Ripretinib (DCC-2618)

Catalog No.S8757

For research use only.

DCC-2618 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of the tumor-associated antigens (TAA) mast/stem cell factor receptor (SCFR) Kit (c-Kit) and PDGFR-alpha, with IC50 values of 4 nM, 8 nM, 18 nM, 5 nM and 14 nM for WT Kit (c-Kit), V654A Kit (c-Kit), T670I Kit (c-Kit), D816H Kit (c-Kit) and D816V Kit (c-Kit), respectively.

Ripretinib (DCC-2618) Chemical Structure

CAS No. 1442472-39-0

Selleck's Ripretinib (DCC-2618) has been cited by 3 Publications

Purity & Quality Control

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Biological Activity

Description DCC-2618 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of the tumor-associated antigens (TAA) mast/stem cell factor receptor (SCFR) Kit (c-Kit) and PDGFR-alpha, with IC50 values of 4 nM, 8 nM, 18 nM, 5 nM and 14 nM for WT Kit (c-Kit), V654A Kit (c-Kit), T670I Kit (c-Kit), D816H Kit (c-Kit) and D816V Kit (c-Kit), respectively.
Targets
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)
Click to View More Targets
4 nM 5 nM 8 nM 14 nM
In vitro

DCC-2618 is a switch-control type II inhibitor of KIT, which arrests KIT in an inactive state, regardless of activating mutations, such as KIT D816V. In CHO cells transiently transfected with both single and double (primary/secondary) KIT mutants, DCC-2618 robustly inhibits exon 17, exon 9/13, exon 9/14, and exon 9/17 KIT mutants, as well as exon 11/17 KIT mutants, including exon 17 D816V, D816G, D820A, D820E, D820Y, N822K, N822Y, N822H, and Y823D primary or secondary mutations[1]. DCC-2618 inhibits the proliferation and survival of various human mast cell lines (HMC-1, ROSA, MCPV-1) as well as primary neoplastic mast cells obtained from patients with advanced systemic mastocytosis (IC50 <1 μM). DCC-2618 decreases growth and survival of primary neoplastic eosinophils obtained from patients with systemic mastocytosis or eosinophilic leukemia, leukemic monocytes obtained from patients with chronic myelomonocytic leukemia with or without concomitant systemic mastocytosis, and blast cells obtained from patients with acute myeloid leukemia. Furthermore, DCC-2618 suppresses the proliferation of endothelial cells and may have additional drug effects on systemic mastocytosis-related angiogenesis. DCC-2618 downregulates IgE-mediated histamine release from basophils and tryptase release from mast cells[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Growth inhibition assay NH7NbXpDSS:IMx?= MnHSO|IhcHK| NECyRYRKdmirYnn0bY9vKG:oIFvpeEBmgG:wIEGxJIRmdGW2aX;uJEg2PTdidH:gOVU5KHKnc3nkeYV{MSCjbnSgRVgzQVBibYX0ZY51KGGwZDDZPFI{TCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFA{KM7:TT6= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
Growth inhibition assay NUjyS2VoSkFxRkO= NGrF[Fc4OiCqcoO= NHHReJVKdmirYnn0bY9vKG:oIFvpeEBmgG:wIEGxJIRmdGW2aX;uJEg2PTdidH:gOVU5KHKnc3nkeYV{MSCjbnSgUlgzOktibYX0ZY51KGGwZDDZPFI{TCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFA1KM7:TT6= MknWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
Growth inhibition assay NI\LeWhDSS:IMx?= M2jGVlczKGi{cx?= MWnJcohq[mm2aX;uJI9nKEurdDDlfI9vKDFzIHTlcIV1cW:wIDi1OVchfG9iNUW4JJJme2mmdXXzLUBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwMEC0JO69VS5? M{TTbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
Growth inhibition assay MorQRmEwTjN? NUHvNnlkPzJiaILz NEjmeHVKdmirYnn0bY9vKG:oIFvpeEBmgG:wIEGxJIRmdGW2aX;uJEg2PTdidH:gOVU5KHKnc3nkeYV{MSCjbnSgSFgzOEFibYX0ZY51KGGwZDDEPFIxSSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFA3KM7:TT6= MlLxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
Growth inhibition assay NGrPZlJDSS:IMx?= M1jHe|czKGi{cx?= M4DQS2lvcGmkaYTpc44hd2ZiS3n0JIV5d25iMUGg[IVt\XSrb36gLFU2PyC2bzC1OVghemW|aXT1[ZMqKGGwZDDEPFE3UCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFE{KM7:TT6= MnL5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
Growth inhibition assay M37jUWJCN0Z| MXm3NkBpenN? MoPJTY5pcWKrdHnvckBw\iCNaYSg[ZhwdiBzMTDk[YxmfGmxbjCoOVU4KHSxIEW1PEBz\XOrZIXld{kh[W6mIGm4NlNFKG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wNVQh|ryPLh?= M3fqflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
Growth inhibition assay M{myVmJCN0Z| MlT2O|IhcHK| MV;Jcohq[mm2aX;uJI9nKEurdDDWOVYxTCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFI{KM7:TT6= NHHtSW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay M{fWPWJCN0Z| MUK3NkBpenN? NFztXlVKdmirYnn0bY9vKG:oIFvpeEBmgG:wIEGxJIRmdGW2aX;uJEg2PTdidH:gOVU5KHKnc3nkeYV{MSCjbnSgWlY2PEFibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTBiPTCwMlA{OSEQvF2u NFPzOlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay M4PMdWJCN0Z| M4Pv[FczKGi{cx?= M4\DT2lvcGmkaYTpc44hd2ZiS3n0JIV5d25iOTDBXVUxOiC2bzC1NFMhcW6|ZYL0bY9vKG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wN|Qh|ryPLh?= NFnjVFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay NWPqN3BjSkFxRkO= Ml[4O|IhcHK| NGfTTpBKdmirYnn0bY9vKG:oIFvpeEBFQDF4VjDteZRidnRiKIXub45wf25ib4Lp[4lvMSC2cnHud4Zm[3SnZDDpckBud3W|ZTDCRU9HOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxiZ4Lve5RpKGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JG1VWyCjc4PhfUwhT0l3MDC9JFAvODN5IN88UU4> M4fWZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
Growth inhibition assay MmflRmEwTjN? NXK2WYF6PzJiaILz NW\ydoJ4UW6qaXLpeIlwdiCxZjDLbZQh\XixbjCxNUBl\WyndHnvckApPTV5IITvJFU2QCC{ZYPp[JVmeyliYX7kJGQ5OT[KIH31eIFvfCCjbnSgWFY4OElibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO|YYmsJGdKPTBiPTCwMlA{PyEQvF2u MmHZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
Growth inhibition assay NYm0S|JISkFxRkO= M2nWc|czKGi{cx?= MYLJcohq[mm2aX;uJI9nKFSHTD3meZNm\CCSRFfGVoFteGijIDj1cotvd3ewIH;ybYdqdilidILhcpNn\WO2ZXSgbY4hdW:3c3WgRmEwTjNiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIHfyc5d1cCCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUCgQUAxNjB2IN88UU4> NHH4N2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay Ml;jRmEwTjN? M{jlfFczKGi{cx?= M2PQcGlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIGDES2ZT[mW2YTCoeY5sdm:5bjDvdolocW5rIITyZY5{\mWldHXkJIlvKG2xdYPlJGJCN0Z|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwJF0hOC5yNEWg{txONg>? NH\tc2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay M1TUW2JCN0Z| NYPERm5kPzJiaILz M1XJ[2lvcGmkaYTpc44hd2ZiS3n0JHY2PjCGL1S4NVZJKG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wOFgh|ryPLh?= NHzvWZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay NFP5[5hDSS:IMx?= MVW3NkBpenN? MVvJcohq[mm2aX;uJI9nKEurdDDWOVYxTC:YNkW0RUBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwMEe1JO69VS5? M3;lPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5|MEKwOFQ1OTxxYU6=
Growth inhibition assay M{DWN2JCN0Z| MmPRO|IhcHK| M1XqVGlvcGmkaYTpc44hd2ZiS3n0JIV5d25iOTDBXVUxOiC2bzC1NFMhcW6|ZYL0bY9vKGGwZDDEPFE3KG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wO|gh|ryPLh?= MlLYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
Growth inhibition assay MoDZRmEwTjN? MnHFO|IhcHK| MUXJcohq[mm2aX;uJI9nKEuGUjCoeY5sdm:5bjDvdolocW5rIITyZY5{\mWldHXkJIlvKG2xdYPlJGJCN0Z|IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwJF0hOC5yOUig{txONg>? NGrwd2s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay MX;CRU9HOw>? NHnScFA4OiCqcoO= NInSN49KdmirYnn0bY9vKG:oIFvpeEBmgG:wIEGxJIRmdGW2aX;uJEg2PjBidH:gOVc5KHKnc3nkeYV{MSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNVMh|ryPLh?= NF:1S3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Growth inhibition assay NInOSYFDSS:IMx?= NFHOdZA4OiCqcoO= MUfJcohq[mm2aX;uJI9nKFCGR1\SZYxxcGFiVkW2NWQwTDh2Mm[gcZV1[W62IDj1cotvd3ewIH;ybYdqdilidILhcpNn\WO2ZXSgbY4hdW:3c3WgRmEwTjNiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIHfyc5d1cCCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUCgQUAxNjF6ODFOwG0v MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
Growth inhibition assay NH:xbmZDSS:IMx?= NWDzT5VvPzJiaILz MoTYTY5pcWKrdHnvckBw\iCNaYSg[ZhwdiB7IFHZOVAzKHSxIEWwN{BqdnOncoTpc44h[W6mIG[2OVQhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkKwOUDPxE1w NHLZVYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Cytotoxicity assay MV7CRU9HOw>? M4PkNlczKGi{cx?= MYnDfZRwfG:6aXPpeJkhcW5ibX;1d4UheGG{ZX70ZYwhSkFxRkOgZ4VtdHNiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwJF0hQC5yM{eg{txONg>? NHLqcVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
Assay
Methods Test Index PMID
Western blot KIT / BTK ; STAT5 / AKT / ERK 29439183
In vivo

In vivo, DCC-2618 administration at 50 mg/kg affords an ED90 for inhibition of KIT phosphorylation in the GIST T1 xenograft model, corresponding to an EC90 concentration of ∼ 470 ng/mL. When give twice daily, this oral dose results in almost complete tumor stasis. This dose of DCC-2618 produces tumor regressions in a patient derived xenograft (PDX) GIST expressing KIT exon 11 delW557K558/exon 17 Y823D, and also in a KIT exon 17 N822K AML xenograft model[1]. In xenograft studies, DCC-2618 blocks KIT and PDGFRA-driven tumor growth, including of KIT exon 17 mutants found in GIST (Y823D), AML (N822K), and mastocytosis (D816V) models[3].

Protocol (from reference)

Cell Research:

[2]

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

    For evaluation of KIT and BTK signaling, HMC-1.1, HMC-1.2, ROSA (KIT WT) and ROSA (KIT D816V) cells are incubated in control medium or in DCC-2618 (0.5–5 μM) for 4 h at 37°C. Western blotting is performed.

  • (Only for Reference)
Animal Research:

[3]

  • Animal Models: xenograft models (mice)
  • Dosages: 100 mg/kg/day or 25 mg/kg/day or 50 mg/kg BID
  • Administration: oral
  • (Only for Reference)

Solubility (25°C)

In vitro

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 510.36
Formula

C24H21BrFN5O2

CAS No. 1442472-39-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN1C2=CC(=NC=C2C=C(C1=O)C3=CC(=C(C=C3Br)F)NC(=O)NC4=CC=CC=C4)NC

In vivo Formulation Calculator (Clear solution)

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%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05080621 Withdrawn Drug: Ripretinib|Drug: binimetinib Gastrointestinal Stromal Tumors Deciphera Pharmaceuticals LLC November 2021 Phase 1|Phase 2
NCT04633122 Recruiting Drug: Ripretinib|Drug: Sunitinib Gastrointestinal Stromal Tumor(GIST) Zai Lab (Shanghai) Co. Ltd.|Zai Lab (Hong Kong) 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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