Regorafenib

別名: Fluoro-Sorafenib, BAY 73-4506 中文名稱：瑞戈非尼

目錄號(hào)：S1178 Purity: 99.98%

Regorafenib是一個(gè)多靶點(diǎn)抑制劑，作用于VEGFR1，VEGFR2，VEGFR3，PDGFR-β，Kit (c-Kit)，RET (c-RET)和Raf-1，在無細(xì)胞試驗(yàn)中IC50分別是13 nM，4.2 nM，46 nM，22 nM，7 nM，1.5 nM和2.5 nM。Regorafenib 可誘導(dǎo)自噬。

Regorafenib Chemical Structure

CAS: 755037-03-7

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	794.43	現(xiàn)貨
5mg	647.01	現(xiàn)貨
25mg	1941.03	現(xiàn)貨
100mg	4823.91	現(xiàn)貨
1g	7944.3	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

批次：純度： 99.98%

99.98

Regorafenib相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	VEGFR1 VEGFR2 VEGFR3	點(diǎn)擊展開
相關(guān)產(chǎn)品	Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Linifanib (ABT-869) SAR131675 Apatinib Apatinib (YN968D1)?mesylate Ki8751 ZM 323881 HCl Semaxanib (SU5416) SU5402 Cediranib Maleate Motesanib Diphosphate (AMG-706) Brivanib (BMS-540215) Motesanib (AMG-706) ZM 306416 KRN 633 Telatinib Fruquintinib SKLB1002 Taxifolin (Dihydroquercetin) BAW2881 (NVP-BAW2881) SU14813 SU1498 SU5614 SKLB 610 Brivanib Alaninate (BMS-582664) SU5408 SU5204	點(diǎn)擊展開
相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) 酪氨酸激酶抑制劑分子庫(kù) PI3K/Akt 抑制劑庫(kù) 細(xì)胞周期化合物庫(kù) 血管生成相關(guān)化合物庫(kù)	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
Hct-116	Growth Inhibition Assay	1-20 μM	48 h	inhibits cell growth in a dose-dependent manner	25071018
HT-29	Growth Inhibition Assay	1-20 μM	48 h	inhibits cell growth in a dose-dependent manner	25071018
DLD1	Growth Inhibition Assay	1-20 μM	48 h	inhibits cell growth in a dose-dependent manner	25071018
HT15	Growth Inhibition Assay	1-20 μM	48 h	inhibits cell growth in a dose-dependent manner	25071018
MDA-MB-231	Function Assay	0.5/5 μM	24 h	inhibits the cell migration	25253994
MCF-7	Function Assay	0.5/5 μM	24 h	inhibits the cell migration	25253994
RJ348	Function Assay	0.5/5 μM	24 h	inhibits the cell migration	25253994
RJ345	Function Assay	0.5/5 μM	24 h	inhibits the cell migration	25253994
GEO-CR	Growth Inhibition Assay	0.01-20 μM	96 h	inhibits cell growth in a dose-dependent manner	25838391
SW48-CR	Growth Inhibition Assay	0.01-20 μM	96 h	inhibits cell growth in a dose-dependent manner	25838391
HCT150	Growth Inhibition Assay	0.01-20 μM	96 h	inhibits cell growth in a dose-dependent manner	25838391
LOVO	Growth Inhibition Assay	0.01-20 μM	96 h	inhibits cell growth in a dose-dependent manner	25838391
HCT116	Growth Inhibition Assay	0.01-20 μM	96 h	inhibits cell growth in a dose-dependent manner	25838391
SW620	Growth Inhibition Assay	0.01-20 μM	96 h	inhibits cell growth in a dose-dependent manner	25838391
SW480	Growth Inhibition Assay	0.01-20 μM	96 h	inhibits cell growth in a dose-dependent manner	25838391
HT29	Growth Inhibition Assay	0.01-20 μM	96 h	inhibits cell growth in a dose-dependent manner	25838391
SW48	Growth Inhibition Assay	0.01-20 μM	96 h	inhibits cell growth in a dose-dependent manner	25838391
GEO	Growth Inhibition Assay	0.01-20 μM	96 h	inhibits cell growth in a dose-dependent manner	25838391
HEK293	Function Assay	0.5?μM	2/4/6 h	reduces GRP78 expression	25858032
HepG2?	Apoptosis Assay	1–5?μM	48 h	inhibits cell growth	26329608
PLC/PRF/5?	Apoptosis Assay	1–5?μM	48 h	inhibits cell growth	26329608
Hep3B	Apoptosis Assay	1–5?μM	48 h	inhibits cell growth	26329608
HT15	Apoptosis Assay	1-10 μM	48 h	induces cell death in a dose-dependent manner	25071018
DLD1	Apoptosis Assay	1-10 μM	48 h	induces cell death in a dose-dependent manner	25071018
HT-29	Apoptosis Assay	1-10 μM	48 h	induces cell death in a dose-dependent manner	25071018
Hct-116	Apoptosis Assay	1-10 μM	48 h	induces cell death in a dose-dependent manner	25071018
GBM5	Apoptosis Assay	0.5–1.0?μM	24 h	interacts with lapatinib to induce cell death	24911215
GBM6	Apoptosis Assay	0.5–1.0?μM	24 h	interacts with lapatinib to induce cell death	24911215
GBM12	Apoptosis Assay	0.5–1.0?μM	24 h	interacts with lapatinib to induce cell death	24911215
GBM14?	Apoptosis Assay	0.5–1.0?μM	24 h	interacts with lapatinib to induce cell death	24911215
Hep3B	Growth Inhibition Assay	1–2.5?μM	24/48/72 h	inhibits cell growth	24885890
PLC/PRF/5?	Growth Inhibition Assay	1–2.5?μM	24/48/72 h	inhibits cell growth	24885890
HepG2?	Growth Inhibition Assay	1–2.5?μM	24/48/72 h	inhibits cell growth	24885890
HCT116?	Function Assay	10/20/40 μM	24 h	induces PUMA protein and mRNA expression in a dose- and time-dependent manner	24763611
Lim2405	Function Assay	40 μM	24 h	induces PUMA protein and cell apoptosis	24763611
LoVo	Function Assay	40 μM	24 h	induces PUMA protein and cell apoptosis	24763611
Lim1215	Function Assay	40 μM	24 h	induces PUMA protein and cell apoptosis	24763611
SW48	Function Assay	40 μM	24 h	induces PUMA protein and cell apoptosis	24763611
RKO?	Function Assay	40 μM	24 h	induces PUMA protein and cell apoptosis	24763611
SW837	Function Assay	40 μM	24 h	induces PUMA protein and cell apoptosis	24763611
SW1463	Function Assay	40 μM	24 h	induces PUMA protein and cell apoptosis	24763611
SW480	Function Assay	40 μM	24 h	induces PUMA protein and cell apoptosis	24763611
Vaco432	Function Assay	40 μM	24 h	induces PUMA protein and cell apoptosis	24763611
Vaco400	Function Assay	40 μM	24 h	induces PUMA protein and cell apoptosis	24763611
DLD1	Function Assay	40 μM	24 h	induces PUMA protein and cell apoptosis	24763611
HT29?	Function Assay	40 μM	24 h	induces PUMA protein and cell apoptosis	24763611
PLC/PRF/5?	Growth Inhibition Assay	1–5μM	24/48/72 h	inhibits cell growth	23169148
HepG2	Growth Inhibition Assay	1–5μM	24/48/72 h	inhibits cell growth	23169148
Hep3B?	Growth Inhibition Assay	1–5μM	24/48/72 h	inhibits cell growth	23169148
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.021 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.029 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.033 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.047 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.049 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.051 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.063 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.094 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.108 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM.	30204441
GISTT1	Cytotoxicity assay		72 hrs	Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.13 μM.	28991465
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.231 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.29 μM.	30204441
GISTT1	Cytotoxicity assay		72 hrs	Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.38 μM.	28991465
BA/F3	Growth inhibition assay		72 hrs	Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.522 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.549 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.833 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.834 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.943 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 1.27 μM.	30204441
GISTT1	Cytotoxicity assay		72 hrs	Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 1.35 μM.	28991465
BA/F3	Growth inhibition assay		72 hrs	Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 2.371 μM.	30204441
GIST430	Cytotoxicity assay		72 hrs	Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 3 μM.	28991465
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay, GI50 = 9.953 μM.	30204441
HROC46	Growth Inhibition Assay			IC50=2.4 μM	25309914
HROC43	Growth Inhibition Assay			IC50=5.3 μM	25309914
HROC24	Growth Inhibition Assay			IC50=4.6 μM	25309914
HROC18	Growth Inhibition Assay			IC50=1.3 μM	25309914
HEK293/OATP1B1	Growth Inhibition Assay			IC50=6.2±0.3 nM	25753361
HEK293	Growth Inhibition Assay			IC50=11.0±1.2 nM	25753361
LLC-PK1/MRP2	Growth Inhibition Assay			IC50=82.4±2.7 nM	25753361
LLC-PK1	Growth Inhibition Assay			IC50=42.0±3.2 nM	25753361
KB-G2	Growth Inhibition Assay			IC50=9.1±0.1 nM	25753361
KB-31	Growth Inhibition Assay			IC50=5.5±0.3 nM	25753361
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
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生物活性

產(chǎn)品描述

特性

Regorafenib是一個(gè)新的口服多激酶抑制劑。

靶點(diǎn)

RET ^[1] (Cell-free assay)	Raf-1 ^[1] (Cell-free assay)	VEGFR2 ^[1] (Cell-free assay)	Kit ^[1] (Cell-free assay)	VEGFR1 ^[1] (Cell-free assay)	點(diǎn)擊更多
1.5 nM	2.5 nM	4.2 nM	7 nM	13 nM	點(diǎn)擊更多

體外研究(In Vitro)
體外研究活性	在 NIH-3T3細(xì)胞中 Regorafenib 強(qiáng)烈抑制 VEGFR2的自磷酸化， IC50 為3 nM. 在HAoSMCs中, Regorafenib 抑制 PDGFR-β經(jīng)過PDGF-BB刺激后的自磷酸化, IC50 為90 nM. 在MCF-7 乳腺癌細(xì)胞中， Regorafenib 也會(huì)抑制FGF10刺激后 FGFR 的信號(hào)傳導(dǎo). Regorafenib 非常有效的抑制KIT^K642E 和 RET^C634W這兩個(gè)突變的受體, IC50 分別是大約 20 nM 和 10 nM。 Regorafenib 抑制經(jīng)過VEGF¹⁶⁵ 刺激后的 HUVECs細(xì)胞的增值, IC50 為大約 3 nM. Regorafenib抑制 FGF2刺激后的 HUVECs和PDGF-BB刺激后的HAoSMCs細(xì)胞的增殖， IC50分別是127 nM 和 146 nM ^[1]。 Regorafenib通過抑制酪氨酸激酶受體(VEGFR, KIT, RET, FGFR和 PDGFR)和絲氨酸/ 蘇氨酸激酶受體(RAF 和 p38MAPK)來靶向作用于腫瘤細(xì)胞增殖和腫瘤脈管系統(tǒng)^[2]。Regorafenib以濃度依賴和時(shí)間依賴方式抑制人Hep3B, PLC/PRF/5 和 HepG2 細(xì)胞的生長(zhǎng)^[3]。
激酶實(shí)驗(yàn)	激酶活性測(cè)定
激酶實(shí)驗(yàn)	體外激酶實(shí)驗(yàn)用重組的VEGFR2 (鼠源， aa785–aa1367), VEGFR3 (鼠源 aa818–aa1363), PDGFR-β (aa561–aa1106), RAF-1 (aa305–aa648) 和 BRAFV600E (aa409–aa765)的激酶活性區(qū)域進(jìn)行。初始的激酶抑制反應(yīng)將Regorafenib的濃度固定為1 μM. IC50的值根據(jù)選定的相應(yīng)的激酶來測(cè)定, 如VEGFR1 和 RET. TIE2 的激酶抑制效果采用均相時(shí)間分辨熒光分析法測(cè)定，利用重組的TIE2細(xì)胞內(nèi)區(qū)域的GST融合蛋白和生物素化的-Ahx-EPKDDAYPLYSDFG多肽作為底物。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	GIST 882 和 TT 細(xì)胞
	濃度	5 nM-10 μM
	孵育時(shí)間	96 小時(shí)
	方法	為了分析細(xì)胞增殖情況, 將GIST 882 和 TT 細(xì)胞培養(yǎng)在含有L-glutamine谷氨酸的RPMI 培養(yǎng)基中,MDA-MB-231, HepG2和A375 細(xì)胞培養(yǎng)在含有10% hiFBS 的 DMEM 培養(yǎng)基中。將細(xì)胞用胰酶消化, 按5× 10⁴ 個(gè)每孔接種在96孔板中并在含有10% FBS 的完全培養(yǎng)基中37°C培養(yǎng)過夜。第二天, 將對(duì)照和Regorafenib用培養(yǎng)基稀釋成從10 μM 到5 nM的連續(xù)終濃度, 加入 0.2% DMSO,加入細(xì)胞培養(yǎng)基中并繼續(xù)培養(yǎng)96小時(shí)。將細(xì)胞增殖情況進(jìn)行量化。
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	PMID
	Western blot	p-STAT3 / STAT3 / PARP / Caspase-9 Cyclin D / Cyclin E / Cyclin A / Cyclin B / p27 / p21 p-FGFR2 / p-FRS2α / p-AKT / p-MAPK / p-P90RSK / FGFR2 / AKT / MAPK / p90RSK p-p65(S536) / p65 Bim / Bid / Bak / Bcl-Xl / Mcl-1 PUMA / p53		25071018
	Immunofluorescence	F-actin / Vimentin / E-cadherin p65		27580057
	Growth inhibition assay	Cell viability GI50		25071018

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在多種臨床前人類異種移植的小鼠模型上， Regorafenib有著很好的腫瘤生長(zhǎng)抑制性，這種抑制具有劑量依賴特性, 表現(xiàn)為在乳腺 MDA-MB-231 和腎臟 786-O 腫瘤模型中腫瘤減小. Regorafenib 不僅阻止了同源主要的 4T1乳腺腫瘤在脂肪墊中的原位生長(zhǎng)，也抑制了腫瘤轉(zhuǎn)移到肺部^[1]。
動(dòng)物實(shí)驗(yàn)	Animal Models	攜帶Colo-205, MDA-MB-231 細(xì)胞或者 786-O腫瘤的雌性無胸腺NCr nu/nu 小鼠
	Dosages	3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
	Administration	口服

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06321055	Not yet recruiting	Advanced Gastrointestinal Stromal Tumor	Bayer	March 20 2024	--
NCT06137170	Active not recruiting	Metastatic Colorectal Cancer	Bayer	March 1 2024	--
NCT06029010	Completed	Metastatic Colorectal Cancer	Bayer	August 31 2023	--
NCT05370807	Recruiting	Melanoma Stage III\|Melanoma Stage IV	Universitair Ziekenhuis Brussel	October 3 2022	Phase 2

參考文獻(xiàn)
[1] Wilhelm SM, et al. Int J Cancer, 2011, 129(1), 245-255. [2] Heng DY, et al. Ther Adv Med Oncol, 2010, 2(1), 39-49. [3] Carr BI, et al. J Cell Physiol, 2013, 228(2), 292-297.

參考文獻(xiàn)

[1] Wilhelm SM, et al. Int J Cancer, 2011, 129(1), 245-255.
[2] Heng DY, et al. Ther Adv Med Oncol, 2010, 2(1), 39-49.
[3] Carr BI, et al. J Cell Physiol, 2013, 228(2), 292-297.

化學(xué)信息&溶解度

分子量	482.82	分子式	C₂₁H₁₅ClF₄N₄O₃
CAS號(hào)	755037-03-7	SDF	Download Regorafenib SDF
Smiles	CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 97 mg/mL ( (200.9 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 5 mg/mL (10.35 mM)

Water : Insoluble

DMSO : 97 mg/mL ( (200.9 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 3 mg/mL (6.21 mM)

Water : Insoluble

DMSO : 96 mg/mL ( (198.83 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 97 mg/mL ( (200.9 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 97 mg/mL ( (200.9 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度批次：現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑					動(dòng)物體內(nèi)配方計(jì)算器
	澄清溶液	2% DMSO 1 30% PEG 300 2 5% Tween 80 3 ddH2O	5.0mg/ml (10.36mM)	以 1 mL 工作液為例，取20 μL 250 mg/ml的澄清DMSO儲(chǔ)備液加到300 μL PEG300中，混合均勻使其澄清；向上述體系中加入50 μL Tween-80，混合均勻使其澄清；然后繼續(xù)加入630 μL ddH2O定容至 1 mL。工作液請(qǐng)現(xiàn)配現(xiàn)用！	動(dòng)物體內(nèi)配方計(jì)算器
澄清溶液	2%DMSO 1 98% Corn oil	5.0mg/ml (10.36mM)	以 1 mL 工作液為例，取20 μL 250 mg/ml的澄清 DMSO 儲(chǔ)備液加到980 μL玉米油中，混合均勻。工作液請(qǐng)現(xiàn)配現(xiàn)用！
澄清溶液	5%DMSO 1 95% Corn oil	5.0mg/ml (10.36mM)	以 1 mL 工作液為例，取50 μL 100 mg/ml的澄清 DMSO 儲(chǔ)備液加到950 μL玉米油中，混合均勻。工作液請(qǐng)現(xiàn)配現(xiàn)用！

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術(shù)支持

在訂購(gòu)、運(yùn)輸、儲(chǔ)存和使用我們的產(chǎn)品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術(shù)支持郵箱tech@selleck.cn，直接聯(lián)系到我們。我們會(huì)在24小時(shí)內(nèi)盡快聯(lián)系您。

操作手冊(cè)

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常見問題及建議解決方法

問題 1:
How to resuspend Regorafenib for in vivo studies?

回答：
For in vivo study, we recommend to use 2% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 5mg/ml.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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Regorafenib

產(chǎn)品質(zhì)控

Regorafenib相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實(shí)驗(yàn)計(jì)算

技術(shù)支持

常見問題及建議解決方法