Ripretinib (DCC-2618)

For research use only. Not for use in humans.

目录号:S8757

Ripretinib (DCC-2618) Chemical Structure

CAS No. 1442472-39-0

DCC-2618是一种具有口服活性的Kit (c-Kit)PDGFR-alpha抑制剂,对WT Kit (c-Kit)、V654A Kit (c-Kit)、T670I Kit (c-Kit)、D816H Kit (c-Kit)和D816V Kit (c-Kit)的IC50分别为4 nM、8 nM、18 nM、5 nM和14 nM。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 3333.33 现货
RMB 1204.6 现货
RMB 1859.41 现货
RMB 5651.24 现货
RMB 13022.99 现货
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客户使用Selleck生产的Ripretinib (DCC-2618)发表文献2篇:

产品安全说明书

c-Kit抑制剂选择性比较

生物活性

产品描述 DCC-2618是一种具有口服活性的Kit (c-Kit)PDGFR-alpha抑制剂,对WT Kit (c-Kit)、V654A Kit (c-Kit)、T670I Kit (c-Kit)、D816H Kit (c-Kit)和D816V Kit (c-Kit)的IC50分别为4 nM、8 nM、18 nM、5 nM和14 nM。
靶点
PDGFR [2]
()
WT KIT [1]
(Cell-free assay)
D816H KIT [1]
(Cell-free assay)
V654A KIT [1]
(Cell-free assay)
D816V KIT [1]
(Cell-free assay)
4 nM 5 nM 8 nM 14 nM
体外研究

DCC-2618有效并广泛地抑制KIT原发性和耐药性突变体,如发生在外显子9、11、13、14、17和18的突变,以及发生在PDGFRA外显子12、14、18的原发性突变[3]。DCC-2618以纳摩尔级别的效力抑制多种性质的KIT:WT (IC50 4 nM), V654A (8 nM), T670I (18 nM), D816H (5 nM), D816V (14 nM)。在瞬时转染了KIT原发性突变体和二次突变的CHO细胞中,DCC-2618抑制了外显子17、外显子9/13、外显子9/14,外显子9/17,外显子11/17突变的KIT,包括位于外显子17的D816V, D816G, D820A, D820E, D820Y, N822K, N822Y, N822H和Y823D原发性或二次突变。在MO7e细胞系中,DCC-2618抑制野生型KIT的磷酸化(IC50=36 nM)。在人源GIST细胞系中,包括GIST T1(缺失外显子11)、GIST 430(缺失外显子11/外显子13 V654A)和GIST 48(外显子11 V560D/外显子17 D820A), DCC-2618也能有效抑制KIT的激活。在小鼠肥大细胞增多症中,DCC-2618可有效抑制P815细胞(表达外显子17 D816Y 突变KIT)的增殖,IC50为2 nM[1]。在多种人类肥大细胞系(HMC-1, ROSA, MCPV-1)和从晚期系统性肥大细胞增多症患者体内分离的原代肿瘤肥大细胞中,DCC-2618可抑制其增殖和生存[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Growth inhibition assay MX;CRU9HOw>? NFPLfZo4OiCqcoO= NFz2empKdmirYnn0bY9vKG:oIFvpeEBmgG:wIEGxJIRmdGW2aX;uJEg2PTdidH:gOVU5KHKnc3nkeYV{MSCjbnSgRVgzQVBibYX0ZY51KGGwZDDZPFI{TCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFA{KM7:TT6= NXHhUm5KRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
Growth inhibition assay NXza[HZLSkFxRkO= NVS0WFVTPzJiaILz MV3Jcohq[mm2aX;uJI9nKEurdDDlfI9vKDFzIHTlcIV1cW:wIDi1OVchfG9iNUW4JJJme2mmdXXzLUBidmRiTkiyNmshdXW2YX70JIFv\CC\OEKzSEBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwMEC0JO69VS5? NXH6TZBCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
Growth inhibition assay MlzrRmEwTjN? NXXwV4NrPzJiaILz Ml;NTY5pcWKrdHnvckBw\iCNaYSg[ZhwdiBzMTDk[YxmfGmxbjCoOVU4KHSxIEW1PEBz\XOrZIXld{khdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkCwOEDPxE1w NXT2c4tnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
Growth inhibition assay Mkj2RmEwTjN? Ml;uO|IhcHK| NGDjNJhKdmirYnn0bY9vKG:oIFvpeEBmgG:wIEGxJIRmdGW2aX;uJEg2PTdidH:gOVU5KHKnc3nkeYV{MSCjbnSgSFgzOEFibYX0ZY51KGGwZDDEPFIxSSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFA3KM7:TT6= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
Growth inhibition assay NUf6dY9MSkFxRkO= NFPkOos4OiCqcoO= M2DkSmlvcGmkaYTpc44hd2ZiS3n0JIV5d25iMUGg[IVt\XSrb36gLFU2PyC2bzC1OVghemW|aXT1[ZMqKGGwZDDEPFE3UCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFE{KM7:TT6= Ml7EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
Growth inhibition assay MYrCRU9HOw>? M3fHeVczKGi{cx?= NE[ydJFKdmirYnn0bY9vKG:oIFvpeEBmgG:wIEGxJIRmdGW2aX;uJEg2PTdidH:gOVU5KHKnc3nkeYV{MSCjbnSgXVgzO0RibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTBiPTCwMlAyPCEQvF2u MmDwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
Growth inhibition assay MV7CRU9HOw>? Ml;wO|IhcHK| NGXvRWxKdmirYnn0bY9vKG:oIFvpeEBXPTZyRDDteZRidnRiKIXub45wf25ib4Lp[4lvMSC2cnHud4Zm[3SnZDDpckBud3W|ZTDCRU9HOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxiZ4Lve5RpKGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JG1VWyCjc4PhfUwhT0l3MDC9JFAvODJ|IN88UU4> NEf0OZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay NFqyZYtDSS:IMx?= M{HHVFczKGi{cx?= NHjV[JlKdmirYnn0bY9vKG:oIFvpeEBmgG:wIEGxJIRmdGW2aX;uJEg2PTdidH:gOVU5KHKnc3nkeYV{MSCjbnSgWlY2PEFibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTBiPTCwMlA{OSEQvF2u NV7GWHRXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
Growth inhibition assay MmTYRmEwTjN? M2\RbFczKGi{cx?= NHTkPWJKdmirYnn0bY9vKG:oIFvpeEBmgG:wIEmgRXk2ODJidH:gOVA{KGmwc3XyeIlwdiCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFM1KM7:TT6= NFXwTpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay NX;GSJNrSkFxRkO= NH3GXmY4OiCqcoO= MWDJcohq[mm2aX;uJI9nKEurdDDEPFE3XiCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFM4KM7:TT6= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
Growth inhibition assay M2HBU2JCN0Z| MmjoO|IhcHK| MWPJcohq[mm2aX;uJI9nKEurdDDlfI9vKDFzIHTlcIV1cW:wIDi1OVchfG9iNUW4JJJme2mmdXXzLUBidmRiREixOmghdXW2YX70JIFv\CCWNkewTUBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwMEO3JO69VS5? NWrHV5RFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
Growth inhibition assay MXzCRU9HOw>? MV[3NkBpenN? MVvJcohq[mm2aX;uJI9nKFSHTD3meZNm\CCSRFfGVoFteGijIDj1cotvd3ewIH;ybYdqdilidILhcpNn\WO2ZXSgbY4hdW:3c3WgRmEwTjNiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIHfyc5d1cCCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUCgQUAxNjB2IN88UU4> M2LY[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
Growth inhibition assay NGH6XJdDSS:IMx?= MXG3NkBpenN? NYrkW5pvUW6qaXLpeIlwdiCxZjDUSWwu\nW|ZXSgVGRITlKkZYThJEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkC0OUDPxE1w M2Dsc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
Growth inhibition assay NELDfGNDSS:IMx?= MX63NkBpenN? MoTnTY5pcWKrdHnvckBw\iCNaYSgWlU3OERxREixOmghdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkC0PEDPxE1w NGLHVWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay M37vfmJCN0Z| MVu3NkBpenN? MWLJcohq[mm2aX;uJI9nKEurdDDWOVYxTC:YNkW0RUBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwMEe1JO69VS5? NEfjT5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay MV\CRU9HOw>? NWPSZ214PzJiaILz M3rScWlvcGmkaYTpc44hd2ZiS3n0JIV5d25iOTDBXVUxOiC2bzC1NFMhcW6|ZYL0bY9vKGGwZDDEPFE3KG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wO|gh|ryPLh?= NGPLd2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay MonHRmEwTjN? NHPWcII4OiCqcoO= NX7kd4E{UW6qaXLpeIlwdiCxZjDLSHIhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFk5KM7:TT6= NIn5O3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay M3Pi[WJCN0Z| NIHRXZE4OiCqcoO= MX;Jcohq[mm2aX;uJI9nKEurdDDlfI9vKDFzIHTlcIV1cW:wIDi1OlAhfG9iNUe4JJJme2mmdXXzLUBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwMUOg{txONg>? NHWxbJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay M1vpcGJCN0Z| NX7XO2FOPzJiaILz NHXqPZhKdmirYnn0bY9vKG:oIGDES2ZT[WyyaHGgWlU3OURxREi0NnYhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkG4PEDPxE1w MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
Growth inhibition assay NIPJcHVDSS:IMx?= NWPFZ48yPzJiaILz M3;qZmlvcGmkaYTpc44hd2ZiS3n0JIV5d25iOTDBXVUxOiC2bzC1NFMhcW6|ZYL0bY9vKGGwZDDWOlU1KG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6yNFUh|ryPLh?= M1\DUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
Cytotoxicity assay MlLxRmEwTjN? MXG3NkBpenN? M{PE[GN6fG:2b4jpZ4l1gSCrbjDtc5V{\SCyYYLlcpRidCCEQT;GN{Bk\WyuczDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSB6LkCzO{DPxE1w NFnjbWs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
KIT / BTK; 

PubMed: 29439183     


DCC-2618 inhibits phosphorylation of KIT and other targets in neoplastic mast cells. (A,C) HMC-1 and ROSA cells were incubated in control medium (ROSAKIT WT: Iscove modified Dulbecco medium (IMDM) with stem cell factor, SCF; ROSAKIT D816V: IMDM without SCF) or medium containing various concentrations of DCC-2618, as indicated, at 37°C for 4 h.

STAT5 / AKT / ERK; 

PubMed: 29439183     


(B) HMC-1 and ROSA cells were first pre-incubated overnight in IMDM devoid of fetal calf serum and of SCF. Cells were then treated with DCC-2618 (0.001–10 μM) for 90 min at 37℃. At the end of the treatment, ROSAKIT WT cells were stimulated with SCF (10% CHO-KL) at room temperature for 10 min.

29439183
体内研究

在体内,50 mg/kg DCC-2618可在GIST T1移植瘤模型抑制KIT磷酸化,达到90%的有效剂量(ED90),EC50约为470 ng/mL。每日两次口服给药,DCC-2618可几乎完全地造成肿瘤瘀滞[1]。在移植瘤模型中,DCC-2618可阻止KIT和PFGFRA驱动的肿瘤生长[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[2]

- 合并
  • Cell lines: HMC-1.1, HMC-1.2, ROSA (KIT WT)和 ROSA (KIT D816V)细胞
  • Concentrations: 0.5-5 μM
  • Incubation Time: 4 h
  • Method:

    将细胞培养于对照组培养基中或加入0.5-5 μM DCC-2618,置于37℃培养4小时。结束后,收集细胞提取蛋白质,进行Western blotting分析。


    (Only for Reference)
动物实验:

[3]

- 合并
  • Animal Models: 小鼠移植瘤模型
  • Dosages: 100 mg/kg/day 或 25 mg/kg/day 或 50 mg/kg BID
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (195.94 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 510.36
化学式

C24H21BrFN5O2

CAS号 1442472-39-0
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04633122 Recruiting Drug: Ripretinib|Drug: Sunitinib Gastrointestinal Stromal Tumor(GIST) Zai Lab (Shanghai) Co. Ltd. November 25 2020 Phase 2
NCT02571036 Active not recruiting Drug: DCC-2618 Gastrointestinal Stromal Tumors|Advanced Systemic Mastocytosis|Advanced Cancers Deciphera Pharmaceuticals LLC October 2015 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

c-Kit Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID