Bosutinib (SKI-606)

Pfizer辉瑞授权 目录号:S1014

Bosutinib (SKI-606) Chemical Structure

Molecular Weight(MW): 530.45

Bosutinib (SKI-606)是一种新型的双重Src/Abl抑制剂,在无细胞试验中IC50分别为1.2 nM 和 1 nM。

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RMB 745.18 现货
RMB 564.16 现货
RMB 2197.71 现货
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客户使用该产品的5个实验数据:

  • 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, 16(6):1145-1154. Bosutinib (SKI-606) purchased from Selleck.

    Abl kinase phosphorylates MNRR1 in vivo. (A) K562 cells harboring the constitutively active BCR-ABL kinase when treated with 100 nM Bosutinib for 24 h show a reduction in MNRR1 phosphorylation. Lysates from vehicle and Bosutinib treated cells were immunoprecipitated using the anti-phosphotyrosine antibody and analyzed for the levels of MNRR1 in the precipitate. The IgG levels are also shown for an equal pull-down. Bosutinib efficacy was confirmed using antibodies against phospho-Abl kinase and phospho-STAT5, a downstream target of Abl kinase. Tubulin was used as a loading control. (B) Bosutinib treatment reduces the levels of phosphorylated proteins only. The total protein levels (Abl kinase and MNRR1) in vehicle and Bosutinib treated cells were similar. (C) Levels of Abl kinase in the WT and Abl kinase deficient MEFs (Abl−/− MEFs). The doublet is caused by the presence of a non-specific band [28]. (D) The level of oxygen consumption in WT MEFs transfected with either WT or phosphomimetic Y99E mutant MNRR1. Oxygen consumption was measured in intact cells on a Seahorse Bioanalyzer. (E) Y99E mutant MNRR1 stimulates oxidative phosphorylation better than WT MNRR1 in Abl deficient MEFs (Abl−/− MEFs) as measured by intact cellular oxygen consumption. (F) Bosutinib also inhibits BCR-Abl kinase in the mitochondrial fraction. NDUFS3 was used as a mitochondrial marker and GAPDH as a cytoplasmic marker to evaluate purity of the fractions. (G) K562 cells treated with Bosutinib, which show a reduction in the level of MNRR1 tyrosine phosphorylation (A), also have a reduction in the levels of oxygen consumption. (H) MNRR1 is not phosphorylated in the Abl−/− MEFs. WT and Abl−/− cellular lysates were immunoprecipitated with the anti-phosphotyrosine antibody and probed for the presence of MNRR1. The total levels of MNRR1 in the WT and Abl−/− MEFs were similar.

    Biochim Biophys Acta, 2017, 1864(2):440-448. Bosutinib (SKI-606) purchased from Selleck.

  • 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.

    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.

产品安全说明书

Src抑制剂选择性比较

生物活性

产品描述 Bosutinib (SKI-606)是一种新型的双重Src/Abl抑制剂,在无细胞试验中IC50分别为1.2 nM 和 1 nM。
靶点
Abl [2]
(Cell-free assay)
Src [1]
(Cell-free assay)
1 nM 1.2 nM
体外研究

Bosutinib作用于Src比非Src家族激酶选择性高,IC50为1.2 nM,且有效抑制Src依赖的细胞增殖,IC50为100 nM。[1] Bosutinib 显著抑制Bcr-Abl阳性白血病细胞系KU812, K562, 和MEG-01 而不是 Molt-4, HL-60, Ramos, 和其他白血病细胞系的增殖,IC50分别为5 nM, 20 nM,和20 nM,比 STI-571更有效。与STI-571类似, Bosutinib 作用于Abl-MLV转化纤维,具有看增殖活性,IC50为 90 nM。Bosutinib浓度分别为50 nM, 10-25 nM, 和200 nM 时,切除CML细胞中的Bcr-Abl 和STAT5及纤维中表达的v-Abl酪氨酸磷酸化,导致Bcr-Abl下游信号Lyn/Hck 磷酸化受抑制。[2] 虽然不能抑制乳腺癌细胞增殖和存活,但是可明显降低乳腺癌细胞运动和入侵,IC50为250 nM,提高细胞间粘附和β-连环蛋白的膜定位。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NB7 NWTKSndsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfTTWM2OD1yLkC4NlMyKCEQvF2= MlX1V2FPT0WU
SW756 NHiyeVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTlTWM2OD1yLkG0NFI1KCEQvF2= NV:1RYdDW0GQR1XS
CTV-1 NIr3UVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHX6[VlKSzVyPUCuNVY{QThiIN88US=> NHvGUplUSU6JRWK=
HSC-4 M{e0eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTBwMUexOVghKM7:TR?= M4\6R3NCVkeHUh?=
LAMA-84 NUD3RYE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTBwMki2OlQhKM7:TR?= MnzqV2FPT0WU
KU812 MnPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfmNGVKSzVyPUCuN|QxPjhiIN88US=> MnLTV2FPT0WU
HCC1806 NVjidXFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7vcIJKSzVyPUCuN|UzOTZiIN88US=> MoX2V2FPT0WU
DOK MoXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvpTWM2OD1yLkO3O|g3KCEQvF2= MXvTRW5ITVJ?
NCI-H209 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTBwNEC4NFghKM7:TR?= MWDTRW5ITVJ?
EoL-1-cell NXLHNZNRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\BXmlEPTB;MD60NVU4PiBizszN NIDqe4dUSU6JRWK=
H9 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;wWWhKSzVyPUCuOFM1PjRiIN88US=> M{jsRnNCVkeHUh?=
EM-2 M2rndGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;WOppKSzVyPUCuOFM5QSBizszN NGPOSpFUSU6JRWK=
NCI-H292 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDp[mFxUUN3ME2wMlQ1OTB6IDFOwG0> NHL5PIFUSU6JRWK=
697 M2\ieWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFP4bHRKSzVyPUCuOFU3OzNiIN88US=> NGHLVZNUSU6JRWK=
BHT-101 NX3IbFVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPQVlNVUUN3ME2wMlQ3PTliIN88US=> NYXDU2s6W0GQR1XS
BE-13 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTBwNEi1O|IhKM7:TR?= NVzmSGJTW0GQR1XS
RS4-11 M2jjZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;FTWM2OD1yLkS4OVg1KCEQvF2= MoPpV2FPT0WU
IGROV-1 M33RTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml65TWM2OD1yLkS4O|k4KCEQvF2= NF;QPI9USU6JRWK=
KE-37 M33Xbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moq4TWM2OD1yLkS5OVA6KCEQvF2= MUXTRW5ITVJ?
BV-173 NIi4WZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTIcZNKSzVyPUCuOVA4QTJiIN88US=> NYDubVF2W0GQR1XS
MEG-01 M17GdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH63N|RKSzVyPUCuOVEzOTRiIN88US=> MmjhV2FPT0WU
LB2241-RCC NXTJc4w3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzUTWM2OD1yLkWzO|E5KCEQvF2= NFTZTHdUSU6JRWK=
ACHN MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrlSm1KSzVyPUCuOVQxPjliIN88US=> MlfrV2FPT0WU
CTB-1 NHrSWI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHPTWM2OD1yLkW0PFIhKM7:TR?= M1TGUHNCVkeHUh?=
HT-1080 M2PEdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXf1NpJ7UUN3ME2wMlU2OzR7IDFOwG0> MmL2V2FPT0WU
CHL-1 NWrBXpZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rYVmlEPTB;MD61OVQ3PSBizszN MXzTRW5ITVJ?
EW-3 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWKzNpM3UUN3ME2wMlU2QTN3IDFOwG0> M4LURXNCVkeHUh?=
ES1 NHu0TndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTBwNke0PVghKM7:TR?= NX34U5RqW0GQR1XS
KASUMI-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mni2TWM2OD1yLkeyN|MhKM7:TR?= NYmxVFNbW0GQR1XS
SW13 NXPWVoMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTBwN{O3PVghKM7:TR?= M1X3VHNCVkeHUh?=
A3-KAW MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHuUmVnUUN3ME2wMlc6OjB6IDFOwG0> M2PGeHNCVkeHUh?=
LB771-HNC M1;IVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1P4RWlEPTB;MD64N|ExPCBizszN M4XSUHNCVkeHUh?=
OC-314 NVj6[I52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PxNWlEPTB;MD64Olk3PSBizszN MWfTRW5ITVJ?
MLMA M1vmVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLaTWM2OD1yLkmwOlc2KCEQvF2= MVrTRW5ITVJ?
KARPAS-45 NFyycIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHtfmVKSzVyPUCuPVI1PjZiIN88US=> NUn1cJo3W0GQR1XS
CAL-27 MnvhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TPNWlEPTB;MD65NlkxPiBizszN NEC3W3pUSU6JRWK=
SK-NEP-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvtXFA6UUN3ME2wMlk4OjR6IDFOwG0> M1jZWHNCVkeHUh?=
COR-L105 NFrwXHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDUVmtKSzVyPUGuNFA{QTRiIN88US=> NXr5RnZ4W0GQR1XS
TI-73 MkfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\MPHpqUUN3ME2xMlAyPjViIN88US=> NU\SWYlCW0GQR1XS
JVM-3 NVrxRpNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTFwMEWwNVchKM7:TR?= NFTVVIlUSU6JRWK=
HAL-01 M{jwfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV[5W2FwUUN3ME2xMlA5QDFiIN88US=> MlO2V2FPT0WU
QIMR-WIL MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTFwMEmwOVghKM7:TR?= MnjZV2FPT0WU
HSC-3 M4LQPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnpfJQ3UUN3ME2xMlEyPzh|IDFOwG0> MYTTRW5ITVJ?
KY821 MmHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTFwMUOzOVEhKM7:TR?= MmfrV2FPT0WU
5637 NX;UW2VtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnDfYRNUUN3ME2xMlE{QDB|IDFOwG0> M4TkdnNCVkeHUh?=
CAL-33 M2LUdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DUXGlEPTB;MT6xPVMxOiBizszN MVXTRW5ITVJ?
ES4 NVP6TIhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfMdpZKSzVyPUGuNlA4QSBizszN MkXtV2FPT0WU
BHY MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\XTWM2OD1zLkKyPFkzKCEQvF2= NGrqUJZUSU6JRWK=
LB1047-RCC NXrEfmllT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLEeol1UUN3ME2xMlI{Pzh3IDFOwG0> MYTTRW5ITVJ?
H4 NW\NcoF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXOUYN[UUN3ME2xMlI1OjV3IDFOwG0> MWXTRW5ITVJ?
RPMI-8866 NGewTnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nkSGlEPTB;MT6yOlExPiBizszN MkLHV2FPT0WU
HO-1-N-1 NW[0O5VmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTFwMk[zOlkhKM7:TR?= MmSwV2FPT0WU
BB30-HNC NYLDcVM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlP6TWM2OD1zLkK4O|E1KCEQvF2= NIXmR2xUSU6JRWK=
PC-14 M3mwfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHRTWM2OD1zLkK5NlA2KCEQvF2= NWjHNFV1W0GQR1XS
NUGC-3 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTFwMkmzOVYhKM7:TR?= M13oTXNCVkeHUh?=
A4-Fuk MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\RTZZKSzVyPUGuN|A4ODRiIN88US=> MlPjV2FPT0WU
MHH-NB-11 NWHmS4trT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPGWnc1UUN3ME2xMlMyOzh|IDFOwG0> M1\obXNCVkeHUh?=
KOSC-2 Mm\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2L6VGlEPTB;MT6zNVc4PSBizszN NVLqfYd6W0GQR1XS
A498 MlLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTFwNECxNVMhKM7:TR?= MmHmV2FPT0WU
KG-1 NXrJZZo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2joZmlEPTB;MT60NVI4OyBizszN NXroWllsW0GQR1XS
DEL MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrBfXVKSzVyPUGuOFM3PTdiIN88US=> MVzTRW5ITVJ?
EW-16 M3rxcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX30boF{UUN3ME2xMlQ{QTd|IDFOwG0> NV3CSVRtW0GQR1XS
BPH-1 M3XRW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{LGfGlEPTB;MT60OFgxPSBizszN MkDEV2FPT0WU
JAR NV7XTGhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LLOGlEPTB;MT60PVM3KCEQvF2= NEPCW|VUSU6JRWK=
J-RT3-T3-5 NFnSRodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3QTWM2OD1zLkWxO|IzKCEQvF2= M4PLUXNCVkeHUh?=
A375 NWLvXHBsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LRWWlEPTB;MT61NVc4OiBizszN M1i2R3NCVkeHUh?=
SW954 M3vqTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\lTWM2OD1zLkW1NFA4KCEQvF2= MU\TRW5ITVJ?
Ca9-22 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjtTWM2OD1zLkW2NlYhKM7:TR?= NHjoVW9USU6JRWK=
D-566MG M{LNTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTFwNUexOVUhKM7:TR?= NYLyUnZqW0GQR1XS
SCC-15 M16zRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrydIwyUUN3ME2xMlYyQDB2IDFOwG0> Mn;mV2FPT0WU
HD-MY-Z NGj4SWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFy2dVNKSzVyPUGuOlM2QDRiIN88US=> MWLTRW5ITVJ?
HT-1376 M2XLWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTFwNkSzOkAh|ryP NGizSXVUSU6JRWK=
CAL-54 NYfyXWc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fBWmlEPTB;MT62OVcxQSBizszN M1XaT3NCVkeHUh?=
ONS-76 NFzHOWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHLTWM2OD1zLk[3OVUyKCEQvF2= NHroT4pUSU6JRWK=
EFO-27 NVrUV3FDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rpVWlEPTB;MT62PFkzKCEQvF2= M1zsUXNCVkeHUh?=
769-P M1zkRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTFwNkm1PVYhKM7:TR?= NXjjUFM2W0GQR1XS
MV-4-11 NY[5TmtKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1j2SmlEPTB;MT62PVg2PiBizszN NFvCUGhUSU6JRWK=
NKM-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlP5TWM2OD1zLkexPFAzKCEQvF2= MnnxV2FPT0WU
LOXIMVI NXG3WVFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1T4eGlEPTB;MT63OFU6QSBizszN NFXwWJBUSU6JRWK=
KYSE-140 NXfTb|ZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfDWYNIUUN3ME2xMlc2PjV3IDFOwG0> MlfHV2FPT0WU
ES5 M2fDO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDwO4VWUUN3ME2xMlg3PzR5IDFOwG0> MYTTRW5ITVJ?
BB65-RCC MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUe1dVNlUUN3ME2xMlg6QDR7IDFOwG0> NWjxNmZzW0GQR1XS
HN NUDLXop1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPUdGp2UUN3ME2xMlg6QDd2IDFOwG0> M{fGRXNCVkeHUh?=
A101D Ml\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1q3XWlEPTB;MT65N|YzQCBizszN MVzTRW5ITVJ?
LoVo M{fMcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTFwOUe2O|khKM7:TR?= NWHwSFJ3W0GQR1XS
NCI-H526 NVrm[ZQ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\KTWM2OD1zLkm5N|I2KCEQvF2= MnfRV2FPT0WU
NCI-H1693 M3;uOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;Kd2lEPTB;MT65PVg5QCBizszN NHvFV2hUSU6JRWK=
OVCAR-4 NUT0T3o1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXNdYxKSzVyPUKuNFA1OzViIN88US=> MV\TRW5ITVJ?
SK-HEP-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3kV5J4UUN3ME2yMlAxPzR3IDFOwG0> MoC0V2FPT0WU
C2BBe1 Mk\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTJwMEOzO|IhKM7:TR?= MlHwV2FPT0WU
MEL-JUSO MmPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTJwMES0OlQhKM7:TR?= NUHlRYtlW0GQR1XS
MOLT-16 NYnhbnRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TzfGlEPTB;Mj6wO|A2QCBizszN MXPTRW5ITVJ?
NBsusSR NXu5WlI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTJwMEm4PFkhKM7:TR?= NVrjOIpNW0GQR1XS
TK10 MkXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\odGlEPTB;Mj6xN|Q2QCBizszN MmLkV2FPT0WU
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KYSE-70 MmLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEC5cm1KSzVyPUK2MlU{OTdiIN88US=> MUPTRW5ITVJ?
MKN7 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkHnTWM2OD1{Nz63OFc6KCEQvF2= M{L2e3NCVkeHUh?=
D-392MG Mmr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHXRYFKSzVyPUK3Mlc3QTRiIN88US=> MkLxV2FPT0WU
NH-12 MlrZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlK4TWM2OD1{OD6xNlI6KCEQvF2= MmPwV2FPT0WU
EW-18 M4\w[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3hW3hKSzVyPUK4MlIzOThiIN88US=> Mmf3V2FPT0WU
LCLC-97TM1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrVRldbUUN3ME2yPE4zPzZ{IDFOwG0> MY\TRW5ITVJ?
NCI-H1770 MoPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vON2lEPTB;MkiuN|U3PiBizszN NIjrXYZUSU6JRWK=
BT-20 NVT5cldnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Xw[WlEPTB;MkiuN|Y5PSBizszN M{XLNXNCVkeHUh?=
DBTRG-05MG MkPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3n3VWlEPTB;MkiuOFg{QCBizszN NGHM[HZUSU6JRWK=
HPAF-II MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1X2cGlEPTB;MkiuO|c6KCEQvF2= MY\TRW5ITVJ?
SW837 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTJ7LkOzPFUhKM7:TR?= M3;se3NCVkeHUh?=
647-V MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPY[JVKSzVyPUK5MlcxODNiIN88US=> NWfNU2VYW0GQR1XS
J82 MlLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\zVXE4UUN3ME2yPU45ODF|IDFOwG0> MojxV2FPT0WU
MC116 NEXadmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TpOmlEPTB;M{CuNFc{OyBizszN NVHUeY17W0GQR1XS
NCI-H69 NH7CfVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTNyLk[wPVMhKM7:TR?= MnTKV2FPT0WU
NB6 M1\zW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fZVmlEPTB;M{GuN|YzQSBizszN NWjTc2lTW0GQR1XS
CAL-120 NE\0Z3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLvdYdKSzVyPUOyMlQ{OTdiIN88US=> MmH6V2FPT0WU
U-87-MG NIHobmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIi3UpBKSzVyPUOzMlAzPTFiIN88US=> MmXPV2FPT0WU
NCI-H1304 Mme3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULFS5R5UUN3ME2zN{4xOzV2IDFOwG0> M33Ob3NCVkeHUh?=
YH-13 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDZTWM2OD1|Mz6yOVM2KCEQvF2= Mm\3V2FPT0WU
RMG-I NWj1b|k1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TWTGlEPTB;M{OuOFI5PSBizszN MnXWV2FPT0WU
LU-65 NX\pRnhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX36dnF5UUN3ME2zOE4yPDB6IDFOwG0> MYDTRW5ITVJ?
GB-1 NGDoe4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTN3LkC3NlkhKM7:TR?= NVvifZR6W0GQR1XS
DU-4475 NEfh[2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fkdmlEPTB;M{WuNVU2OyBizszN MlnKV2FPT0WU
SBC-5 M1v1fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXTbYtKSzVyPUO2MlU6ODJiIN88US=> Mm\kV2FPT0WU
OE33 M3fTdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\hNmlEPTB;M{euO|U4PyBizszN NFjNVoJUSU6JRWK=
C8166 M4DyVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELFbY1KSzVyPUO4MlUzPjdiIN88US=> NFTrfWpUSU6JRWK=
COLO-684 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXITWM2OD1|OD63OFI5KCEQvF2= M{i0Z3NCVkeHUh?=
NCI-H1155 NWDZTmQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrCfGhyUUN3ME2zPU4xPDdzIDFOwG0> NUm2OGlXW0GQR1XS
ATN-1 NHfFc3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTN7Lke3PVIhKM7:TR?= MlX3V2FPT0WU
KARPAS-299 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUm3PJdoUUN3ME2zPU45OzliIN88US=> NVHORnR3W0GQR1XS
KNS-81-FD MorKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrRTWM2OD12MD6zOlA1KCEQvF2= M{LFcXNCVkeHUh?=
NCI-H1563 NVvQdXE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfVcIpJUUN3ME20NU42ODN7IDFOwG0> M3\VZXNCVkeHUh?=
NB14 M3LPOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojwTWM2OD12Mj63NlY{KCEQvF2= M33ORXNCVkeHUh?=
COLO-800 M3P4dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrIUotKSzVyPUSyMlg2OTdiIN88US=> NULKUFJLW0GQR1XS
MS-1 NGnnN25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn71TWM2OD12Mz6wOFg{KCEQvF2= NH3NbmFUSU6JRWK=
OVCAR-8 NGDOfIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTR|Lk[4NFkhKM7:TR?= NWfBTHg2W0GQR1XS
SK-PN-DW NGjGe2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7hToFOUUN3ME20N{45Pzd4IDFOwG0> M1\kT3NCVkeHUh?=
G-402 MnLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTR|LkmwNFYhKM7:TR?= M1\5N3NCVkeHUh?=
NCI-H2291 NHHxR2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTR2LkiwNVchKM7:TR?= NIXPfpJUSU6JRWK=
PC-3 M3HXNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTR3LkiwNlMhKM7:TR?= Mo\SV2FPT0WU
NCI-H1581 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWf4U2FPUUN3ME20OU46QDh7IDFOwG0> Mn;oV2FPT0WU
SW1116 Mn\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjTOnZvUUN3ME20O{4xOTh{IDFOwG0> MUfTRW5ITVJ?
ZR-75-30 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{X5PWlEPTB;NEeuNFI{QSBizszN NX2w[pRwW0GQR1XS
OCI-AML2 NIPnWYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHrfnRKUUN3ME20O{4xQTF6IDFOwG0> NY\lcZM6W0GQR1XS
MDA-MB-231 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXJUWwxUUN3ME20O{43OjR7IDFOwG0> Ml\0V2FPT0WU
ES3 M13scmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DkNWlEPTB;NEiuN|UzQSBizszN NEPmS|dUSU6JRWK=
NCI-H630 NWXsb2hpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHPN3hKSzVyPUS5MlE4PDJiIN88US=> M132UnNCVkeHUh?=
OE19 MkO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHTTWM2OD12OT6yPVAzKCEQvF2= NV\E[lFzW0GQR1XS
NCI-H1573 NHK4PI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;LNlJEUUN3ME20PU43QDZzIDFOwG0> MkDvV2FPT0WU
EW-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;u[2lEPTB;NEmuPVA5PCBizszN NELFendUSU6JRWK=

... Click to View More Cell Line Experimental Data

体内研究 Bosutinib每天按60 mg/kg剂量有效作用于携带Src-转化纤维移植瘤和HT29移植瘤的裸鼠,T/C值分别为18%和30%。[1] Bosutinib口服给药小鼠5天,显著抑制K562 肿瘤生长,这种作用存在剂量依赖性,按100 mg/kg 剂量处理可根除大的肿瘤,按150 mg/kg剂量处理可除去肿瘤,且没有毒性。[2] 与作用于HT29 移植瘤的效果相比,Bosutinib按 75 mg/kg剂量作用于携带Colo205移植瘤的裸鼠,每天两次,可抑制肿瘤生长,提高剂量后不会有更高效果,但是 按50 mg/kg剂量处理则没有效果。[4]

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]
+ 展开

Src和Abl激酶实验:

使用ELISA法测定Src激酶活性。Src(每次反应3单位), 反应buffer(50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.5 mM Na3VO4)和cdc2底物肽,加入不同浓度Bosutinib,然后在30oC下温育10分钟。加入ATP,终浓度为 100 μM,开始反应,30oC下温育1小时,然后加入 EDTA终止反应。在DELFIA 固相基于铕的检测法格板上进行 Abl 激酶实验。2 μM生物素化的肽段结合到链霉亲和素包被的微量滴定板上,在溶于PBS的1 mg/mL 卵清蛋白中进行1.5小时。用PBS/0.1% Tween-80冲洗板1小时,随后用PBS 冲洗。激酶反应在30oC下进行1小时。Abl激酶(10单位)与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 卵清蛋白及不同浓度 Bosutinib混合。加入EDTA反应终止,终浓度为50 mM。使用Eu标记的磷酸酪氨酸抗体和DELFIA增强液监测反应。
细胞实验:[2]
+ 展开
  • Cell lines: Abl-MLV,Rat 2,KU812,K562,和MEG-01
  • Concentrations: 溶于DMSO,终浓度为1 μM 左右
  • Incubation Time: 72小时
  • Method: 用不同浓度Bosutinib处理细胞72小时。在Sigmacote处理的超低结合96孔板上检测Abl-MLV转化纤维的Anchorage非依赖增殖,阻止剩余细胞粘附。使用MTS或 Cell-Glo测定细胞增殖。为了测定细胞周期或者细胞死亡,细胞准备在CycleTest和DNA试剂盒中,用于FACS分析,在荧光激活的细胞分选流式细胞仪中进行分析。
    (Only for Reference)
动物实验:[2]
+ 展开
  • Animal Models: 注射K562细胞的雌性裸鼠
  • Formulation: 悬浮于0.5%甲基纤维素/0.4% Tween-80
  • Dosages: 150 mg/kg/day
  • Administration: 口服饲喂
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (188.51 mM)
Ethanol 2 mg/mL (3.77 mM)
Water 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):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
10mg/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 530.45
化学式

C26H29Cl2N5O3

CAS号 380843-75-4
稳定性 powder
in solvent
别名 N/A

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 (g) = 浓度 (mol/L) x 体积 (L) 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、MSDS / 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、MSDS / 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 Conditions Sponsor/Collaborators Start Date Phases
NCT02228382 Active not recruiting Previously Treated PH + CML Pfizer|Developmental Therapeutics Consortium November 7 2014 Phase 4
NCT03297606 Recruiting Lymphoma Non-Hodgkin|Multiple Myeloma|Advanced Solid Tumors Canadian Cancer Trials Group|AstraZeneca|Bristol-Myers Squibb|Hoffmann-La Roche|Pfizer October 6 2017 Phase 2
NCT03106779 Recruiting Chronic Myelogenous Leukemia Novartis Pharmaceuticals|Novartis October 26 2017 Phase 3
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 dell''Adulto November 2016 Phase 2
NCT02906696 Recruiting Chronic Myelogenous Leukemia M.D. Anderson Cancer Center|Pfizer October 2016 Phase 2

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:

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

  • 回答:

    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

Src Inhibitors with Unique Features

相关Src产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID