，7，1.5 和 2.5 nM。RegoRafenib mesylate 显示出非常强的抗肿瘤和抗血管生成活性。

Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC 50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity [1].

Regorafenib mesylate (0-10 μM, 96 h) shows anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells [1]. Regorafenib mesylate (0-3000 nM, 30 min) inhibits the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2 [1]. Regorafenib mesylate causes a concentration-dependent decrease in Hep3B cell growth, with an IC 50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells [2]. Cell Proliferation Assay [1] Cell Line: GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells Concentration: 10 μM and 5 nM Incubation Time: 96 h Result: Showed anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells, with IC 50 values of 45 ± 20, 34 ± 8, 401 ± 88, 560 ± 200, 900, 967 ± 287 nM. respectively. Western Blot Analysis [1] Cell Line: NIH-3T3/VEGFR2 cells, (CHO)-TIE2 cells, HAoSMCs cells, MCF-7 cells Concentration: 0, 10, 30, 100, 300, 1000, 3000 nM Incubation Time: 30 min Result: Inhibited the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, with IC 50 values of 3, 31, and 90 nM, respectively, inhibited FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10, and showed inhibition of phosphorylated FGFR substrate 2 (pFRS2) and the downstream signaling kinase pERK1/2.

Regorafenib mesylate (10 mg/kg, Orally, single dose or daily for 4 days) inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model [1]. Regorafenib mesylate (0-100 mg/kg, Orally, qd × 9) exhibits antitumorigenic and antiangiogenic effects in the Colo-205, MDA-MB-231 and 786-O model [1]. Animal Model: Rat GS9L glioblastoma xenograft [1] Dosage: 10 mg/kg Administration: Orally, single dose or daily for 4 days Result: Inhibited tumor vasculature and tumor growth in a rat GS9L glioblastoma model. Animal Model: Female athymic NCr nu/nu mice, Multiple xenograft models, including models derived from CRC (Colo-205), BC (MDA-MB-231) and RCC (786-O) tumors [1] Dosage: 0, 3, 10, 30, 100 mg/kg Administration: Orally, qd × 9 Result: Effectively inhibited growth of the Colo-205, MDA-MB-231 and 786-O model. Significantly reduces tumor MVA, effectively inhibited the RAF/MEK/ERK signaling cascade, and drastically inhibited tumor cell proliferation.

835621-08-4

C22H19ClF4N4O6S

578.92

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years