Sunitinib (SU11248) malate

For research use only. Not for use in humans.

Pfizer辉瑞授权 目录号:S1042 中文名称:苹果酸舒尼替尼

Sunitinib (SU11248) malate Chemical Structure

CAS No. 341031-54-7

Sunitinib (SU11248) malate是一种多靶点RTK抑制剂,作用于VEGFR2 (Flk-1)PDGFRβ,在无细胞试验中IC50分别为80 nM 和2 nM,也会抑制c-Kit的活性。Sunitinib Malate 可有效地抑制 Ire1α 的自身磷酸化。Sunitinib Malate 可增加 death receptor线粒体依赖的凋亡 mitochondrial-dependent apoptosis

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1565.28 现货
RMB 630.63 现货
RMB 876.33 现货
RMB 1204.22 现货
RMB 2104.83 现货
RMB 3652.98 现货
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客户使用Selleck生产的Sunitinib (SU11248) malate发表文献118篇:

产品安全说明书

PDGFR抑制剂选择性比较

生物活性

产品描述 Sunitinib (SU11248) malate是一种多靶点RTK抑制剂,作用于VEGFR2 (Flk-1)PDGFRβ,在无细胞试验中IC50分别为80 nM 和2 nM,也会抑制c-Kit的活性。Sunitinib Malate 可有效地抑制 Ire1α 的自身磷酸化。Sunitinib Malate 可增加 death receptor线粒体依赖的凋亡 mitochondrial-dependent apoptosis
靶点
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
体外研究

Sunitinib也是有效的c-Kit抑制剂,IC50为211 nM。[1] Sunitinib是有效的ATP竞争性VEGFR2 (Flk1)和PDGFRβ抑制剂, Ki 分别为9 nM和 8 nM,作用于VEGFR2和 PDGFR 比作用于FGFR-1, EGFR, Cdk2, Met, IGFR-1, Abl,和 src选择性高10多倍。Sunitinib 作用于血清饥饿处理的表达VEGFR2或PDGFRβ的NIH-3T3细胞, 抑制VEGF依赖的 VEGFR2磷酸化和 PDGF依赖的PDGFRβ磷酸化,IC50分别为10 nM和 10 nM。Sunitinib抑制VEGF诱导的血清饥饿处理的 HUVECs 增殖,IC50为40 nM, 且抑制PDGF诱导的过量表达PDGFRβ或 PDGFRα的NIH-3T3细胞,IC50分别为39 nM和 69 nM。[2] Sunitinib 抑制野生型FLT3, FLT3-ITD,和FLT3-Asp835磷酸化,IC50分别为250 nM, 50 nM, 和 30 nM。Sunitinib 抑制MV4;11和 OC1-AML5细胞增殖,IC50分别为8 nM 和4 nM, 且诱导凋亡,这种作用存在剂量依赖性。 [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
3T3 Mmm2T4lv[XOnIFHzd4F6 MlvrTY5pcWKrdHnvckBw\iCSRFfGMYlv\HWlZXSgRpJlXSCrbnPvdpBwemG2aX;uJJdqfGhiSVO1NEBw\iByLkCwO{DPxE1? NIPp[5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMk[0OlAyQSd-MUK2OFYxOTl:L3G+
3T3 MoflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJcohq[mm2aX;uJI9nKFCuYYTlcIV1NWSncnn2[YQh\3Kxd4ToJIZi[3SxcjDpcoR2[2WmIEPUN{Bk\WyuIIDyc4xq\mW{YYTpc44hf2m2aDDJR|UxKG:oIECuNFEh|ryP NGTvcWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMk[0OlAyQSd-MUK2OFYxOTl:L3G+
3T3 MWnGeY5kfGmxbjDBd5NigQ>? MmTQTY5pcWKrdHnvckBw\iCYYYPjeYxieiCnbnTveIhmdGmjbDDndo94fGhiZnHjeI9zKHKnY3XweI9zKHerdHigTWM2OCCxZjCwMlA2KM7:TR?= NF\S[pg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMk[0OlAyQSd-MUK2OFYxOTl:L3G+
3T3 MmfPT4lv[XOnIFHzd4F6 M3y3b|IxKG2rbh?= NGT0OoZFVVOR MmLJR4VtdHWuYYKgbY5pcWKrdHnvckBw\iCYRVfGJIlv\HWlZXSgbJVu[W5iS1TSJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOC5yMkKg{txO NVfFbYV2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[xOlIxODhpPkG2NVYzODB6PD;hQi=>
NIH3T3 NUfNZnVqU2mwYYPlJGF{e2G7 MkX1NlAhdWmw NFfqe2JFVVOR MXfpcohq[mm2IHj1cYFvKEuGUjDrbY5ie2ViZYjwdoV{e2WmIIfpeIghUUN3MDDv[kAxNjBzODFOwG0> MnHqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZzNkKwNFgoRjF4MU[yNFA5RC:jPh?=
A549 MV7GeY5kfGmxbjDBd5NigQ>? M4\ZdWROW09? M1jtR2lvcGmkaYTpc44hd2ZiYz3N[ZQh\GWyZX7k[Y51KEiJRj3pcoR2[2WmIHj1cYFvKEF3NEmgZ4VtdCCvaXfyZZRqd25id3n0bEBKSzVyIH;mJFIh|ryP NYO4Z4R5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi0N|QyPDVpPkG4OFM1OTR3PD;hQi=>
DU145 MnfrSpVv[3Srb36gRZN{[Xl? M1vtcWROW09? M3fZb2lvcGmkaYTpc44hd2ZiYz3N[ZQh\GWyZX7k[Y51KEiJRj3pcoR2[2WmIHj1cYFvKESXMUS1JINmdGxic3PheJRmemmwZzD3bZRpKEmFNUCgc4YhOTBizszN NFz2S4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOESzOFE1PSd-MUi0N|QyPDV:L3G+
KB3-1 NEX3OZlEgXSxdH;4bYMhSXO|YYm= MWG3NkBp NYCzdlR5TE2VTx?= M17SZ2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHAu\3BvbnXnZZRqfmViS1KtN{0yKGOnbHzzJJdqfGhiSVO1NEBw\iB{LkOg{txO NG[1fpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUO5O|MzOid-MUmzPVc{OjJ:L3G+
KBV1 MYLDfZRwfG:6aXOgRZN{[Xl? Mk\sO|IhcA>? M2KxUWROW09? NXnaTJJyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWC2pbInjc5Bzd3SnaX6t[ZhxemW|c3nu[{BMSlZzIHPlcIx{KHerdHigTWM2OCCxZjC0MlEh|ryP NG\Td4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUO5O|MzOid-MUmzPVc{OjJ:L3G+
A375 NVnoTIlKS3m2b4TvfIlkKEG|c3H5 M{Xp[lczKGh? MWrEUXNQ NVvp[Gp6UUN3ME21MlQh|ryP MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ3NESwPEc,OTl4NUS0NFg9N2F-
RS4-11 Ml7TSpVv[3Srb36gRZN{[Xl? MYiyJIg> NI\aNGZKdmirYnn0bY9vKG:oIF\MWFMh[XW2b4Doc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gNE4xODl7IN88US=> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTZ3NESwPEc,OTl4NUS0NFg9N2F-
RS4-11 MX7GeY5kfGmxbjDBd5NigQ>? NGDOeFYzKGh? M2PTZWlvcGmkaYTpc44hd2ZiRlzUN{BKXERibYX0ZY51KGG3dH;wbI9{eGixconsZZRqd25id3n0bEBKSzVyIH;mJFAvODN2IN88US=> NWDHN|Y3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm2OVQ1ODhpPkG5OlU1PDB6PD;hQi=>
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Ba/F3 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[5O|IhcA>? MnHMTWM2OD1zLkKg{txO M2foVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMUG3NFA1Lz5{MEGxO|AxPDxxYU6=
BaPTC2 NVvHbYxrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX63NkBp MoDjTWM2OD1yLkKyJO69VQ>? NV74cYw4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxNVcxODRpPkKwNVE4ODB2PD;hQi=>
Sf9 NWnjbFNUTnWwY4Tpc44hSXO|YYm= NYXW[4ZsOSCq MnfzSG1UVw>? Mo\KTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCKaYOteIFo\2WmIGLFWEBmgHC{ZYPz[YQhf2m2aDDJR|UxKG:oIEGuN{DPxE1? NU\xVpNkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxNVcxODRpPkKwNVE4ODB2PD;hQi=>
H4 M2fZb2N6fG:2b4jpZ{BCe3OjeR?= MYWxNEDPxE1? MonWWI95cWOrdImgbY4hcHWvYX6gTFQh[2WubIO= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODN3MEiwOkc,OjB|NUC4NFY9N2F-
SF-539 NXHZOGZJU2mwYYPlJGF{e2G7 MmjjN|M{KM7:TR?= NX;ZSlZrPjBibXnu MWjEUXNQ NYfxRnVDUW6qaXLpeIlwdiCxZjDQSGdHWmKndHGgdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAyOi5{IN88US=> NH3PTpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MESwN|cxOCd-MkC0NFM4ODB:L3G+
U251 Ml3YT4lv[XOnIFHzd4F6 NXzt[3RqOzN|IN88US=> MYm2NEBucW5? NHj2XW5FVVOR MYHJcohq[mm2aX;uJI9nKF[HR1\SNkBxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDF6Lkmg{txO Mn;PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB2MEO3NFAoRjJyNECzO|AxRC:jPh?=
A431 MWjLbY5ie2ViQYPzZZk> M{nZOGlvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIHX4dJJme3OnZDD3bZRpKEmFNUCgc4YhOTJwMjFOwG0> MkHuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB3NUiwO|IoRjJyNUW4NFczRC:jPh?=
A431 NGnWbI9McW6jc3WgRZN{[Xl? NIP2UGFKdmirYnn0bY9vKG:oIG\FS2ZTOiCneIDy[ZN{\WRid3n0bEBKSzVyIH;mJFE5NjlizszN NFe4Smk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEW1PFA4Oid-MkC1OVgxPzJ:L3G+
HepG2 M2fWVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\MclczKGh? NWrkd|NyUUN3ME2zMlgyKM7:TR?= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODV5MEWyOkc,OjB3N{C1NlY9N2F-
Kasumi-1 MlvVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XsVlczKGh? Ml\qTWM2OD1yLkCxOkDPxE1? NWPUNmtFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC1O|A2OjZpPkKwOVcxPTJ4PD;hQi=>
RS4-11 NVPIdnI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zwc|czKGh? NF3IXYpKSzVyPUGg{txO NHrZeZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEW3NFUzPid-MkC1O|A2OjZ:L3G+
THP1 NV7oUYFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2ntNlczKGh? NH\R[WhKSzVyPUCuOUDPxE1? M3HROVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNUewOVI3Lz5{MEW3NFUzPjxxYU6=
Kasumi-1 MmThSpVv[3Srb36gRZN{[Xl? NX\UboN6UW6qaXLpeIlwdiCxZjDjMWtqfCCjdYTvdIhwe3Cqb4L5cIF1cW:wIIfpeIghUUN3MDDv[kAxNjBzNTFOwG0> NGHhbpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEizN|A{QSd-MkC4N|MxOzl:L3G+
A549 M4\NTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGT2emgyPiCq M4ezcGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIO= Mn\RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2NUC0OlMoRjJzNEWwOFY{RC:jPh?=
HL60 NWPhW|VjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITlZYEyPiCq MoDDRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\Wyucx?= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTR3MES2N{c,OjF2NUC0OlM9N2F-
HUVEC MniwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPvNVYhcA>? MWTJcohq[mm2aX;uJI9nKF[HR1[tbY5lfWOnZDDj[YxtKHC{b3zp[oVz[XSrb36ge4l1cCCLQ{WwJI9nKDJwN{Wg{txO M2TZUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNEWwOFY{Lz5{MUS1NFQ3OzxxYU6=
HUVEC NG\UVoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1n3VlE3KGh? NWOyTnhyUW6qaXLpeIlwdiCxZjDiSmdHNWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKHerdHigTWM2OCCxZjC0MlA1KM7:TR?= MkfqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2NUC0OlMoRjJzNEWwOFY{RC:jPh?=
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K562 NVjVfJJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\5XnAyPiCq MmDkRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\Wyucx?= MoTuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF2NUC0OlMoRjJzNEWwOFY{RC:jPh?=
MDA-MB-231 M37m[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnYU3MyPiCq MUTBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{ NUH2[Gx3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG0OVA1PjNpPkKxOFUxPDZ|PD;hQi=>
H460 M{H5UGN6fG:2b4jpZ{BCe3OjeR?= M1LxeVczKGh? MY\JR|UxRTJwNzFOwG0> NFT6NZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MU[yNVg5OCd-MkG2NlE5QDB:L3G+
SMMC7721 MUTDfZRwfG:6aXOgRZN{[Xl? M3zW[lczKGh? NInxS3BKSzVyPU[uOFch|ryP NYmySYlvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG2NlE5QDBpPkKxOlIyQDhyPD;hQi=>
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A431 M1PwWWtqdmG|ZTDBd5NigQ>? NFO5dI8yOCEQvF2= MUexJIg> NGrC[4xFVVOR NXzuN45{UW6qaXLpeIlwdiCxZjDFS2ZTKHerdHigTWM2OCCxZjCwMlE4OjFizszN NX6wb3htRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PVA3PTJpPkK0PFkxPjV{PD;hQi=>
SH-SY5Y M4K5SWtqdmG|ZTDBd5NigQ>? NIXjfWQyOCEQvF2= NHPWXowyKGh? NEnEWFlFVVOR M{fLN2lvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIIfpeIghUUN3MDDv[kAxNjB6M{Gg{txO MojwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OUC2OVIoRjJ2OEmwOlUzRC:jPh?=
U251 NFrtb5BMcW6jc3WgRZN{[Xl? MX[xNEDPxE1? M3jL[lEhcA>? NYXOfW86TE2VTx?= MnLlTY5pcWKrdHnvckBw\iCYRVfGVlIhf2m2aDDJR|UxKG:oIECuNFE5QSEQvF2= MoHPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OUC2OVIoRjJ2OEmwOlUzRC:jPh?=
Bel7402 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;oOFczKGh? NVjnUpMzTE2VTx?= MUjJR|UxRTJwNkeg{txO NFf3cW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwOFk3OSd-MkS5NFQ6PjF:L3G+
HK2 NF3Eb2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXPO|IhcA>? M33lSWROW09? NGrEUXZKSzVyPUWuPFUh|ryP MkPrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MES5OlEoRjJ2OUC0PVYyRC:jPh?=
LO2 NYjlfWtIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33INlczKGh? NWj2TIdtTE2VTx?= NG\lVVFKSzVyPUG5Mlk{KM7:TR?= NWLT[pBbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFQ6PjFpPkK0PVA1QTZzPD;hQi=>
MV4-11 NILhdoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUK0PEBp NU[4ZoNXTE2VTx?= M4LEXmlEPTB;MD6wNFMh|ryP M3fOe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUC0PVYyLz5{NEmwOFk3OTxxYU6=
NCI-H3122 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrTdGc4OiCq MVPEUXNQ MlrwTWM2OD1yLkizJO69VQ>? M1LmPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUC0PVYyLz5{NEmwOFk3OTxxYU6=
NCI-H460 NGX1WGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LrUFczKGh? MXPEUXNQ MWTJR|UxRTRwM{Gg{txO MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyNEm2NUc,OjR7MES5OlE9N2F-
NCI-H526 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjyTXo4OiCq MV3EUXNQ MWfJR|UxRTFwMEGg{txO NUjac2NxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFQ6PjFpPkK0PVA1QTZzPD;hQi=>
TT NWPSXolWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTD[YI4OiCq NHjxUoFFVVOR NH7ESFdKSzVyPUCuNFQh|ryP M4W4TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUC0PVYyLz5{NEmwOFk3OTxxYU6=
3T3 NVv6Wo5MSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NVe5R|ZWPzJiaILz MknDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SB|VEOgZ4VtdHNiZYjwdoV{e2mwZzDoeY1idiCFU1[xVkBi\nSncjC3NkBpenNiYomgR4VtdHSrdHXyJIF{e2G7LDDBZ5Rqfmm2eTC9JFAvODlizszNMi=> NYjSOnVQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi2PVQ3PDFpPkG4Olk1PjRzPD;hQi=>
MV4-11 NFL0T4JCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M1nqe|czKGi{cx?= NEHPTXFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3WOE0yOSClZXzsd{Bi\nSncjC3NkBpenNiYomgZ4VtdCC2aYTldk1jdHWnIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gNE4xODR|IN88UU4> NITLRnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe1OFE6QSd-MUm3OVQyQTl:L3G+
HEK293 NX7xTHFtTnWwY4Tpc44h[XO|YYm= MmfCRolv\GmwZzDh[oZqdmm2eTD0c{BHVFR|IHPheIFtgXSrYzDkc41icW5iZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCkeTDjc41x\XSrdHn2[UBjcW6maX7nJIF{e2G7LDDL[EA:KDBwMECwOFch|ryPLh?= M4LIeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{W0NVk6Lz5zOUe1OFE6QTxxYU6=
FDC-P1 M3zvO2Z2dmO2aX;uJIF{e2G7 NVTsVohnPDhiaILz MorCTY5pcWKrdHnvckBw\iCqdX3hckBHVVNiZYjwdoV{e2WmIHnuJIdzd3e2aDDmZYN1d3JiZHXw[Y5l\W62IH3veZNmKE[GQz3QNUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIF\NV{1u\WSrYYTl[EBk\WyuIIDyc4xq\mW{YYTpc44hcW5icILld4Vv[2ViaIXtZY4hS1OIMTDh[pRmeiB2ODDodpMh[nlicnXzZZp2emmwIHT5[UBz\WS3Y4Tpc44h[XO|YYmsJGlEPTBiPTCwMlE2PSEQvF2u Mly5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjBzNU[2PFkoRjJyMUW2Olg6RC:jPh?=
primary leukemia cells MnW5R5l1d3SxeHnjbZR6KGG|c3H5 MkiwO|IhcHK| M4eyRWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJJBzcW2jcomgcIV2c2WvaXGgZ4VtdHNiaYPvcIF1\WRiZoLvcUBi[3W2ZTDtfYVtd2mmIHzleYtmdWmjIIDheIlmdnRiZYjwdoV{e2mwZzDGUHQ{NUmWRDDteZRifGmxbjDhd5Nme3OnZDDhd{Bk\WyuII\pZYJqdGm2eTDh[pRmeiB5MjDodpMh[nlibIXjbYZmemG|ZTDhd5NigSxiSVO1NEA:KDBwMEOg{txONg>? NHvLeII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkKyNVIxOSd-MkKyNlEzODF:L3G+
primary leukemia cells M17vNmN6fG:2b4jpZ4l1gSCjc4PhfS=> MWO3NkBpenN? NHj0bGpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBxemmvYYL5JIxmfWunbXnhJINmdGy|IHnzc4xifGWmIH\yc40h[WO3dHWgcZlmdG:rZDDs[ZVs\W2rYTDwZZRq\W62IHX4dJJme3Orbnege4lt\CC2eYDlJGZNXDNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KGy3Y3nm[ZJie2ViYYPzZZktKEmFNUCgQUAxNjB|IN88UU4> MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ{MUKwNUc,OjJ{MkGyNFE9N2F-
primary leukemia cells MnXkR5l1d3SxeHnjbZR6KGG|c3H5 Ml3XO|IhcHK| M3voTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJJBzcW2jcomgcIV2c2WvaXGgZ4VtdHNiaYPvcIF1\WRiZoLvcUBi[3W2ZTDtfYVtd2mmIHzleYtmdWmjIIDheIlmdnRiZYjwdoV{e2mwZzDGUHQ{NUR6M{XZJI12fGG2aX;uJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5JIFnfGW{IEeyJIhzeyCkeTDseYNq\mW{YYPlJIF{e2G7LDDJR|UxKD1iMT6xJO69VS5? MlPqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{MkGyNFEoRjJ{MkKxNlAyRC:jPh?=
endothelial precursor cells NUD2UW4xTnWwY4Tpc44h[XO|YYm= Mon0TY5pcWKrdHnvckBw\iCnbnTveIhmdGmjbDDjc5JlKGG{ZXGg[o9zdWG2aX;uJIlvKGWwZH;0bIVtcWGuIIDy[YN2enOxcjDj[YxteyCkeTDDSFMyKGOxcnSgZZJm[SCmZYTlZ5Rqd25iYnHz[YQheGinbn;0fZBq[yCmcoXnJIRqe2OxdnXyfUBj[XOnZDDhd5NigSxiSVO1NEA:KDBwMEC5OkDPxE1w M3TUT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEC5OlY3Lz5{MkSwPVY3PjxxYU6=
endothelial precursor cells M3jhbGZ2dmO2aX;uJIF{e2G7 MXrJcohq[mm2aX;uJI9nKGOnbHygcYloemG2aX;uJIlvKGWwZH;0bIVtcWGuIIDy[YN2enOxcjDj[YxteyCkeTDPdol{KGOnbHygcYloemG2aX;uJItqfCCkYYPl[EBxcGWwb4T5dIlkKGS{dXeg[Il{[2:4ZYL5JIJie2WmIHHzd4F6NCCLQ{WwJF0hOTNwNjFOwG0v M3XwfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEC5OlY3Lz5{MkSwPVY3PjxxYU6=
U251 NHTGOXBHfW6ldHnvckBie3OjeR?= M2DnWFYxKG2rboO= NWLRSnB[UW6qaXLpeIlwdiCxZjDWSWdHWjJiaX6gbJVu[W5iVUK1NUBk\WyuczDwdoV1emWjdHXkJIZweiB4MDDtbY5{KG2nYYP1doVlKGGodHXyJFEhcHJiYomgSWxKW0FuIFnDOVAhRSBzOD65JO69VS5? Ml20QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ5M{mwPVAoRjJ{N{O5NFkxRC:jPh?=
U251 MVrGeY5kfGmxbjDhd5NigQ>? NFjZe5o3OCCvaX7z MWjJcohq[mm2aX;uJI9nKF[HR1[tbY5lfWOnZDDWSWdHWjJicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFV{NUGgZ4VtdHNib4\ldoV5eHKnc4PpcochTmytLUGgdJJmfHKnYYTl[EBnd3JiNkCgcYlveyCycnnvdkB1dyCYRVfGJIFl\Gm2aX;uJI1m[XO3cnXkJIFnfGW{IEGwJI1qdnNiYomgdIhwe3Cqb4T5do9{cW6nIFXMTXNCKGO7dH;icI91KGGwYXz5d4l{NCCLQ{WwJF0hOThwOTFOwG0v MnSwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|N{WwPVAoRjJ|M{e1NFkxRC:jPh?=
U251 NXXMSohkTnWwY4Tpc44h[XO|YYm= NHjHNoE3OCCvaX7z MWnJcohq[mm2aX;uJI9nKF[HR1\SNkBqdiCqdX3hckBWOjVzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhXkWJRj3pcoR2[2WmIIT5do9{cW6nIIDoc5NxcG:{eXzheIlwdiCrbnP1ZoF1\WRiZn;yJFYxKG2rboOgdJJqd3JidH:gWmVITi2jY4TpeoF1cW:wIH3lZZN2emWmIEGwJI1qdnNiYomgSWxKW0FuIFnDOVAhRSBzOD65JO69VS5? M3fBOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NEO0NVM6Lz5{M{SzOFE{QTxxYU6=
CHO NYGyTXFSTnWwY4Tpc44h[XO|YYm= M33PSmlvcGmkaYTpc44hd2ZiQ3H2NU4zKGO3coLlcpQhdWWjc4Xy[YQhfXOrbnegVXBifGOqIHH1eI9u[XSrYzDwZZRpKGOuYX3wJJN6e3SnbTDpckBEUE9iY3XscJMh\XiycnXzd4lv\yCFYY[xMlItKGKndHGtNkBidmRiYXzwbIEuOi:mZXz0ZU0yKHO3YoXubZR{NCCLQ{WwJF0hOzNwNDFOwG0v M{HjVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEGyOVA{Lz5{M{ixNlUxOzxxYU6=
U251 M1PlfmZ2dmO2aX;uJIF{e2G7 M{XQ[2lvcGmkaYTpc44hd2ZiVlXHSnIzKGmwIHj1cYFvKFV{NUGgZ4VtdHNiYomgdIhwe3Cqb4T5do9{cW6nIFXMTXNCNCCLQ{WwJF0hOC5yMUi5JO69VS5? M2r3fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwPFY2Lz5{NEmwNFg3PTxxYU6=
MCF7 MmfVRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NUCyTJhyPDhiaILz MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDFyLkWg{txONg>? NV:1eZJrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlQ{PDdpPkK1NFY1OzR5PD;hQi=>
HepG2 NELq[JRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NEjHSlc1QCCqcoO= NWD1e455SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNVMvPiEQvF2u Mnz4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNkSzOFcoRjJ3ME[0N|Q4RC:jPh?=
CHO MVrGeY5kfGmxbjDhd5NigQ>? MmnZTY5pcWKrdHnvckBw\iC{YYDp[EBl\WyjeXXkJIlvf2G{ZDDy[YN1cW[7aX7nJJBwfGG|c3n1cUBkfXK{ZX70JEhKU3JrIHnuJGNpcW6nc3WgbIFue3SncjDveoFzgSBqQ1jPLUBk\WyuczDzeIFjdGViZYjwdoV{e2mwZzDoSXJIKG2nYYP1doVlKHW|aX7nJGlwdlexcnvzJGJienKjY4XkZUBifXSxbXH0[YQheGG2Y3igZ4xidXBicHzheIZwem1uIFnDOVAhRSB5Lkm0N|I5KM7:TT6= MofNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOEe3OVMoRjJ3MEi3O|U{RC:jPh?=
CHO K1 NVrTbIo6TnWwY4Tpc44h[XO|YYm= M365OmlvcGmkaYTpc44hd2ZicnHwbYQh\GWuYYnl[EBqdnejcnSgdoVkfGmoeXnu[{Bxd3Sjc4PpeY0h[3W{cnXueEApUUu{KTDpckBEcGmwZYPlJIhidXO2ZYKgc5ZienliKFPIU{khUzFiY3XscJMhe3SjYnz5JIV5eHKnc4PpcochcEWURzDt[YF{fXKnZDD1d4lv\yCLb37Xc5JseyCTdXH0eJJwKGG3dH;tZZRm\CCyYYTjbEBkdGGvcDDwcIF1\m:{bTygTWM2OCB;IEGwJO69VS5? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB6N{e1N{c,OjVyOEe3OVM9N2F-
CHO K1 NUnq[WJKTnWwY4Tpc44h[XO|YYm= MUTJcohq[mm2aX;uJI9nKG[jc4Sgd49lcXWvIHP1dpJmdnRiKFnOZUkhcW5iQ3jpcoV{\SCKYX3zeIVzKE:4YYL5JEhEUE9rIFuxJINmdGy|IITyZY5{\mWldHXkJJdqfGhiaIXtZY4hVmG4MT61JI1m[XO3cnXkJJV{cW6pIFnvcndwemu|IGH1ZZR1em9iYYX0c41ifGWmIIDheINpKGOuYX3wJJBt[XSob4LtMEBKSzVyIE2gNVUvQDR6OTFOwG0v NXHQd4hKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwPFc4PTNpPkK1NFg4PzV|PD;hQi=>
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SK-UT-1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\Pd4pZUUN3ME20PU45QDJ3IN88US=> NEWx[HM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2OzVxJ{7TRW5ITVJ:L3G+

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Assay
Methods Test Index PMID
Western blot
p-STAT3 / STAT3 / p-Src / Src / p-AKT / AKT / p-ERK / ERK ; 

PubMed: 19244102     


Sunitinib reduced Stat3 and Src activity, with no dramatic reduction of AKT, MAPK and JAK signaling in 786-O cells. Tumor cells were treated with sunitinib at indicated concentrations for 2 h (left panels) or 24 h (right panels). Total cell lysates were prepared and western blots were performed using relevant antibodies to detect total protein levels, with β-actin used as the loading control.

p-GSK3β / GSK3β / MYCN ; 

PubMed: 24759734     


Effect of sunitinib on GSK3β phosphorylation and on MYCN total protein in MYCN amplified NB cell lines.

p-AKT / AKT / p-ERK / ERK; 

PubMed: 24759734     


Effect of 72 h treatment with sunitinib on SH-SY5Y, SK N BE(2), SK-N-AS and IMR-32 NB cell lines analyzed by Western blot with pSer473Akt, Akt, pThr202/Thr204 Erk1/2 and Erk1/2 antibodies. β-actin was used as a loading control.

19244102 24759734
Growth inhibition assay
Cell viability; 

PubMed: 24369536     


Isolated effects of sunitinib malate on urinary bladder-cancer cell lines viability, assessed by using the MTT assay. The data shown and bars represent the mean values ± SD (SD: standard deviation). *P < 0.05 versus untreated cells.

24369536
体内研究

与体内大量且选择性抑制VEGFR2或PDGFR磷酸化和信号相一致, Sunitinib每天按 20-80 mg/kg 剂量处理多种移植瘤模型,包括HT-29, A431, Colo205, H-460, SF763T, C6, A375,或 MDA-MB-435,具有广泛且有效的抗癌活性,这种作用存在剂量依赖性。Sunitinib 每天按 80 mg/kg剂量处理,持续21天,使八只鼠中有六只肿瘤完全衰退,且在处理结束后,观察110天,肿瘤不会复发。使用 Sunitinib进行第二轮处理,仍然高效作用于第一轮没有完全衰退的肿瘤。Sunitinib处理SF763T胶质瘤,导致肿瘤MVD显著降低,降低~40%。SU11248 处理,完全抑制表达荧光素酶的PC-3M移植瘤生长,而肿瘤尺寸没有减小。[2] Sunitinib 每天按20 mg/kg剂量处理,显著阻断皮下MV4;11 (FLT3-ITD)移植瘤生长,且作用于FLT3-ITD骨髓移植瘤模型,抑制延长的寿命。[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)

激酶实验:

[1]

- 合并

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.
细胞实验:

[3]

- 合并
  • Cell lines: RS4;11, MV4;11, 和 OC1-AML5
  • Concentrations: 溶于DMSO,终浓度为~10 μM
  • Incubation Time: 24 和48 小时
  • Method:

    细胞在含0.1% FBS 的培养基上饥饿处理过夜,然后加入Sunitinib和 FL (50 ng/mL; FLT3-WT)。培养48小时后,使用 Alamar Blue 检测或台酚蓝细胞活力检测测定增殖。加入Sunitinib 24小时后,测量凋亡,通过Western blotting测定caspase-3水平的PARP分裂。


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: 皮下移植 HT-29, A431, Colo205, H-460, SF763T, C6, A375,或 MDA-MB-435的雌性nu/nu小鼠,携带表达荧光素酶 PC-3M肿瘤的雄性nu/nu小鼠
  • Dosages: ~80 mg/kg
  • Administration: 口服处理,每天一次
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 15 mg/mL (28.16 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4% DMSO+30% PEG 300+ddH2O
2mg/mL

* 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 532.56
化学式

C22H27FN4O2.C4H6O5

CAS号 341031-54-7
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
NCT04669366 Recruiting 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. November 25 2020 Phase 2
NCT04115189 Completed Drug: Sunitinib Metastatic Renal Cell Carcinoma ( mRCC) Pfizer December 13 2019 --
NCT03916458 Completed -- Carcinoma Renal Cell Pfizer December 17 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 --

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

常见问题及建议解决方法

  • 问题 1:

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

  • 回答:

    S1042 Sunitinib Malate is Z form.

  • 问题 2:

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

  • 回答:

    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.

PDGFR Signaling Pathway Map

PDGFR Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID