Regorafenib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的多激酶抑制剂，可在纳摩尔范围的生化和细胞激酶磷酸化测定中有效抑制这些内皮细胞激酶 (IC50=3-200 nM)。

A potent multikinase inhibitor that potently inhibits these endothelial cell kinases in biochemical and cellular kinase phosphorylation assays with nanomolar range (IC50=3-200 nM); inhibits VEGFR1/2/3, PDGFRβ, FGFR1, KIT, RET and B-RAF etc.; exhibits potent dose-dependent TGI in various preclinical human xenograft models in mice; orally active.Colon Cancer Approved(In Vitro):Regorafenib (0-10 μM, 96 h) shows anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells.Regorafenib (0-3000 nM, 30 min) inhibits the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2.Regorafenib causes a concentration-dependent decrease in Hep3B cell growth, with an IC50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells.(In Vivo):Regorafenib (10 mg/kg, Orally, single dose or daily for 4 days) inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model.Regorafenib (0-100 mg/kg, Orally, qd × 9) exhibits antitumorigenic and antiangiogenic effects in the Colo-205, MDA-MB-231 and 786-O model.

Regorafenib (0-10 μM, 96 h) shows anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells.Regorafenib (0-3000 nM, 30 min) inhibits the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2.Regorafenib causes a concentration-dependent decrease in Hep3B cell growth, with an IC50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells. Cell Proliferation Assay 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 IC50 values of 45 ± 20, 34 ± 8, 401 ± 88, 560 ± 200, 900, 967 ± 287 nM. respectively.Western Blot Analysis 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 IC50 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 (10 mg/kg, Orally, single dose or daily for 4 days) inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model.Regorafenib (0-100 mg/kg, Orally, qd × 9) exhibits antitumorigenic and antiangiogenic effects in the Colo-205, MDA-MB-231 and 786-O model. Animal Model:Rat GS9L glioblastoma xenograft 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 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.

BAY 73-4506 | BAY73-4506

Angiogenesis

VEGFR

Kit|Raf-1|RET|VEGFR1|VEGFR2|B-Raf(V600E)

Cancer

Colon Cancer

755037-03-7

482.8154

C21H15ClF4N4O3

>98% (HPLC)

DMSO: ≥ 260 mg/mL

C12=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC(NC5CCCCC5)=C1NC=N2

2-Pyridinecarboxamide, 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-

(-20℃)

With Ice Pack

≥ 2 years