Bosutinib (SKI-606)

Licensed by Pfizer Catalog No.S1014

Bosutinib (SKI-606) Chemical Structure

Molecular Weight(MW): 530.45

Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively.

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4 Customer Reviews

  • A,IC50 of Bosutinib that block ANDV-induced EC permeability. Endothelial cells were ANDV infected, and 3 days postinfection the permeability of cells in response to VEGF addition was determined in the presence or absence of increasing amounts of kinase inhibitor. The effect of inhibitors is presented as the percentage of ANDV-induced permeability of inhibitor-treated monolayers 3 days postinfection and 30 min post-VEGF and FITC-dextran addition. B, VEGFR2-Src inhibitors block ANDV-induced permeability. Endothelial cells were plated on vitronectin-coated Transwell inserts and infected at an MOI of 0.5 in triplicate with ANDV. Three days postinfection, the permeability of ANDV- and mock-infected endothelial cell monolayers was determined as described for Fig. 1 at indicated times in the presence or absence of Bosutinib .

    J Virol 2011 85, 2296–2303. Bosutinib (SKI-606) purchased from Selleck.

    Both parental and HR cell lines were treated with bosutinib (0.01, 0.1, and 1 μmol/L) for 24 hours. Src-related signaling pathway molecules were then analyzed.

    Mol Cancer Ther, 2017. Bosutinib (SKI-606) purchased from Selleck.

  • SFK inhibitors abrogate tyrosine phosphorylation associated with sperm capacitation. Mouse sperm were incubated in the absence or in the presence of SKI606 for 60 min in capacitating (cap, with HCO3) or non-capacitating media (NC, without HCO3). Western blot analyses were performed withanti-pY antibodies.

    J Biol Chem 2010 285, 7977–7985. Bosutinib (SKI-606) purchased from Selleck.

    Rescue ofPKAand tyrosine phosphorylation by Ser/Thr phosphatase inhibitors. A and B, spermwere incubated in capacitating medium supplemented with SFK inhibitors and different concentrations of okadaic acid (OA) (A) or calyculin-A (B), before immunodetection of p-PKA substrates (clone 100G7E). C and D, PVDF membranes used in A and B were stripped as described and used for Western blot immunodetection with anti-PY antibodies (clone 4G10).

    Dr. Pablo E.Visconti from University of Massachusetts. Bosutinib (SKI-606) purchased from Selleck.

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.
Targets
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 MoP5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTtTWM2OD1yLkC4NlMyKCEQvF2= NXzEZlh6W0GQR1XS
SW756 M3HR[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwMUSwNlQhKM7:TR?= MnzwV2FPT0WU
CTV-1 NUfZ[otsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUH1T212UUN3ME2wMlE3Ozl6IDFOwG0> NGPqWFBUSU6JRWK=
HSC-4 M4f3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXH4elZ{UUN3ME2wMlE4OTV6IDFOwG0> MV7TRW5ITVJ?
LAMA-84 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTBwMki2OlQhKM7:TR?= M3XyU3NCVkeHUh?=
KU812 NUnkc2VbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\4WpFsUUN3ME2wMlM1ODZ6IDFOwG0> NX;FSlNKW0GQR1XS
HCC1806 NFn4OJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XxfWlEPTB;MD6zOVIyPiBizszN NUP0S5lYW0GQR1XS
DOK M2TvWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHryeo5KSzVyPUCuN|c4QDZiIN88US=> NWK4NWZLW0GQR1XS
NCI-H209 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXKRZhuUUN3ME2wMlQxQDB6IDFOwG0> MmLyV2FPT0WU
EoL-1-cell MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mkj3TWM2OD1yLkSxOVc3KCEQvF2= M4HhbnNCVkeHUh?=
H9 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\uOGdTUUN3ME2wMlQ{PDZ2IDFOwG0> M4fsZ3NCVkeHUh?=
EM-2 M4PTXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LXNWlEPTB;MD60N|g6KCEQvF2= MUjTRW5ITVJ?
NCI-H292 NIjse3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\wZZp6UUN3ME2wMlQ1OTB6IDFOwG0> MlzDV2FPT0WU
697 M3nQZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTBwNEW2N|MhKM7:TR?= MkG1V2FPT0WU
BHT-101 NV3KN5hJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4TZS2lEPTB;MD60OlU6KCEQvF2= MX\TRW5ITVJ?
BE-13 M2rxPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHLW5RjUUN3ME2wMlQ5PTd{IDFOwG0> NEmxdYVUSU6JRWK=
RS4-11 Moj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmq1TWM2OD1yLkS4OVg1KCEQvF2= NV\VVppJW0GQR1XS
IGROV-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Tt[GlEPTB;MD60PFc6PyBizszN MUnTRW5ITVJ?
KE-37 NIXsNnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEC4W3JKSzVyPUCuOFk2ODliIN88US=> MnLuV2FPT0WU
BV-173 MnLvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LzUWlEPTB;MD61NFc6OiBizszN NFHmSmVUSU6JRWK=
MEG-01 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTBwNUGyNVQhKM7:TR?= MXLTRW5ITVJ?
LB2241-RCC NUf2NmRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnn4TWM2OD1yLkWzO|E5KCEQvF2= NYDsfHBSW0GQR1XS
ACHN MlTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrlO|A{UUN3ME2wMlU1ODZ7IDFOwG0> NUK0[4I1W0GQR1XS
CTB-1 NXnXPFQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\GOFRKSzVyPUCuOVQ5OiBizszN Ml;PV2FPT0WU
HT-1080 M{\sV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fO[mlEPTB;MD61OVM1QSBizszN MljsV2FPT0WU
CHL-1 M4rwZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXtTWM2OD1yLkW1OFY2KCEQvF2= NGTyS|BUSU6JRWK=
EW-3 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7WemtKSzVyPUCuOVU6OzViIN88US=> M4jkXXNCVkeHUh?=
ES1 Ml\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTBwNke0PVghKM7:TR?= M1jpTHNCVkeHUh?=
KASUMI-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlW0TWM2OD1yLkeyN|MhKM7:TR?= MXfTRW5ITVJ?
SW13 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;KTWM2OD1yLkezO|k5KCEQvF2= MW\TRW5ITVJ?
A3-KAW MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnvTWM2OD1yLke5NlA5KCEQvF2= MUjTRW5ITVJ?
LB771-HNC MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjsTWM2OD1yLkizNVA1KCEQvF2= MkjYV2FPT0WU
OC-314 NFLW[FFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DPUWlEPTB;MD64Olk3PSBizszN M3nC[XNCVkeHUh?=
MLMA MoTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\UbWlEPTB;MD65NFY4PSBizszN M1LST3NCVkeHUh?=
KARPAS-45 NYXCboV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvTfXV1UUN3ME2wMlkzPDZ4IDFOwG0> M37xbXNCVkeHUh?=
CAL-27 NHm2VphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfm[ZdKSzVyPUCuPVI6ODZiIN88US=> MY\TRW5ITVJ?
SK-NEP-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjue5pKSzVyPUCuPVczPDhiIN88US=> NX7jVXZbW0GQR1XS
COR-L105 MnqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTFwMECzPVQhKM7:TR?= MX3TRW5ITVJ?
TI-73 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVq3RZIzUUN3ME2xMlAyPjViIN88US=> NYjhcFhOW0GQR1XS
JVM-3 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnHTWM2OD1zLkC1NFE4KCEQvF2= NYDrc4Y6W0GQR1XS
HAL-01 Mn3HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4L2V2lEPTB;MT6wPFgyKCEQvF2= NXTXXWxiW0GQR1XS
QIMR-WIL MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TVVmlEPTB;MT6wPVA2QCBizszN MmLMV2FPT0WU
HSC-3 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIn3T3hKSzVyPUGuNVE4QDNiIN88US=> NIXiflJUSU6JRWK=
KY821 MoLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFwMUOzOVEhKM7:TR?= MWPTRW5ITVJ?
5637 NV3XS3NQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTFwMUO4NFMhKM7:TR?= NVz4bGFFW0GQR1XS
CAL-33 NVvPOIk{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjw[nh[UUN3ME2xMlE6OzB{IDFOwG0> M3jHU3NCVkeHUh?=
ES4 NWKxSpZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoC0TWM2OD1zLkKwO|khKM7:TR?= M3m2NXNCVkeHUh?=
BHY Mny3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7oTWM2OD1zLkKyPFkzKCEQvF2= MULTRW5ITVJ?
LB1047-RCC M1nRemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;OTWM2OD1zLkKzO|g2KCEQvF2= NFTvSJFUSU6JRWK=
H4 NIjaSoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7uTZlFUUN3ME2xMlI1OjV3IDFOwG0> Mn;YV2FPT0WU
RPMI-8866 NEm3UndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1L1d2lEPTB;MT6yOlExPiBizszN NY\UXm1ZW0GQR1XS
HO-1-N-1 M3HzXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTFwMk[zOlkhKM7:TR?= MlPDV2FPT0WU
BB30-HNC MoHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEXZbIxKSzVyPUGuNlg4OTRiIN88US=> NYDtV5E2W0GQR1XS
PC-14 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFwMkmyNFUhKM7:TR?= NHXjPW1USU6JRWK=
NUGC-3 NWHrZnlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jqdmlEPTB;MT6yPVM2PiBizszN NEHIPFVUSU6JRWK=
A4-Fuk M2TwU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmS2TWM2OD1zLkOwO|A1KCEQvF2= MVzTRW5ITVJ?
MHH-NB-11 MoLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTFwM{GzPFMhKM7:TR?= MmrKV2FPT0WU
KOSC-2 M3GwNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPBPHBPUUN3ME2xMlMyPzd3IDFOwG0> MnPwV2FPT0WU
A498 NFXp[YxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DBbWlEPTB;MT60NFEyOyBizszN M{fx[nNCVkeHUh?=
KG-1 MmXqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjySHpKSzVyPUGuOFEzPzNiIN88US=> Mlj2V2FPT0WU
DEL M3XlUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;JfYxQUUN3ME2xMlQ{PjV5IDFOwG0> NFPTO2xUSU6JRWK=
EW-16 MmPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1:4WGlEPTB;MT60N|k4OyBizszN NIXUPXdUSU6JRWK=
BPH-1 NGnKd3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTFwNES4NFUhKM7:TR?= MV\TRW5ITVJ?
JAR NWTpVW04T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\tVWlEPTB;MT60PVM3KCEQvF2= M1XZcXNCVkeHUh?=
J-RT3-T3-5 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHseGFKSzVyPUGuOVE4OjJiIN88US=> MXPTRW5ITVJ?
A375 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTFwNUG3O|IhKM7:TR?= MVjTRW5ITVJ?
SW954 MmrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;hcJVsUUN3ME2xMlU2ODB5IDFOwG0> M4KxPXNCVkeHUh?=
Ca9-22 M{nJfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTOTWM2OD1zLkW2NlYhKM7:TR?= NGW2V3VUSU6JRWK=
D-566MG MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3oZZdKUUN3ME2xMlU4OTV3IDFOwG0> NIOzUHZUSU6JRWK=
SCC-15 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\kTWM2OD1zLk[xPFA1KCEQvF2= M{PkTnNCVkeHUh?=
HD-MY-Z M{nUfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGS3RW9KSzVyPUGuOlM2QDRiIN88US=> M1zp[HNCVkeHUh?=
HT-1376 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFuwT29KSzVyPUGuOlQ{PiBizszN MkjrV2FPT0WU
CAL-54 NIH2NFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTFwNkW3NFkhKM7:TR?= M1XQWnNCVkeHUh?=
ONS-76 MlfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;uSWlEPTB;MT62O|U2OSBizszN MXvTRW5ITVJ?
EFO-27 M1;0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmP6TWM2OD1zLk[4PVIhKM7:TR?= MlnKV2FPT0WU
769-P M4r4ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrtTWM2OD1zLk[5OVk3KCEQvF2= NHnX[odUSU6JRWK=
MV-4-11 NHjNW5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13xT2lEPTB;MT62PVg2PiBizszN M3LyUnNCVkeHUh?=
NKM-1 M322O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\2NGlEPTB;MT63NVgxOiBizszN MnvLV2FPT0WU
LOXIMVI NETOPGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TIVGlEPTB;MT63OFU6QSBizszN M3PmeXNCVkeHUh?=
KYSE-140 Mkm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjnO3NKSzVyPUGuO|U3PTViIN88US=> MYDTRW5ITVJ?
ES5 M2PINmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\EfZpYUUN3ME2xMlg3PzR5IDFOwG0> NILOOIZUSU6JRWK=
BB65-RCC MonJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTWeHFtUUN3ME2xMlg6QDR7IDFOwG0> MmLMV2FPT0WU
HN MnLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\nOVFPUUN3ME2xMlg6QDd2IDFOwG0> MWXTRW5ITVJ?
A101D M361T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn61TWM2OD1zLkmzOlI5KCEQvF2= NYPnepFrW0GQR1XS
LoVo MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmq4TWM2OD1zLkm3Olc6KCEQvF2= M1\GO3NCVkeHUh?=
NCI-H526 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfnfXpNUUN3ME2xMlk6OzJ3IDFOwG0> M2XVS3NCVkeHUh?=
NCI-H1693 NH\ZWmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{C1e2lEPTB;MT65PVg5QCBizszN Mm\aV2FPT0WU
OVCAR-4 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\QeIhKSzVyPUKuNFA1OzViIN88US=> NX\ZSGJYW0GQR1XS
SK-HEP-1 NYi0XlEyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\2TWM2OD1{LkCwO|Q2KCEQvF2= MX3TRW5ITVJ?
C2BBe1 NHrtc2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTJwMEOzO|IhKM7:TR?= NGnDXlNUSU6JRWK=
MEL-JUSO M4fZeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPWV3RKSzVyPUKuNFQ1PjRiIN88US=> NFzRUVVUSU6JRWK=
MOLT-16 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTJwMEewOVghKM7:TR?= NEnqPIZUSU6JRWK=
NBsusSR M1f2PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUj4ZZdHUUN3ME2yMlA6QDh7IDFOwG0> MoPyV2FPT0WU
TK10 NULVcXJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTJwMUO0OVghKM7:TR?= MYDTRW5ITVJ?
CAL-39 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\YTWM2OD1{LkG0OFghKM7:TR?= NYjGOoJ4W0GQR1XS
NCI-H2030 MoriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTJwMUi5O|MhKM7:TR?= MmjMV2FPT0WU
HCT-116 NHjOSVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTJwMkK5PFQhKM7:TR?= M{nlbXNCVkeHUh?=
HTC-C3 M2n1Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHe1bItKSzVyPUKuNlY5OjRiIN88US=> M4LDZ3NCVkeHUh?=
TYK-nu MlPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTJwM{C5NFkhKM7:TR?= M2KyWHNCVkeHUh?=
FADU NFnnT4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mli4TWM2OD1{LkOyNlk3KCEQvF2= M1HaVHNCVkeHUh?=
A431 NHz3ZXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnW2TWM2OD1{LkO3NFI2KCEQvF2= NYH4OYx[W0GQR1XS
TE-11 NFvWZnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrZbJJKSzVyPUKuN|gxOTliIN88US=> NILVOlJUSU6JRWK=
CAL-12T M13zVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPXTWM2OD1{LkSwOFE4KCEQvF2= M{fTSnNCVkeHUh?=
DB MlflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\4RllKSzVyPUKuOFI5PjliIN88US=> NED3XHFUSU6JRWK=
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NCI-H69 MmXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NELUWpNKSzVyPUOwMlYxQTNiIN88US=> M3j3[HNCVkeHUh?=
NB6 NFzVXoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTnV3V3UUN3ME2zNU4{PjJ7IDFOwG0> NWOwfGF2W0GQR1XS
CAL-120 M2m3RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnNTWM2OD1|Mj60N|E4KCEQvF2= NIHnOFhUSU6JRWK=
U-87-MG NVGxUYc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXfJR|UxRTN|LkCyOVEhKM7:TR?= NIPkSlVUSU6JRWK=
NCI-H1304 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTN|LkCzOVQhKM7:TR?= M4nNRXNCVkeHUh?=
YH-13 MlXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnOTWM2OD1|Mz6yOVM2KCEQvF2= NIrDOo9USU6JRWK=
RMG-I NV7EdGlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILkUWtKSzVyPUOzMlQzQDViIN88US=> NFnmV5JUSU6JRWK=
LU-65 NGTLN4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PsSGlEPTB;M{SuNVQxQCBizszN MnzyV2FPT0WU
GB-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rDOWlEPTB;M{WuNFczQSBizszN MmPsV2FPT0WU
DU-4475 NXHyeWFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTN3LkG1OVMhKM7:TR?= M3fYcXNCVkeHUh?=
SBC-5 MoS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFXLeXJKSzVyPUO2MlU6ODJiIN88US=> NFPWd|RUSU6JRWK=
OE33 MlLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIWz[o1KSzVyPUO3Mlc2PzdiIN88US=> MXXTRW5ITVJ?
C8166 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTN6LkWyOlchKM7:TR?= NXnPTmlWW0GQR1XS
COLO-684 NEPm[mhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTN6Lke0NlghKM7:TR?= NWfOOop4W0GQR1XS
NCI-H1155 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1K5SmlEPTB;M{muNFQ4OSBizszN NHTUU5FUSU6JRWK=
ATN-1 MnTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTVTWM2OD1|OT63O|kzKCEQvF2= MUnTRW5ITVJ?
KARPAS-299 MljjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTN7LkizPUAh|ryP Mkn3V2FPT0WU
KNS-81-FD M1:4Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTRyLkO2NFQhKM7:TR?= M2DteHNCVkeHUh?=
NCI-H1563 Ml7TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TMemlEPTB;NEGuOVA{QSBizszN NYnWfmY{W0GQR1XS
NB14 NGnJTWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTrUFhKSzVyPUSyMlczPjNiIN88US=> MV3TRW5ITVJ?
COLO-800 NFPzN2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;iTmdKSzVyPUSyMlg2OTdiIN88US=> NG[4c4JUSU6JRWK=
MS-1 NX7jd455T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGezToZKSzVyPUSzMlA1QDNiIN88US=> M{nQeHNCVkeHUh?=
OVCAR-8 M1P4Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTR|Lk[4NFkhKM7:TR?= NFLEd5ZUSU6JRWK=
SK-PN-DW M3fDeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkT5TWM2OD12Mz64O|c3KCEQvF2= MlGzV2FPT0WU
G-402 NVnDbYg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELzcIVKSzVyPUSzMlkxODZiIN88US=> NGTxTHJUSU6JRWK=
NCI-H2291 NHrDWXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTR2LkiwNVchKM7:TR?= MVvTRW5ITVJ?
PC-3 Ml7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrXcHZ{UUN3ME20OU45ODJ|IDFOwG0> MV;TRW5ITVJ?
NCI-H1581 NWrlfnlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmC2TWM2OD12NT65PFg6KCEQvF2= M1\aNXNCVkeHUh?=
SW1116 Mo\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVy5WXR2UUN3ME20O{4xOTh{IDFOwG0> M1iwOnNCVkeHUh?=
ZR-75-30 NIr2XnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PtcmlEPTB;NEeuNFI{QSBizszN NX[3WoFVW0GQR1XS
OCI-AML2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTR5LkC5NVghKM7:TR?= NITzR4dUSU6JRWK=
MDA-MB-231 NIHEWmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLCXIdKSzVyPUS3MlYzPDliIN88US=> NUTE[YlOW0GQR1XS
ES3 NGC5PJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTR6LkO1NlkhKM7:TR?= NFzNVWVUSU6JRWK=
NCI-H630 NIjNepNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTR7LkG3OFIhKM7:TR?= M36xeXNCVkeHUh?=
OE19 NWr3dVZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvVPFA{UUN3ME20PU4zQTB{IDFOwG0> NYfseFN[W0GQR1XS
NCI-H1573 NF71N3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTR7Lk[4OlEhKM7:TR?= MmjoV2FPT0WU
EW-1 NXPjZo9lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTR7LkmwPFQhKM7:TR?= NHjYd49USU6JRWK=

... Click to View More Cell Line Experimental Data

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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • Animal Models: Nude female mice injected with K562 cells
  • Formulation: Suspended in 0.5% methocel/0.4% Tween 80
  • 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 <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 10mg/mL

* 1 mg/ml means slightly soluble or 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 530.45
Formula

C26H29Cl2N5O3

CAS No. 380843-75-4
Storage powder
in solvent
Synonyms N/A

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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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 MSDS / 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 )

  • C1
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    C2
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / 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):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    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 Conditions Sponsor/Collaborators Start Date Phases
NCT03023319 Recruiting Carcinoma, Non-Small-Cell Lung|Mesothelioma|Bladder Cancer|Ovarian Cancer|Peritoneal Cancer|Thymoma|Thymus Cancer|Uterine Cervical Cancer Nagla Karim|University of Cincinnati January 2017 Phase 1
NCT02810990 Recruiting Chronic Myeloid Leukemia Gruppo Italiano Malattie EMatologiche dellAdulto November 2016 Phase 2
NCT02906696 Recruiting Chronic Myelogenous Leukemia M.D. Anderson Cancer Center|Pfizer October 2016 Phase 2
NCT02782403 Not yet recruiting Leukemia M.D. Anderson Cancer Center|Pfizer September 2016 Phase 1|Phase 2
NCT02921477 Enrolling by invitation Mild Cognitive Impairment|Dementia Neurological Associates of West Los Angeles|Pfizer September 2016 Phase 1
NCT02693535 Recruiting Lymphoma, Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors American Society of Clinical Oncology|AstraZeneca|Bayer|Bristol-Myers Squibb|Eli Lilly and Company|Genentech, Inc.|Merck Sharp & Dohme Corp.|Pfizer March 2016 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID