Bosutinib (SKI-606)

For research use only.

Licensed by Pfizer Catalog No.S1014

99 publications

Bosutinib (SKI-606) Chemical Structure

CAS No. 380843-75-4

Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.

Selleck's Bosutinib (SKI-606) has been cited by 99 publications

Purity & Quality Control

Choose Selective Src Inhibitors

Biological Activity

Description Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.
Targets
S6 kinase [7]
()
ERK [7]
()
STAT3 [7]
()
Abl [2]
(Cell-free assay)
Src [1]
(Cell-free assay)
1 nM 1.2 nM
In vitro

Bosutinib is selective for Src over non-Src family kinases with an IC50 of 1.2 nM, and potently inhibits Src-dependent cell proliferation with an IC50 of 100 nM. [1] Bosutinib significantly inhibits the proliferation of Bcr-Abl-positive leukemia cell lines KU812, K562, and MEG-01 but not Molt-4, HL-60, Ramos, and other leukemia cell lines, with IC50 of 5 nM, 20 nM and 20 nM, respectively, more potently than that of STI-571. Similar to STI-571, Bosutinib displays antiproliferative activity against the Abl-MLV-transformed fibroblasts with IC50 of 90 nM. Bosutinib ablates tyrosine phosphorylation of Bcr-Abl and STAT5 in CML cells and of v-Abl expressed in fibroblasts at the concentration of ~50 nM, 10-25 nM and 200 nM, respectively, leading to the Bcr-Abl downstream signaling inhibition of Lyn/Hck phosphorylation. [2] Although unable to inhibit the proliferation and survival of breast cancer cells, Bosutinib significantly decreases the motility and invasion of breast cancer cells with IC50 of ~250 nM, involved with an increase in cell-to-cell adhesion and membrane localization of β-catenin. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NB7 NEi2WWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;ZRm5pUUN3ME2wMlA5OjNzIDFOwG0> M2DU[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
SW756 M2XDU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfxNJZjUUN3ME2wMlE1ODJ2IDFOwG0> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
CTV-1 M1jl[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XvS2lEPTB;MD6xOlM6QCBizszN NHPWOVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
HSC-4 MmG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXu3fGVCUUN3ME2wMlE4OTV6IDFOwG0> M4S4d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
LAMA-84 M4nCcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjZbWJKSzVyPUCuNlg3PjRiIN88US=> NH:2Zo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
KU812 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nTfmlEPTB;MD6zOFA3QCBizszN MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
HCC1806 NIPSZlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zpTWlEPTB;MD6zOVIyPiBizszN MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
DOK NXvtdnNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jJRmlEPTB;MD6zO|c5PiBizszN MmnTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
NCI-H209 MmTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\DWnZKSzVyPUCuOFA5ODhiIN88US=> NULqZpNkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjh6NESxM{c,W0GQR1XSQE9iRg>?
EoL-1-cell NWX5eJFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVO4RmI3UUN3ME2wMlQyPTd4IDFOwG0> NW\EZohSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjh6NESxM{c,W0GQR1XSQE9iRg>?
H9 NVXsRZNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTBwNEO0OlQhKM7:TR?= M2PMRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
EM-2 NXzZVYNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTBwNEO4PUAh|ryP MoHuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
NCI-H292 M1LmfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInJNlVKSzVyPUCuOFQyODhiIN88US=> NGjPVW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
697 MkHaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlK5TWM2OD1yLkS1OlM{KCEQvF2= NEnkW2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
BHT-101 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjTTWM2OD1yLkS2OVkhKM7:TR?= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
BE-13 NWHCNIQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3Rb4lKSzVyPUCuOFg2PzJiIN88US=> MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
RS4-11 NYPmS|d3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fpeWlEPTB;MD60PFU5PCBizszN NHywNGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
IGROV-1 NYj5[Y5jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DkfmlEPTB;MD60PFc6PyBizszN NWDXe5M4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjh6NESxM{c,W0GQR1XSQE9iRg>?
KE-37 NHPUUG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\JfldKSzVyPUCuOFk2ODliIN88US=> NEXtNWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
BV-173 NVrZV|hvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4e4d2lEPTB;MD61NFc6OiBizszN M2DZWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
MEG-01 NIH6XmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknKTWM2OD1yLkWxNlE1KCEQvF2= Mn7TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
LB2241-RCC MmfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTBwNUO3NVghKM7:TR?= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
ACHN M4S4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnQPIRvUUN3ME2wMlU1ODZ7IDFOwG0> NH7MOIs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
CTB-1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzpc2JKSzVyPUCuOVQ5OiBizszN NIflOpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
HT-1080 NIDhVHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrsSmZZUUN3ME2wMlU2OzR7IDFOwG0> NFrvT3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
CHL-1 NGHCXINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\UVpkzUUN3ME2wMlU2PDZ3IDFOwG0> NXG1T3N{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjh6NESxM{c,W0GQR1XSQE9iRg>?
EW-3 NEL1WWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvlOVlKSzVyPUCuOVU6OzViIN88US=> MmLRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
ES1 M2rQWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFK5fVNKSzVyPUCuOlc1QThiIN88US=> NF3QVmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
KASUMI-1 NF[xeFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmm3TWM2OD1yLkeyN|MhKM7:TR?= Mmj1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
SW13 NFi5bIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LjWGlEPTB;MD63N|c6QCBizszN NXfHOY1vRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjh6NESxM{c,W0GQR1XSQE9iRg>?
A3-KAW NFXhW45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjB[5FKSzVyPUCuO|kzODhiIN88US=> M3HqZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
LB771-HNC NHWycVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXVTWM2OD1yLkizNVA1KCEQvF2= M1jJXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
OC-314 NYjYbnRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDrO4VKSzVyPUCuPFY6PjViIN88US=> NYi1VmxERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjh6NESxM{c,W0GQR1XSQE9iRg>?
MLMA MlHBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHSbIdKUUN3ME2wMlkxPjd3IDFOwG0> NWHPPVBORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjh6NESxM{c,W0GQR1XSQE9iRg>?
KARPAS-45 NUXx[FlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTBwOUK0OlYhKM7:TR?= NE\PW2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
CAL-27 NGG3fpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTBwOUK5NFYhKM7:TR?= M3[4bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
SK-NEP-1 MlTMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTBwOUeyOFghKM7:TR?= M3fieVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
COR-L105 NIrvfFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPaSXVKSzVyPUGuNFA{QTRiIN88US=> M2joe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
TI-73 M{nE[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjFTWM2OD1zLkCxOlUhKM7:TR?= Mof0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
JVM-3 M1\UVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnnS2oyUUN3ME2xMlA2ODF5IDFOwG0> NH7Zc289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK|5USU6JRWK8M4E,
HAL-01 Mnz0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoPFTWM2OD1zLkC4PFEhKM7:TR?= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
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HSC-3 NEjzdmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDRTWM2OD1zLkGxO|g{KCEQvF2= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
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SW954 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LNUmlEPTB;MT61OVAxPyBizszN M3;UblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
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HT-1376 NWrBbFRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nzT2lEPTB;MT62OFM3KCEQvF2= MnSzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlg5PDRzLze+V2FPT0WUPD;hQi=>
CAL-54 Mn\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkD1TWM2OD1zLk[1O|A6KCEQvF2= M2fOXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
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EFO-27 NVezflN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTFwNki5NkAh|ryP MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
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NCI-H526 NIXBPJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTFwOUmzNlUhKM7:TR?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
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OVCAR-4 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fmV2lEPTB;Mj6wNFQ{PSBizszN MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
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HepG2 NY\iZYMySW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MoXkOFghcHK| MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKDR6IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBIUTVyIE2gNU4yPSEQvF2u NITZVI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOES4OVcyPSd-MUi0PFU4OTV:L3G+
HT29 M3nHPGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MnzqOFghcHK| MmLMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVEK5JINmdGy|IHHmeIVzKDR6IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBIUTVyIE2gNU4yPyEQvF2u MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDR6NUexOUc,OTh2OEW3NVU9N2F-
BA/F3 MmnZR5l1d3SxeHnjbZR6KGG|c3H5 NW\Tfph[PzJiaILz MnX5R5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCEQ2KtRWJNKFR|MUXJJI12fGGwdDDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMz6yJO69VS5? NYHYb2lwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4NVQ5QTBpPkK2PFE1QDlyPD;hQi=>
HeLa NE[1XXNHfW6ldHnvckBie3OjeR?= NVnod5pWPC53IHjydy=> MkXiTY5pcWKrdHnvckBw\iCHYn;sZZZqenW|IHfsfYNweHKxdHXpck9u[XS{aYigdJJwfGWrbjDWVFQxKGWwdIL5JIlvKGi3bXHuJGhmVGFiY3XscJMh[W[2ZYKgOE42KGi{czDi[ZRiNWyjY4ThcYF{\SC{ZYDvdpRmeiCjc4PhfUwhUUN3MDC9JFMvQDVizszNMi=> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ{NEO4O{c,Ojl4MkSzPFc9N2F-
HT29 M4PhUGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M1[yVlQ5KGi{cx?= NH60ZZJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUNlkh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEmFNUCgQUA{Njh5IN88UU4> NEC1c5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOES4OVcyPSd-MUi0PFU4OTV:L3G+
HepG2 M3:zTmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MoLHOFghcHK| MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKDR6IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBKSzVyIE2gN{46OSEQvF2u M2SxbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NEi1O|E2Lz5zOES4OVcyPTxxYU6=
HT29 NGTzSXJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NVXX[2JMPDhiaILz MlLlRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVEK5JINmdGy|IHHmeIVzKDR6IHjyd{BjgSC|dXzmc5Jpd2SjbXnu[UBDKGG|c3H5MEBVT0liPTC2MlUh|ryPLh?= NIjaTIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOES4OVcyPSd-MUi0PFU4OTV:L3G+
HepG2 MljrRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NWHWd3N5PDhiaILz M3LNTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZYZ1\XJiNEigbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKFSJSTC9JFcvPjZizszNMi=> NVXZcXRLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi0PFU4OTVpPkG4OFg2PzF3PD;hQi=>
Ba/F3 M2jhcmNmdGxiZHXheIgh[XO|YYm= NV\tUJM{UW6mdXP0bY9vKG:oIHPlcIwh\GWjdHigc4YhdXW{aX7lJGJiTjNiY3XscJMh\XiycnXzd4lv\yCQUF2vRWxMKEx{NU\UJI12fGGwdDDifUB1enmyYX6gZox2\SCneHPseZNqd25iYYPzZZk> NI\hdpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNkm3NFQxOCd-MU[5O|A1ODB:L3G+
A673 NVnwXFFPeUiWUzDhd5NigQ>? NIPYS2JyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= M2f0dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
DAOY NWfydHFreUiWUzDhd5NigQ>? NEXDcJlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= NW\iZpJzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 NF\KWpJyUFSVIHHzd4F6 MUPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| NX;VRYF2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD NI[5eXRyUFSVIHHzd4F6 MofhdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ Mm\4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 M3HkNJFJXFNiYYPzZZk> MUXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| M1Lvc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC NYnIc2xTeUiWUzDhd5NigQ>? NV7kTppjeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NI\ISIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Src / Src / p-c-Abl / c-Abl / p-S6 / S6 / p-ERK / ERK / p-STAT3 / STAT3; 

PubMed: 27903968     


IMR-32, NB-19, SH-SY5Y, and SK-N-AS cells were treated with indicated concentrations of bosutinib for 0-8 hrs and the cells were lysed and subjected to immunoblotting with the indicated antibodies. β-Actin was used as a loading control in all experiments.

p-FAK / FAK / p-Pyk2 / p-p130Cas / p-AKT; 

PubMed: 18483306     


Western blot analysis of MDA-MB-468 whole cell extracts. Cells were treated with SKI-606 or 0.01% DMSO at the indicated concentrations for times up to 3 h prior to extraction. Immunoblots were probed as indicated with antibodies to phospho-Src (pY419), phospho-FAK (pYpY576/577 or pY925), phospho-Pyk2 (pY580), phospho-p130Cas (pY410), phospho-Stat3 (pY705), phospho-Akt (pS473), phospho-MAPK p44/42, beta-catenin, or PARP. Blots were re-probed with total anti-Src, anti-FAK, or anti-Stat3 antibodies, as indicated.

p-ABL / ABL ; 

PubMed: 28199182     


Cells were transfected with human wild-type ABL, and p190 and p210 variants of BCR-ABL, treated with inhibitors for 24 hr and analyzed for activating phosphorylation (p) by immunoblot. Actin and total levels of expressed kinases serve as loading controls. Cells transfected with empty plasmid serve as transfection control. 

27903968 18483306 28199182
Immunofluorescence
p-FAK / p-STAT3 / beta-catenin; 

PubMed: 18483306     


MDA-MB-231 cells were treated with 0.01% DMSO or 1 µM SKI-606 for 48 h then fixed, probed with antibodies to phospho-FAK (pY576/pY577), FAK, phospho-Stat3 (pY705) or beta-catenin as indicated, and stained with DAPI. Images were captured under fluorescence at 40x magnification.

18483306
Growth inhibition assay
Cell viability; 

PubMed: 24812339     


Proliferation curves for bosutinib, gefitinib and sorafenib in (A) H1650 and (B) H1975. 

IC50; 

PubMed: 27903968     


Six NB cell lines, IMR-32, NGP, NB-19, CHLA-255, SH-SY5Y, and SK-N-AS, were treated with increasing concentrations of bosutinib for 48 hrs. Cell viability was measured by performing the Cell Counting Kit-8 (CCK-8) assay.

24812339 27903968
In vivo

Bosutinib (60 mg/kg/day) is active against Src-transformed fibroblasts xenografts and HT29 xenografts in nude mice with T/C of 18% and 30%, respectively. [1] Oral administration of Bosutinib for 5 days significantly suppresses K562 tumor growth in mice in a dose-dependent manner, with the large tumors eradicated at dose of 100 mg/kg and tumor free at 150 mg/kg without overt toxicity. [2] As being inactive against Colo205 xenografts in nude mice at 50 mg/kg twice daily, Bosutinib dosing at 75 mg/kg twice daily is necessary against Colo205 xenografts, and increasing the dose of Bosutinib has no additional benefit, in contrast to the significant dose-dependent ability against HT29 xenografts. [4]

Protocol

Kinase Assay:

[1]

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The Src and Abl kinase assays:

The Src kinase activity is measured in an ELISA format. Src (3 units/reaction), reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.5 mM Na3VO4) and cdc2 substrate peptide are added to various concentration of Bosutinib and incubated at 30 °C for 10 minutes. The reaction is started by the addition of ATP to a final concentration of 100 μM, incubated at 30 °C for 1 hour and stopped by addition of EDTA. Instructions from the manufacturer are followed for subsequent steps. The Abl kinase assay is performed in a DELFIA solid phase europium-based detection assay format. Biotinylated peptide (2 μM) is bound to streptavidin-coated microtitration plates for 1.5 hours in 1 mg/mL ovalbumin in PBS. The plates are washed for 1 hour with PBS/0.1% Tween 80, followed by a PBS wash. The kinase reaction is incubated for 1 hour at 30°C. Abl kinase (10 units) is mixed with 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, 80 μM EGTA, 100 μM ATP, 0.5 mM Na3VO4, 1% DMSO, 1 mM HEPES (pH 7.0), 200 μg/mL ovalbumin and various concentration of Bosutinib. The reaction is stopped with EDTA at a final concentration of 50 mM. The reaction is monitored with Eu-labeled phosphotyrosine antibody and DELFIA enhancement solution.
Cell Research:

[2]

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  • Cell lines: Abl-MLV, Rat 2, KU812, K562, and MEG-01 cells
  • Concentrations: Dissolved in DMSO, final concentrations ~1 μM
  • Incubation Time: 72 hours
  • Method:

    Cells are exposed to various concentrations of Bosutinib for 72 hours. Anchorage-independent proliferation of Abl-MLV-transformed fibroblasts is measured in 96-well ultra-low binding plates treated with Sigmacote to block residual cell attachment. Cell proliferation is measured with MTS or Cell-Glo. For the determination of cell cycle or cell death, cells are prepared for FACS analysis in the CycleTest Plus DNA reagent kit and analyzed on a fluorescence-activated cell sorter flow cytometer.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: Nude female mice injected with K562 cells
  • Dosages: ~150 mg/kg/day
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (188.51 mM)
Ethanol 2 mg/mL (3.77 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
10mg/mL

* 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 530.45
Formula

C26H29Cl2N5O3

CAS No. 380843-75-4
Storage powder
in solvent
Synonyms N/A
Smiles CN1CCN(CC1)CCCOC2=C(C=C3C(=C2)N=CC(=C3NC4=CC(=C(C=C4Cl)Cl)OC)C#N)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04258943 Recruiting Drug: Bosutinib Philadelphia Chromosome Positive CML|Accelerated Phase Chronic Myelogenous Leukemia|Blastic Phase Chronic Myelogenous Leukemia|Chronic Phase Chronic Myelogenous Leukemia Children''s Oncology Group|Erasmus MC|Dutch Childhood Oncology Group|Innovative Therapies for Children with Cancer|Pfizer April 6 2020 Phase 1|Phase 2
NCT03023319 Recruiting Drug: Bosutinib|Drug: Pemetrexed Carcinoma Non-Small-Cell Lung|Mesothelioma|Bladder Cancer|Ovarian Cancer|Peritoneal Cancer|Thymoma|Thymus Cancer|Uterine Cervical Cancer Nagla Abdel Karim|Augusta University December 10 2019 Phase 1
NCT03888222 Active not recruiting Drug: Placebo Oral Tablet|Drug: Bosutinib Oral Tablet Dementia With Lewy Bodies Georgetown University|Alzheimer''s Association April 23 2019 Phase 2
NCT03854903 Recruiting Drug: Palbociclib|Drug: Bosutinib|Drug: Fulvestrant Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Hormone Receptor Positive Breast Cancer Georgetown University|Pfizer April 1 2019 Phase 1
NCT03831776 Recruiting Drug: Bosutinib|Drug: Ropeginterferon Chronic Myeloid Leukemia St. Olavs Hospital|Haukeland University Hospital|Oslo University Hospital|University Hospital of North Norway|Helse Stavanger HF|Henri Mondor University Hospital|Hôpital René Huguenin|Hôpital Mignot Versailles Paris|Uppsala University Hospital|Odense University Hospital March 25 2019 Phase 2

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    Can I give S1014 Bosutinib to mice by oral gavage? If so, how to dissolve the drug?

  • Answer:

    For oral gavage, S1014 Bosutinib can be dissolved in 5% Tween 80+0.5% CMC Na at 30 mg/ml as a suspension.

Src Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID