Sunitinib (SU11248) malate

Licensed by Pfizer Catalog No.S1042

For research use only.

Sunitinib (SU11248) malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.

Sunitinib (SU11248) malate Chemical Structure

CAS No. 341031-54-7

Selleck's Sunitinib (SU11248) malate has been cited by 134 publications

Purity & Quality Control

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Biological Activity

Description Sunitinib (SU11248) malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.
Targets
IRE1α [7]
()
Kit [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
2 nM 80 nM
In vitro

Sunitinib also potently inhibits Kit and FLT-3. [1] Sunitinib is a potent ATP-competitive inhibitor of VEGFR2 (Flk1) and PDGFRβ with Ki of 9 nM and 8 nM, respectively, displaying >10-fold higher selectivity for VEGFR2 and PDGFR than FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl, and src. In serum-starved NIH-3T3 cells expressing VEGFR2 or PDGFRβ, Sunitinib inhibits VEGF-dependent VEGFR2 phosphorylation and PDGF-dependent PDGFRβ phosphorylation with IC50 of 10 nM and 10 nM, respectively. Sunitinib inhibits VEGF-induced proliferation of serum-starved HUVECs with IC50 of 40 nM, and inhibits PDGF-induced proliferation of NIH-3T3 cells overexpressing PDGFRβ or PDGFRα with IC50 of 39 nM and 69 nM, respectively. [2] Sunitinib inhibits phosphorylation of wild-type FLT3, FLT3-ITD, and FLT3-Asp835 with IC50 of 250 nM, 50 nM, and 30 nM, respectively. Sunitinib inhibits the proliferation of MV4;11 and OC1-AML5 cells with IC50 of 8 nM and 14 nM, respectively, and induces apoptosis in a dose-dependent manner. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3 MVnLbY5ie2ViQYPzZZk> MUDJcohq[mm2aX;uJI9nKFCGR1[tbY5lfWOnZDDCdoRWKGmwY3;ydI9z[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEC3JO69VQ>? M4jO[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF{NkS2NFE6Lz5zMk[0OlAyQTxxYU6=
3T3 NHT5N2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HCUmlvcGmkaYTpc44hd2ZiUHzheIVt\XRvZHXybZZm\CCpcn;3eIgh\mGldH;yJIlv\HWlZXSgN3Q{KGOnbHygdJJwdGmoZYLheIlwdiC5aYToJGlEPTBib3[gNE4xOSEQvF2= NV;1UFY1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUK2OFYxOTlpPkGyOlQ3ODF7PD;hQi=>
3T3 M4PzVGZ2dmO2aX;uJGF{e2G7 MXLJcohq[mm2aX;uJI9nKF[jc3P1cIFzKGWwZH;0bIVtcWGuIHfyc5d1cCCoYXP0c5IhemWlZYD0c5Ihf2m2aDDJR|UxKG:oIECuNFUh|ryP NY\iSG5rRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUK2OFYxOTlpPkGyOlQ3ODF7PD;hQi=>
3T3 MnK5T4lv[XOnIFHzd4F6 NHLXZ4UzOCCvaX6= NGjRb2pFVVOR NF35V3hE\WyudXzhdkBqdmirYnn0bY9vKG:oIG\FS2YhcW6mdXPl[EBpfW2jbjDLSHIheGixc4Doc5J6dGG2aX;uJJdqfGhiSVO1NEBw\iByLkCyNkDPxE1? MmrMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZzNkKwNFgoRjF4MU[yNFA5RC:jPh?=
NIH3T3 NIroZXhMcW6jc3WgRZN{[Xl? NHPYbWwzOCCvaX6= Mn3vSG1UVw>? M{DtOIlvcGmkaYSgbJVu[W5iS1TSJItqdmG|ZTDlfJBz\XO|ZXSge4l1cCCLQ{WwJI9nKDBwMEG4JO69VQ>? M4exWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4MU[yNFA5Lz5zNkG2NlAxQDxxYU6=
A549 MY\GeY5kfGmxbjDBd5NigQ>? M{TH[GROW09? NHuycJJKdmirYnn0bY9vKG:oIHOtUYV1KGSncHXu[IVvfCCKR1[tbY5lfWOnZDDoeY1idiCDNUS5JINmdGxibXnndoF1cW:wIIfpeIghUUN3MDDv[kAzKM7:TR?= NGXGVWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOESzOFE1PSd-MUi0N|QyPDV:L3G+
DU145 MX3GeY5kfGmxbjDBd5NigQ>? NI\NblFFVVOR NXPzTG0zUW6qaXLpeIlwdiCxZjDjMW1mfCCmZYDlcoRmdnRiSFfGMYlv\HWlZXSgbJVu[W5iRGWxOFUh[2WubDDzZ4F1fGW{aX7nJJdqfGhiSVO1NEBw\iBzMDFOwG0> NYnZTW4{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi0N|QyPDVpPkG4OFM1OTR3PD;hQi=>
KB3-1 NXPOU5BXS3m2b4TvfIlkKEG|c3H5 M3PoWlczKGh? MV\EUXNQ M2LFd2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHAu\3BvbnXnZZRqfmViS1KtN{0yKGOnbHzzJJdqfGhiSVO1NEBw\iB{LkOg{txO NFzwXWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUO5O|MzOid-MUmzPVc{OjJ:L3G+
KBV1 NUPVPHRSS3m2b4TvfIlkKEG|c3H5 M3fKbFczKGh? MmjDSG1UVw>? MnHRR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVE1odHmlb4Dyc5RmcW5vZYjwdoV{e2mwZzDLRnYyKGOnbHzzJJdqfGhiSVO1NEBw\iB2LkGg{txO MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTN7N{OyNkc,OTl|OUezNlI9N2F-
A375 M1XZUmN6fG:2b4jpZ{BCe3OjeR?= MXu3NkBp MYnEUXNQ NVH3foE6UUN3ME21MlQh|ryP MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ3NESwPEc,OTl4NUS0NFg9N2F-
RS4-11 M176SGZ2dmO2aX;uJGF{e2G7 M4jYWFIhcA>? M{LMcmlvcGmkaYTpc44hd2ZiRlzUN{BifXSxcHjvd5Bpd3K7bHH0bY9vKHerdHigTWM2OCCxZjCwMlAxQTlizszN MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ3NESwPEc,OTl4NUS0NFg9N2F-
RS4-11 MmntSpVv[3Srb36gRZN{[Xl? NE\Ce44zKGh? NX7UWHZNUW6qaXLpeIlwdiCxZjDGUHQ{KEmWRDDteZRidnRiYYX0c5Bpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yM{Sg{txO MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ3NESwPEc,OTl4NUS0NFg9N2F-
Sf9 M3rzWGtqdmG|ZTDBd5NigQ>? MoPoN|AhdWmw MY\Jcohq[mm2aX;uJI9nKEeVVD30ZYdo\WRiVlXHSnIh\XiycnXzd4VlKHerdHigTWM2OCCxZjCwMlE5PSEQvF2= Mn:yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl6NUSwOVEoRjF7OEW0NFUyRC:jPh?=
Ba/F3 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjO[G46PzJiaB?= NVHnfWZiUUN3ME2xMlIh|ryP M{njT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMUG3NFA1Lz5{MEGxO|AxPDxxYU6=
BaPTC2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGiwVng4OiCq MXvJR|UxRTBwMkKg{txO NHK2N5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEGxO|AxPCd-MkCxNVcxODR:L3G+
Sf9 MlLsSpVv[3Srb36gRZN{[Xl? MoPUNUBp NUC0em9DTE2VTx?= NF;iU3NKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IFjpd{11[WepZXSgVmVVKGW6cILld5Nm\CC5aYToJGlEPTBib3[gNU4{KM7:TR?= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODFzN{CwOEc,OjBzMUewNFQ9N2F-
H4 NH3jN2tEgXSxdH;4bYMhSXO|YYm= MUWxNEDPxE1? MXHUc5hq[2m2eTDpckBpfW2jbjDIOEBk\Wyucx?= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODN3MEiwOkc,OjB|NUC4NFY9N2F-
SF-539 MkHUT4lv[XOnIFHzd4F6 MWCzN|Mh|ryP Mn;YOlAhdWmw MU\EUXNQ M4rGfmlvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNVIvOiEQvF2= NUXEUXl5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC0NFM4ODBpPkKwOFA{PzByPD;hQi=>
U251 NIHafoVMcW6jc3WgRZN{[Xl? MX[zN|Mh|ryP NEXXc2M3OCCvaX6= M13BZmROW09? MX3Jcohq[mm2aX;uJI9nKF[HR1\SNkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDF6Lkmg{txO NUPkUJRoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC0NFM4ODBpPkKwOFA{PzByPD;hQi=>
A431 NXXicml[U2mwYYPlJGF{e2G7 M4\y[mlvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOTJwMjFOwG0> MlfwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3NUiwO|IoRjJyNUW4NFczRC:jPh?=
A431 Mn6zT4lv[XOnIFHzd4F6 MmC0TY5pcWKrdHnvckBw\iCYRVfGVlIh\XiycnXzd4VlKHerdHigTWM2OCCxZjCxPE46KM7:TR?= NGHWfXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEW1PFA4Oid-MkC1OVgxPzJ:L3G+
HepG2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3FO|IhcA>? NUnlN4w{UUN3ME2zMlgyKM7:TR?= NFfFS2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEW3NFUzPid-MkC1O|A2OjZ:L3G+
Kasumi-1 NUm0cHA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkOwO|IhcA>? NYCxenVvUUN3ME2wMlAyPiEQvF2= NVzPTJJMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1O|A2OjZpPkKwOVcxPTJ4PD;hQi=>
RS4-11 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXrR3lSPzJiaB?= MYrJR|UxRTFizszN M2q5dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUewOVI3Lz5{MEW3NFUzPjxxYU6=
THP1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWe3NkBp NUHCV4tEUUN3ME2wMlUh|ryP MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV5MEWyOkc,OjB3N{C1NlY9N2F-
Kasumi-1 NYDzTnpGTnWwY4Tpc44hSXO|YYm= MYPJcohq[mm2aX;uJI9nKGNvS3n0JIF2fG:yaH;zdIhwenmuYYTpc44hf2m2aDDJR|UxKG:oIECuNFE2KM7:TR?= M{S2SFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyOEOzNFM6Lz5{MEizN|A{QTxxYU6=
A549 NXLzNVRCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVmxOkBp Mm[4RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\Wyucx?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR3MES2N{c,OjF2NUC0OlM9N2F-
HL60 M2Dadmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\rdpZIOTZiaB?= MkP1RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\Wyucx?= NV\1NnM6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OVA1PjNpPkKxOFUxPDZ|PD;hQi=>
HUVEC NHXWbZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTlTHRxOTZiaB?= NYrGSmV7UW6qaXLpeIlwdiCxZjDWSWdHNWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjCyMlc2KM7:TR?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR3MES2N{c,OjF2NUC0OlM9N2F-
HUVEC NXjB[4ZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYexOkBp M1XQOmlvcGmkaYTpc44hd2ZiYl\HSk1qdmS3Y3XkJINmdGxicILvcIln\XKjdHnvckB4cXSqIFnDOVAhd2ZiND6wOEDPxE1? Ml23QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2NUC0OlMoRjJzNEWwOFY{RC:jPh?=
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MDA-MB-231 NF\iUWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPKc3Q3OTZiaB?= MYfBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{ MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR3MES2N{c,OjF2NUC0OlM9N2F-
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HUVEC NE\JTY9HfW6ldHnvckBCe3OjeR?= NESwS5MyKM7:TR?= NFjC[YgzPCCq NF7wTGtCdnSrYX7nbY9o\W6rYzDhZ5Rqfmm2eTDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCYRVfGMYlv\HWlZXSgZ4VtdCCvaXfyZZRqd25? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl4M{OwOUc,OjF7NkOzNFU9N2F-
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Bel7402 M1rPOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3r6dFczKGh? MmXXSG1UVw>? MlrTTWM2OD1{Lk[3JO69VQ>? MlXDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MES5OlEoRjJ2OUC0PVYyRC:jPh?=
HK2 NVqxN|NQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzTO|IhcA>? NGrtSZFFVVOR MlXzTWM2OD13Lki1JO69VQ>? NULYTWdvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFQ6PjFpPkK0PVA1QTZzPD;hQi=>
LO2 MnGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWK3W|NFPzJiaB?= NX7VTYhWTE2VTx?= M4rITWlEPTB;MUmuPVMh|ryP NV\xdphSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFQ6PjFpPkK0PVA1QTZzPD;hQi=>
MV4-11 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXzOFghcA>? MYDEUXNQ NGXGZnhKSzVyPUCuNFA{KM7:TR?= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyNEm2NUc,OjR7MES5OlE9N2F-
NCI-H3122 M{jkR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH:0ZpM4OiCq MXrEUXNQ NU[4OGdVUUN3ME2wMlg{KM7:TR?= MnTrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MES5OlEoRjJ2OUC0PVYyRC:jPh?=
NCI-H460 M4XueGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVG3NkBp NYDGenhoTE2VTx?= M4XQOWlEPTB;ND6zNUDPxE1? MnzIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MES5OlEoRjJ2OUC0PVYyRC:jPh?=
NCI-H526 M3;sSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY[3NkBp NIHGd4JFVVOR NEXveG1KSzVyPUGuNFEh|ryP MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyNEm2NUc,OjR7MES5OlE9N2F-
TT MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{OyOFczKGh? NWXIempQTE2VTx?= M3m2Z2lEPTB;MD6wOEDPxE1? NEPBVo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwOFk3OSd-MkS5NFQ6PjF:L3G+
3T3 NFOwe4tCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MnT2O|IhcHK| MkK3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SB|VEOgZ4VtdHNiZYjwdoV{e2mwZzDoeY1idiCFU1[xVkBi\nSncjC3NkBpenNiYomgR4VtdHSrdHXyJIF{e2G7LDDBZ5Rqfmm2eTC9JFAvODlizszNMi=> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDZ7NE[0NUc,OTh4OUS2OFE9N2F-
MV4-11 NVLGOoJmSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MmHSO|IhcHK| MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YND2xNUBk\WyuczDh[pRmeiB5MjDodpMh[nliY3XscEB1cXSncj3icJVmKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxKD1iMD6wNFQ{KM7:TT6= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd3NEG5PUc,OTl5NUSxPVk9N2F-
HEK293 NV73WmduTnWwY4Tpc44h[XO|YYm= NWXtS4c1SmmwZHnu[{Bi\m[rbnn0fUB1dyCITGSzJINifGGueYTpZ{Bld22jaX6g[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDifUBkd22yZYTpeIl3\SCkaX7kbY5oKGG|c3H5MEBM\CB;IECuNFAxPDdizszNMi=> M4HVUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{W0NVk6Lz5zOUe1OFE6QTxxYU6=
FDC-P1 NYjSTpdtTnWwY4Tpc44h[XO|YYm= NV\VeotXPDhiaILz NGXjcotKdmirYnn0bY9vKG:oIHj1cYFvKE[PUzDlfJBz\XO|ZXSgbY4h\3Kxd4ToJIZi[3SxcjDk[ZBmdmSnboSgcY92e2ViRlTDMXAyKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gSm1UNW2nZHnheIVlKGOnbHygdJJwdGmoZYLheIlwdiCrbjDwdoV{\W6lZTDoeY1idiCFU1[xJIFnfGW{IES4JIhzeyCkeTDy[ZNignW{aX6g[JlmKHKnZIXjeIlwdiCjc4PhfUwhUUN3MDC9JFAvOTV3IN88UU4> NIHOWHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEG1OlY5QSd-MkCxOVY3QDl:L3G+
primary leukemia cells NFWyeGpEgXSxdH;4bYNqfHliYYPzZZk> NUnCW3dGPzJiaILz MkHnR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gdJJqdWG{eTDs[ZVs\W2rYTDj[YxteyCrc3;sZZRm\CCocn;tJIFkfXSnIH35[YxwcWRibHX1b4VucWFicHH0bYVvfCCneIDy[ZN{cW6pIF\MWFMuUVSGIH31eIF1cW:wIHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDd{IHjyd{BjgSCudXPp[oVz[XOnIHHzd4F6NCCLQ{WwJF0hOC5yMzFOwG0v M1LhTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkKxNlAyLz5{MkKyNVIxOTxxYU6=
primary leukemia cells MnPaR5l1d3SxeHnjbZR6KGG|c3H5 MUS3NkBpenN? M1\RWGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJJBzcW2jcomgcIV2c2WvaXGgZ4VtdHNiaYPvcIF1\WRiZoLvcUBi[3W2ZTDtfYVtd2mmIHzleYtmdWmjIIDheIlmdnRiZYjwdoV{e2mwZzD3bYxlKHS7cHWgSmxVOyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhdHWlaX\ldoF{\SCjc4PhfUwhUUN3MDC9JFAvODNizszNMi=> M{\FUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MkKxNlAyLz5{MkKyNVIxOTxxYU6=
primary leukemia cells MoTWR5l1d3SxeHnjbZR6KGG|c3H5 MVW3NkBpenN? NIDx[ldEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBxemmvYYL5JIxmfWunbXnhJINmdGy|IHnzc4xifGWmIH\yc40h[WO3dHWgcZlmdG:rZDDs[ZVs\W2rYTDwZZRq\W62IHX4dJJme3OrbnegSmxVOy2GOEO1XUBufXSjdHnvckBie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgcJVkcW[ncnHz[UBie3OjeTygTWM2OCB;IEGuNUDPxE1w NHrYSmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKyNVIxOSd-MkKyNlEzODF:L3G+
endothelial precursor cells NUDtU|g{TnWwY4Tpc44h[XO|YYm= M4HOSGlvcGmkaYTpc44hd2ZiZX7kc5Rp\WyrYXygZ49z\CCjcnXhJIZwem2jdHnvckBqdiCnbnTveIhmdGmjbDDwdoVkfXK|b4KgZ4VtdHNiYomgR2Q{OSClb4LkJIFz\WFiZHX0[YN1cW:wIHLhd4VlKHCqZX7veJlxcWNiZIL1[{BlcXOlb4\ldpkh[mG|ZXSgZZN{[XluIFnDOVAhRSByLkCwPVYh|ryPLh?= MlK2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ2MEm2OlYoRjJ{NEC5OlY3RC:jPh?=
endothelial precursor cells MV7GeY5kfGmxbjDhd5NigQ>? Mo\lTY5pcWKrdHnvckBw\iClZXzsJI1q\3KjdHnvckBqdiCnbnTveIhmdGmjbDDwdoVkfXK|b4KgZ4VtdHNiYomgU5JqeyClZXzsJI1q\3KjdHnvckBscXRiYnHz[YQheGinbn;0fZBq[yCmcoXnJIRqe2OxdnXyfUBj[XOnZDDhd5NigSxiSVO1NEA:KDF|Lk[g{txONg>? NInBbWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkSwPVY3Pid-MkK0NFk3PjZ:L3G+
U251 MkPESpVv[3Srb36gZZN{[Xl? NWfMdpJjPjBibXnudy=> Mo\TTY5pcWKrdHnvckBw\iCYRVfGVlIhcW5iaIXtZY4hXTJ3MTDj[YxteyCycnX0doVifGWmIH\vdkA3OCCvaX7zJI1m[XO3cnXkJIFnfGW{IEGgbJIh[nliRVzJV2EtKEmFNUCgQUAyQC57IN88UU4> NES0bmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkezPVA6OCd-MkK3N|kxQTB:L3G+
U251 NFjSemhHfW6ldHnvckBie3OjeR?= MX:2NEBucW6| NFPPfWJKdmirYnn0bY9vKG:oIG\FS2YucW6mdXPl[EBXTUeIUkKgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIGWyOVEh[2WubIOgc5ZmemW6cILld5NqdmdiRnzrMVEheHKndILlZZRm\CCob4KgOlAhdWmwczDwdolweiC2bzDWSWdHKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFExKG2rboOgZpkheGixc4Doc5R6em:|aX7lJGVNUVODIHP5eI9jdG:2IHHuZYx6e2m|LDDJR|UxKD1iMUiuPUDPxE1w NF7rVHk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3OVA6OCd-MkOzO|UxQTB:L3G+
U251 NX:wZ4RTTnWwY4Tpc44h[XO|YYm= NXPaUYU5PjBibXnudy=> MkLhTY5pcWKrdHnvckBw\iCYRVfGVlIhcW5iaIXtZY4hXTJ3MTDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKF[HR1[tbY5lfWOnZDD0fZJwe2mwZTDwbI9{eGixconsZZRqd25iaX7jeYJifGWmIH\vdkA3OCCvaX7zJJBzcW:{IITvJHZGT0ZvYXP0bZZifGmxbjDt[YF{fXKnZDCxNEBucW6|IHL5JGVNUVODLDDJR|UxKD1iMUiuPUDPxE1w M4LleFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEO0NVM6Lz5{M{SzOFE{QTxxYU6=
CHO MYHGeY5kfGmxbjDhd5NigQ>? NY\FZ2t6UW6qaXLpeIlwdiCxZjDDZZYyNjJiY4XydoVvfCCvZXHzeZJm\CC3c3nu[{BSWGG2Y3igZZV1d22jdHnjJJBifGhiY3zhcZAhe3m|dHXtJIlvKEOKTzDj[YxteyCneIDy[ZN{cW6pIFPhelEvOixiYnX0ZU0zKGGwZDDhcJBp[S1{L3TlcJRiNTFic4XieY5qfHNuIFnDOVAhRSB|Mz60JO69VS5? NH3pRpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{ixNlUxOyd-MkO4NVI2ODN:L3G+
U251 MmflSpVv[3Srb36gZZN{[Xl? MYjJcohq[mm2aX;uJI9nKF[HR1\SNkBqdiCqdX3hckBWOjVzIHPlcIx{KGK7IIDoc5NxcG:2eYLvd4lv\SCHTFnTRUwhUUN3MDC9JFAvODF6OTFOwG0v MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEi2OUc,OjR7MEC4OlU9N2F-
MCF7 NFLFdlRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M2nFRlQ5KGi{cx?= NGjM[GlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEGwMlUh|ryPLh?= NGThfFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2OFM1Pyd-MkWwOlQ{PDd:L3G+
HepG2 NIjsc5RCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MnzUOFghcHK| M4rubWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEGzMlYh|ryPLh?= NFHzPVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2OFM1Pyd-MkWwOlQ{PDd:L3G+
CHO MWnGeY5kfGmxbjDhd5NigQ>? NULMZYZwUW6qaXLpeIlwdiCxZjDyZZBq\CCmZXzhfYVlKGmwd3Hy[EBz\WO2aX\5bY5oKHCxdHHzd4l2dSCldYLy[Y51KCiLS4KpJIlvKEOqaX7ld4UhcGGvc4TldkBwfmG{eTCoR2hQMSClZXzsd{B{fGGkbHWg[ZhxemW|c3nu[{BpTVKJIH3lZZN2emWmIIXzbY5oKEmxbmfvdot{KEKjcoLhZ5Vl[SCjdYTvcYF1\WRicHH0Z4gh[2yjbYCgdIxifG[xcn2sJGlEPTBiPTC3Mlk1OzJ6IN88UU4> NY\PV4FvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPFc4PTNpPkK1NFg4PzV|PD;hQi=>
CHO K1 MnWySpVv[3Srb36gZZN{[Xl? M2LvWGlvcGmkaYTpc44hd2ZicnHwbYQh\GWuYYnl[EBqdnejcnSgdoVkfGmoeXnu[{Bxd3Sjc4PpeY0h[3W{cnXueEApUUu{KTDpckBEcGmwZYPlJIhidXO2ZYKgc5ZienliKFPIU{khUzFiY3XscJMhe3SjYnz5JIV5eHKnc4PpcochcEWURzDt[YF{fXKnZDD1d4lv\yCLb37Xc5JseyCTdXH0eJJwKGG3dH;tZZRm\CCyYYTjbEBkdGGvcDDwcIF1\m:{bTygTWM2OCB;IEGwJO69VS5? NF3I[Yg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC4O|c2Oyd-MkWwPFc4PTN:L3G+
CHO K1 M{TGNmZ2dmO2aX;uJIF{e2G7 NYnUV4gyUW6qaXLpeIlwdiCxZjDmZZN1KHOxZHn1cUBkfXK{ZX70JEhKVmFrIHnuJGNpcW6nc3WgTIFue3SncjDPeoFzgSBqQ1jPLUBMOSClZXzsd{B1emGwc3\lZ5Rm\CC5aYToJIh2dWGwIF7helEvPSCvZXHzeZJm\CC3c3nu[{BKd26Zb4Lrd{BSfWG2dILvJIF2fG:vYYTl[EBx[XSlaDDjcIFueCCybHH0[o9zdSxiSVO1NEA:KDF3Lki0PFkh|ryPLh?= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB6N{e1N{c,OjVyOEe3OVM9N2F-
HEK293 NYLnd3B2TnWwY4Tpc44h[XO|YYm= MlfZTY5pcWKrdHnvckBw\iCoYYP0JJNw\Gm3bTDjeZJz\W62IDjJUoEqKGmwIFjFT|I6OyClZXzsd{B1emGwc3\lZ5Rm\CC5aYToJIh2dWGwIF7helEvPSCvZXHzeZJm\CC3c3nu[{BKd26Zb4Lrd{BSfWG2dILvJIF2fG:vYYTl[EBx[XSlaDDjcIFueCCybHH0[o9zdSxiSVO1NEA:KDN7LkixNFch|ryPLh?= NW[2N41mRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPFc4PTNpPkK1NFg4PzV|PD;hQi=>
MOLM13 MnnsR5l1d3SxeHnjbZR6KGG|c3H5 M4XxOFQ5KGi{cx?= MmC0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUW9NVTF|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUCgQUAxNjBzN{eg{txONg>? NGnacZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC4PVgyOCd-MkWwPFk5OTB:L3G+
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BAF3 MkjtSpVv[3Srb36gZZN{[Xl? MX[3NkBpenN? NHPlSYdKdmirYnn0bY9vKG:oIGTlcE1nfXOnZDDjT2lVKCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlHGN{Bk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KGOnbHz0bZRmei2pbH:vR2NMQCCjc4PhfUwhT0l3MDC9JFAvODd6IN88UU4> NYXLdI01RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|c4ODVpPkK3NFc4PzB3PD;hQi=>
GIST882 MXTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NFXOWGs4OiCqcoO= MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHPLTXQh\GWyZX7k[Y51KGi3bXHuJGdKW1R6OEKgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDj[YxtfGm2ZYKt[4xwN0OFS{igZZN{[XluIFfJOVAhRSByLkGxJO69VS5? MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{ewOUc,OjdyN{e3NFU9N2F-
BAF3 MX\GeY5kfGmxbjDhd5NigQ>? NVzaS5ZLPzJiaILz NXriPJhoUW6qaXLpeIlwdiCxZjDU[Ywu\nW|ZXSgZ2tKXCCQOEKyT{BufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSUZ|IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJINmdGxicILvcIln\XKjdHnvckBi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXyMYdtdy:FQ1u4JIF{e2G7LDDHTVUxKD1iMD61NUDPxE1w NGmwU3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{C3O|cxPSd-MkewO|c4ODV:L3G+
Rec1 MnXYRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NFrMVnI4OiCqcoO= NYLuTJQySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDS[YMyKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVzNWeubz;DR2s5KGG|c3H5MEBIUTVyIE2gNE45PyEQvF2u M4LBSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3O|A2Lz5{N{C3O|cxPTxxYU6=
K562 MXXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M2W1W|czKGi{cx?= M4nO[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgRmNTNUGETDDk[ZBmdmSnboSgbJVu[W5iS{W2NkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO|IhcHK|IHL5JINmdGy2aYTldk1odG9xQ1PLPEBie3OjeTygS2k2OCB;IEGg{txONg>? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{ewOUc,OjdyN{e3NFU9N2F-
KU812 MUTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M2ToZVczKGi{cx?= NFi1ZphCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGJEWi2DQlyg[IVx\W6mZX70JIh2dWGwIFvVPFEzKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVzNWeubz;DR2s5KGG|c3H5MEBIUTVyIE2gNU4yKM7:TT6= M{WxZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3O|A2Lz5{N{C3O|cxPTxxYU6=
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U937 NHPYUWxCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NFfPRWQ4OiCqcoO= MlLxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXOUO3JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgZ4VtdHSrdHXyMYdtdy:FQ1u4JIF{e2G7LDDHTVUxKD1iMT63JO69VS5? NX7QNGhsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewO|c4ODVpPkK3NFc4PzB3PD;hQi=>
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CHO M2C0XGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NUj1XlF5PzJiaILz NGrSfItCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGNJVyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KGOnbHz0bZRmei2pbH:vR2NMQCCjc4PhfUwhT0l3MDC9JFIvODNizszNMi=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB5N{ewOUc,OjdyN{e3NFU9N2F-
CHL MUTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M4i2dlczKGi{cx?= M{S0dGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgR2hNKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkh[2WubITpeIVzNWeubz;DR2s5KGG|c3H5MEBIUTVyIE2gNk41QCEQvF2u M4n4NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MEe3O|A2Lz5{N{C3O|cxPTxxYU6=
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MDA-MB-231 M1jDNGN6fG:2b4jpZ4l1gSCjc4PhfS=> M{CxfVQ5KGi{cx?= MXLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB5LkSg{txONg>? MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF{OEG3N{c,OjdzMkixO|M9N2F-
BT549 NV\kSVFVS3m2b4TvfIlkcXS7IHHzd4F6 NUjNVnp{PDhiaILz NUPjNVNOS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSlR3NEmgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDF3LkWg{txONg>? M{HnNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MUK4NVc{Lz5{N{GyPFE4OzxxYU6=
DU145 M3nqd2N6fG:2b4jpZ4l1gSCjc4PhfS=> NUjGVo5oPDhiaILz MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNVYvPCEQvF2u MkO4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzMkixO|MoRjJ5MUK4NVc{RC:jPh?=
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LNCAP NHK2ZVhEgXSxdH;4bYNqfHliYYPzZZk> NU\4dXN1PDhiaILz M2XlUWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxPS0GSIHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzMj62NUDPxE1w MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzJzMESzPEc,Ojd{MUC0N|g9N2F-
RWPE1 NUXBc5Y5S3m2b4TvfIlkcXS7IHHzd4F6 NET4VWQ1QCCqcoO= MX3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSW3BGOSClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOjNizszNMi=> M4PxVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MkGwOFM5Lz5{N{KxNFQ{QDxxYU6=
MCF7 M2XSdGN6fG:2b4jpZ4l1gSCjc4PhfS=> NXH4dYZTPDhiaILz MnzNR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOjNwN{[g{txONg>? NIHtbnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{KxNFQ{QCd-MkeyNVA1Ozh:L3G+
MDA-MB-231 NIKze2VEgXSxdH;4bYNqfHliYYPzZZk> NHz4dHc1QCCqcoO= MnXFR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFcvPDRizszNMi=> NUXyTVFTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0OFg6OTZpPkK3OFQ5QTF4PD;hQi=>
A549 NYLpOHNwS3m2b4TvfIlkcXS7IHHzd4F6 NGjae401QCCqcoO= M4PNdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzND60JO69VS5? NY\HbJh{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke0OFg6OTZpPkK3OFQ5QTF4PD;hQi=>
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Assay
Methods Test Index PMID
Western blot p-STAT3 / STAT3 / p-Src / Src / p-AKT / AKT / p-ERK / ERK ; p-GSK3β / GSK3β / MYCN ; p-AKT / AKT / p-ERK / ERK 19244102 24759734
Growth inhibition assay Cell viability 24369536
In vivo

Consistent with the substantial and selective inhibition of VEGFR2 or PDGFR phosphorylation and signaling in vivo, Sunitinib (20-80 mg/kg/day) exhibits broad and potent dose-dependent anti-tumor activity against a variety of tumor xenograft models including HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435. Sunitinib dosing at 80 mg/kg/day for 21 days leads to complete tumor regression in six of eight mice, without tumor re-growing during a 110-day observation period after the end of treatment. Second round of treatment with Sunitinib remains efficacious against tumors that are not fully regressed during the first round of treatment. Sunitinib treatment results in significant decrease in tumor MVD, with ~40% reduction in SF763T glioma tumors. SU11248 treatment results in a complete inhibition of additional tumor growth of luciferase-expressing PC-3M xenografts, despite no reduction in tumor size. [2] Sunitinib treatment (20 mg/kg/day) dramatically suppresses the growth subcutaneous MV4;11 (FLT3-ITD) xenografts and prolongs survival in the FLT3-ITD bone marrow engraftment model. [3]

Protocol (from reference)

Kinase Assay:

[1]

  • Biochemical Tyrosine Kinase Assays:

    IC50 values for Sunitinib against VEGFR2 (Flk-1) and PDGFRβ are determined using glutathione S-transferasefusion proteins containing the complete cytoplasmic domain of the RTK. Biochemical tyrosine kinase assays to quantitate the trans-phosphorylation activity of VEGFR2 (Flk-1) and PDGFRβ are performed in 96-well microtiter plates precoated (20 μg/well in PBS; incubated overnight at 4 °C) with the peptide substrate poly-Glu,Tyr (4:1). Excess protein binding sites are blocked with the addition of 1-5% (w/v) BSA in PBS. Purified GST-fusion proteins are produced in baculovirus-infected insect cells. GST-VEGFR2 and GST-PDGFRβ are then added to the microtiter wells in 2 × concentration kinase dilution buffer consisting of 100 mM HEPES, 50 mM NaCl, 40 μM NaVO4, and 0.02% (w/v) BSA. The final enzyme concentration for GST-VEGFR2 or GST-PDGFRβ is 50 ng/mL. Twenty-five μL of diluted Sunitinib are subsequently added to each reaction well to produce a range of inhibitor concentrations appropriate for each enzyme. The kinase reaction is initiated by the addition of different concentrations of ATP in a solution of MnCl2 so that the final ATP concentrations spanned the Km for the enzyme, and the final concentration of MnCl2 is 10 mM. The plates are incubated for 5-15 minutes at room temperature before stopping the reaction with the addition of EDTA. The plates are then washed three times with TBST. Rabbit polyclonal antiphosphotyrosine antisera are added to the wells at a 1:10,000 dilution in TBST containing 0.5% (w/v) BSA, 0.025% (w/v) nonfat dry milk, and 100 μM NaVO4 and incubated for 1 hour at 37 °C. The plates are then washed three times with TBST, followed by the addition of goat antirabbit antisera conjugated with horseradish peroxidase (1:10,000 dilution in TBST). The plates are incubated for 1 hour at 37 °C and then washed three times with TBST. The amount of phosphotyrosine in each well is quantitated after the addition of 2,2′-azino-di-[3-ethylbenzthiazoline sulfonate] as substrate.

Cell Research:

[3]

  • Cell lines: RS4;11, MV4;11, and OC1-AML5
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 24 and 48 hours
  • Method:

    Cells are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay or trypan blue cell viability assays. Apoptosis is measured 24 hours after Sunitinib addition by Western blotting to detect cleavage of poly (ADP-ribose) polymerase (PARP) or levels of caspase-3.

Animal Research:

[2]

  • Animal Models: Female nu/nu mice implanted s.c. with HT-29, A431, Colo205, H-460, SF763T, C6, A375, or MDA-MB-435, and male nu/nu mice bearing luciferase-expressing PC-3M tumors
  • Dosages: ~80 mg/kg
  • Administration: Orally once daily

Solubility (25°C)

In vitro

DMSO 15 mg/mL
(28.16 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

2mg/mL

Chemical Information

Molecular Weight 532.56
Formula

C22H27FN4O2.C4H6O5

CAS No. 341031-54-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCN(CC)CCNC(=O)C1=C(NC(=C1C)C=C2C3=C(C=CC(=C3)F)NC2=O)C.C(C(C(=O)O)O)C(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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
NCT05043090 Recruiting Drug: savolitinib|Drug: durvalumab|Drug: sunitinib Papillary Renal Cell Carcinoma AstraZeneca October 28 2021 Phase 3
NCT04669366 Completed Drug: sunitinib|Drug: axitinib Kidney Neoplasms Pfizer January 20 2021 --
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
NCT04115189 Completed Drug: Sunitinib Metastatic Renal Cell Carcinoma ( mRCC) Pfizer December 13 2019 --
NCT04175262 Completed Drug: sunitinib Metastatic Renal Cell Carcinoma (mRCC) Pfizer|IMDC group|Analysis Group October 31 2019 --
NCT04033991 Completed Drug: Sunitinib|Drug: Axitinib Carcinoma|Renal Cell Pfizer September 27 2019 --

(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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Frequently Asked Questions

Question 1:
I was wondering that the compound is in its cis or trans form?

Answer:
S1042 Sunitinib Malate is Z form.

Question 2:
What is the difference between Sunitinib Malate(S1042) and Sunitinib(S7781)?

Answer:
S1042 is the Malate salt form of Sunitinib. The biological activities of these two compounds are the same but the solubility of these two compounds in aqueous solvent are different.

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