Bosutinib (SKI-606)

Name: Bosutinib (SKI-606)
Brand: Selleck Chemicals
SKU: S1014
Rating: 5 (99 reviews)

For research use only.

Licensed by Pfizer Catalog No.S1014

99 publications

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

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

Nat Med, 2018, 24(2):232-238

PubMed: 29309057 ( click the link to review the publication )

Cancer Discov, 2016, 6(7):727-39

PubMed: 27231123 ( click the link to review the publication )

Br J Anaesth, 2021, S0007-0912(21)00090-8

PubMed: 33685634 ( click the link to review the publication )

EBioMedicine, 2021, 69:103457

PubMed: 34224975 ( click the link to review the publication )

Cell Chem Biol, 2021, S2451-9456(21)00303-2

PubMed: 34216546 ( click the link to review the publication )

Drug Metab Dispos, 2021, 49(1):53-61

PubMed: 33148688 ( click the link to review the publication )

Phytother Res, 2021, 10.1002/ptr.7089

PubMed: 33792976 ( click the link to review the publication )

Arch Virol, 2021, 166(5):1433-1438

PubMed: 33683474 ( click the link to review the publication )

Hum Cell, 2021, 10.1007/s13577-021-00579-z

PubMed: 34304386 ( click the link to review the publication )

Mol Cell, 2020, 80(6):1104-1122.e9

PubMed: 33259812 ( click the link to review the publication )

Nat Protoc, 2020, 15(2):421-449

PubMed: 31932771 ( click the link to review the publication )

Nat Commun, 2020, 11(1):5842

PubMed: 33203880 ( click the link to review the publication )

Nat Commun, 2020, 11(1):5704

PubMed: 33177525 ( click the link to review the publication )

Nat Commun, 2020, 29;11(1):2086

PubMed: 32350249 ( click the link to review the publication )

Genome Med, 2020, 18;12(1):17

PubMed: 32070411 ( click the link to review the publication )

Gut Microbes, 2020, 12(1):1-20

PubMed: 33006494 ( click the link to review the publication )

Cancers (Basel), 2020, 27;12(5)pii: E1087

PubMed: 32349331 ( click the link to review the publication )

Cancers (Basel), 2020, 13;12(2) pii: E436

PubMed: 32069833 ( click the link to review the publication )

PLoS Pathog, 2020, 16;16(3):e1008341

PubMed: 32176725 ( click the link to review the publication )

Cell Death Dis, 2020, 11(10):831

PubMed: 33024087 ( click the link to review the publication )

FASEB J, 2020, 34(3):3773-3791

PubMed: 31945226 ( click the link to review the publication )

Aging (Albany NY), 2020, 7;12(9):8221-8240

PubMed: 32379705 ( click the link to review the publication )
J Cell Sci, 2020, 14;133(9) pii: jcs240077

PubMed: 32198280 ( click the link to review the publication )

Int J Mol Sci, 2020, 21(23)E9276

PubMed: 33291786 ( click the link to review the publication )

Cancer Cell Int, 2020, 19;20:58

PubMed: 32099531 ( click the link to review the publication )

J Tissue Eng Regen Med, 2020, 14(4):575-587

PubMed: 32061178 ( click the link to review the publication )

Oncol Rep, 2020, 44(6):2581-2594

PubMed: 33125153 ( click the link to review the publication )

Hum Cell, 2020, 10.1007/s13577-020-00420-z

PubMed: 32870449 ( click the link to review the publication )

Hum Cell, 2020, 10.1007/s13577-020-00425-8

PubMed: 32886306 ( click the link to review the publication )

Exp Neurol, 2020, 328:113272

PubMed: 32142802 ( click the link to review the publication )

Blood Adv, 2020, 4(24):6106-6116

PubMed: 33351104 ( click the link to review the publication )

FEBS Lett, 2020, 10.1002/1873-3468.14008

PubMed: 33249578 ( click the link to review the publication )

J Immunother Cancer, 2020, 8(1):e000285

PubMed: 32581055 ( click the link to review the publication )

Nat Cell Biol, 2019, 21(6):778-790

PubMed: 31160710 ( click the link to review the publication )

J Clin Invest, 2019, 129(3):1167-1179

PubMed: 30629551 ( click the link to review the publication )

Haematologica, 2019, 10.3324/haematol.2019.215939

PubMed: 31289206 ( click the link to review the publication )

J Cell Biol, 2019, 218(9):3060-3076

PubMed: 31308216 ( click the link to review the publication )

Cancers (Basel), 2019, 11(6)

PubMed: 31181609 ( click the link to review the publication )

J Physiol, 2019, 597(6):1627-1642

PubMed: 30488437 ( click the link to review the publication )

Front Oncol, 2019, 9:586

PubMed: 31428570 ( click the link to review the publication )

Sci Rep, 2019, 9(1):5309

PubMed: 30926929 ( click the link to review the publication )

Mol Carcinog, 2019, 10.1002/mc.23139

PubMed: 31777985 ( click the link to review the publication )

Molecules, 2019, 24(3)

PubMed: 30754629 ( click the link to review the publication )

Leuk Lymphoma, 2019, 60(1):189-199

PubMed: 29741440 ( click the link to review the publication )

Exp Hematol, 2019, 77:36-40.e2

PubMed: 31493432 ( click the link to review the publication )

BMC Complement Altern Med, 2019, 19(1):105

PubMed: 31113420 ( click the link to review the publication )
Drugs R D, 2019, 19(2):149-166

PubMed: 30919310 ( click the link to review the publication )

Oncotarget, 2019, 10(23):2237-2251

PubMed: 31040916 ( click the link to review the publication )

Leuk Res, 2019, 78:36-44

PubMed: 30711891 ( click the link to review the publication )

Anat Rec (Hoboken), 2019, 302(12):2193-2200

PubMed: 31569304 ( click the link to review the publication )

Cancer Res, 2018, 78(22):6497-6508

PubMed: 30262461 ( click the link to review the publication )

Cancers (Basel), 2018, 10(12)

PubMed: 30572654 ( click the link to review the publication )

Pigment Cell Melanoma Res, 2018, 31(2):253-266

PubMed: 28972303 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(12):2622-2632

PubMed: 30282811 ( click the link to review the publication )

Mol Biol Cell, 2018, 10.1091/mbc.E18-08-0496

PubMed: 30303751 ( click the link to review the publication )

Biochem Pharmacol, 2018, 156:248-264

PubMed: 30142322 ( click the link to review the publication )

Int J Mol Sci, 2018,

PubMed: 29933569 ( click the link to review the publication )

Int J Oncol, 2018, 53(4):1544-1556

PubMed: 30066854 ( click the link to review the publication )

Transl Oncol, 2018, 11(6):1406-1418

PubMed: 30219696 ( click the link to review the publication )

Onco Targets Ther, 2018,

PubMed: 29695913 ( click the link to review the publication )

J Neurol Sci, 2018, 391:90-99

PubMed: 30103978 ( click the link to review the publication )

Biochem Biophys Res Commun, 2018, 502(1):110-115

PubMed: 29787755 ( click the link to review the publication )

Nat Commun, 2017, 1;8(1):1232

PubMed: 29089541 ( click the link to review the publication )

Elife, 2017, 6

PubMed: 28199182 ( click the link to review the publication )

Arch Toxicol, 2017, 91(8):2921-2938

PubMed: 28032146 ( click the link to review the publication )

Mol Cancer Ther, 2017, 16(11):2563-2571

PubMed: 28839001 ( click the link to review the publication )

Mol Cancer Ther, 2017, pii: molcanther.0669

PubMed: 28223426 ( click the link to review the publication )

Mol Cancer Ther, 2017, 16(9):1989-1998

PubMed: 28637715 ( click the link to review the publication )

Transl Lung Cancer Res, 2017, 6(5):600-610

PubMed: 29114475 ( click the link to review the publication )

Biochim Biophys Acta, 2017, 1864(2):440-448

PubMed: 27913209 ( click the link to review the publication )
Oncotarget, 2017, 8(8):13832-13845

PubMed: 28099155 ( click the link to review the publication )

Cell Host Microbe, 2017, 21(6):754-768

PubMed: 28618271 ( click the link to review the publication )

Cancer Res, 2016, 76(23):6937-6949

PubMed: 27758892 ( click the link to review the publication )

Mol Cancer Ther, 2016, 10.1158/1535-7163

PubMed: 27196758 ( click the link to review the publication )

J Neurochem, 2016, 139(4):610-623

PubMed: 27507246 ( click the link to review the publication )

Int J Oncol, 2016, 49(1):402-10

PubMed: 27120977 ( click the link to review the publication )

Hum Mol Genet, 2015, 24(15):4296-305

PubMed: 25948553 ( click the link to review the publication )

Biochem J, 2015, 465(2):271-9

PubMed: 25351958 ( click the link to review the publication )

BMC Genomics, 2015, 16 Suppl 12:S2

PubMed: 26681397 ( click the link to review the publication )

Neuroscience, 2015, 304:316-27

PubMed: 26235435 ( click the link to review the publication )

Neurotox Res, 2015, 27(4):384-98

PubMed: 25782580 ( click the link to review the publication )

Oncotarget, 2015,

PubMed: 26325669 ( click the link to review the publication )

Drug Metab Dispos, 2014, 42(11):1851-7

PubMed: 25165131 ( click the link to review the publication )

Mol Hum Reprod, 2014, 10.1093/molehr/gau073

PubMed: 25180269 ( click the link to review the publication )

PLoS One, 2014, 9(1):e87014

PubMed: 24466315 ( click the link to review the publication )

PLoS One, 2014, 9(10):e111534

PubMed: 25356636 ( click the link to review the publication )

Pharmacogenet Genomics, 2014, 24(1):52-61

PubMed: 24322003 ( click the link to review the publication )

Anticancer Res, 2014, 34(4):1629-35

PubMed: 24692691 ( click the link to review the publication )

Blood, 2013, 122(7):1203-13

PubMed: 23836556 ( click the link to review the publication )

Mol Hum Reprod, 2013, 19(9):570-80

PubMed: 23630234 ( click the link to review the publication )

Pharmgenomics Pers Med, 2013, 6:63-72

PubMed: 24019750 ( click the link to review the publication )

Cancer Res, 2012, 72(5):1229-38

PubMed: 22241084 ( click the link to review the publication )

Mol Cell Biol, 2012, 32(2):320-32

PubMed: 22037769 ( click the link to review the publication )

Blood, 2011, 118(7):1885-98

PubMed: 21680801 ( click the link to review the publication )
Cancer Res, 2010, 70(19):7489-99

PubMed: 20709760 ( click the link to review the publication )

J Virol, 2010, 85(5):2296-303

PubMed: 21177802 ( click the link to review the publication )

J Biol Chem, 2010, 285(11):7977-85

PubMed: 20068039 ( click the link to review the publication )

Purity & Quality Control

Choose Selective Src Inhibitors

Biological Activity

Description

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	Incubation Time	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,
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RPMI-8866	NFvMcWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NWXBPWtmUUN3ME2xMlI3OTB4IDFOwG0>	NFHPbYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzQDh2NEGvK\|5USU6JRWK8M4E,
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OVCAR-8	MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NXzhWVNsUUN3ME20N{43QDB7IDFOwG0>	MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
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PC-3	NHPIVXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NV:3XplKUUN3ME20OU45ODJ\|IDFOwG0>	NVH0PVZXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjh6NESxM{c,W0GQR1XSQE9iRg>?
NCI-H1581	NF\4cZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NHOyTY5KSzVyPUS1Mlk5QDliIN88US=>	M2HPV\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
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ZR-75-30	M3rBVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		M1LyUGlEPTB;NEeuNFI{QSBizszN	M4mwPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
OCI-AML2	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NVTzRVZvUUN3ME20O{4xQTF6IDFOwG0>	MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyPFg1PDFxJ{7TRW5ITVJ:L3G+
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NCI-H1573	M{\OdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NF;S[XBKSzVyPUS5MlY5PjFiIN88US=>	M1i4S\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI5QDR2MT:nQnNCVkeHUkyvZV4>
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fibroblast cells	MoPORY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IGPyZ{11emGwc3\vdo1m\CC{YYSyJIZq[nKxYnzhd5Qh[2WubIOsJGlEPTBiPTCwMlEh\|ryPLh?=	NHzqUIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{G4NVE4OCd-MUexPFEyPzB:L3G+
fibroblast cells	NHHLZolHfW6ldHnvckBie3OjeR?=		NWLlZVNJUW6qaXLpeIlwdiCxZjDoeY1idiClU4LjMZZUemNiZoXzbY9vKHC{b4TlbY4h\XiycnXzd4VlKGmwIILheEBncWK{b3LsZZN1KGOnbHzzJIJ6KEWOSWPBMEBKSzVyIE2gNE4yKM7:TT6=	M2nUNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5OUC1OVg3Lz5zN{mwOVU5PjxxYU6=
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HEK293	M{PvdmZ2dmO2aX;uJIF{e2G7	NVvSNXZbOSCqch?=	M2HufGlvcGmkaYTpc44hd2ZiaIXtZY4h\nWubDDs[Y5ofGhiUFvNXXQyKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMhfXOrbnegSWZUKCh{NEegeI8hOjV7IILld4llfWW\|KTDhd{B{fWK\|dILheIUh[W[2ZYKgNUBpeiCkeTDmcJVwemW\|Y3XuZ4UheG:uYYLpfoF1cW:wIHntcZVvd2G\|YYmsJGlEPTBiPTCwMlE{OyEQvF2u	MlrpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl7NEGxPVMoRjJ7OUSxNVk{RC:jPh?=
Ba/F3	Mn7kSpVv[3Srb36gZZN{[Xl?	NX2zdI1JPDhiaILz	NIjJW\|FKdmirYnn0bY9vKG:oIFLDVk1CSkxzIFW0OVlMKG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBD[S:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEKFUj3BRmwyNW2nZHnheIVlKGOnbHygdJJwdGmoZYLheIlwdiCjZoTldkA1QCCqcoOgZpkhSnKrdHXMbYdpfCCudXPp[oVz[XOnIHHzd4F6NCCJSUWwJF0hOC5zNDFOwG0v	MoqwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzBzM{e5PFEoRjNyMUO3PVgyRC:jPh?=
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Ba/F3	MlrJSpVv[3Srb36gZZN{[Xl?		M{f3SWlvcGmkaYTpc44hd2ZiTmDNM2FNUyCOMkW2WEBufXSjboSgb4lv[XOnIHHjeIl3cXS7IHnuJGJiTjNiY3XscJMh[nlicnHkbY9mdnq7bXH0bYMh[XO\|YYmsJGlEPTBiPTCwMlE2KM7:TT6=	MomzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ7N{C0NFAoRjF4OUewOFAxRC:jPh?=
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Ba/F3	NYrwUHc5SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		M{PLTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgcZVzcW6nIFLhSlMh[2WubIOg[ZhxemW\|c3nu[{BPWE1xQVzLJGwzPT[WIH31eIFvfCCkeTDbN2hefGi7bXnkbY5mKHWydHHr[UBie3OjeTygTWM2OCB;IECuNkDPxE1w	NV;HOXM3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[5O\|A1ODBpPkG2PVcxPDByPD;hQi=>
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Ba/F3	MXfGeY5kfGmxbjDhd5NigQ>?	MlO4OFghcHK\|	Ml;OTY5pcWKrdHnvckBw\iCEQ2KtRWJNOSCTMkWyTEBufXSjboSgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO\|ZXSgbY4hdW:3c3WgRoEwTjNiY3XscJMh[XO\|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBDS1JvQVLMNU1u\WSrYYTl[EBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgOFghcHK\|IHL5JGJzcXSnTHnnbJQhdHWlaX\ldoF{\SCjc4PhfUwhT0l3MDC9JFAvOjR\|IN88UU4>	M4rnWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMUO3PVgyLz5\|MEGzO\|k5OTxxYU6=
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Ba/F3	MlHkSpVv[3Srb36gZZN{[Xl?	NVXjZ\|FWPDhiaILz	MWPJcohq[mm2aX;uJI9nKEKFUj3BRmwyKEV{NUXLJI12fGGwdDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBud3W\|ZTDCZU9HOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGJEWi2DQlyxMY1m\GmjdHXkJINmdGxicILvcIln\XKjdHnvckBi\nSncjC0PEBpenNiYomgRpJqfGWOaXfoeEBtfWOrZnXyZZNmKGG\|c3H5MEBIUTVyIE2gNE4{PTZizszNMi=>	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODF\|N{m4NUc,OzBzM{e5PFE9N2F-
fibroblast cells	M1v2ZWZ2dmO2aX;uJIF{e2G7		MkTPTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiQXLsJJRz[W6\|Zn;ycYVlKHKjdDDmbYJzd2KuYYP0JINmdGy\|LDDJR\|UxKD1iMD60PUDPxE1w	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjF4MUm5OUc,OTZzNkG5PVU9N2F-
Ba/F3	M2jYPWZ2dmO2aX;uJIF{e2G7	M4DjPVQ5KGi{cx?=	MWnJcohq[mm2aX;uJI9nKEKFUj3BRmwyKFR\|MUXJJI12fGGwdDCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBud3W\|ZTDCZU9HOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBi\nSncjC0PEBpenNiYomgRpJqfGWOaXfoeEBtfWOrZnXyZZNmKGG\|c3H5MEBIUTVyIE2gNE43PDJizszNMi=>	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODF\|N{m4NUc,OzBzM{e5PFE9N2F-
Ba/F3	NHfEcIZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?=		NYrUVmpuSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBufXKrbnWgRoFHOyClZXzsd{BmgHC{ZYPzbY5oKHerbHSgeJlx\SCQUF2vRWxMKGK7IGuzTH11cHmvaXTpcoUhfXC2YXvlJIF{e2G7LDDJR\|UxKD1iMTFOwG0v	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjl5MESwNEc,OTZ7N{C0NFA9N2F-
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-
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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+
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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 Oncotarget 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 Mol Cancer Ther 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 eLife 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 Mol Cancer Ther 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 Bioinformatics Proliferation curves for bosutinib, gefitinib and sorafenib in (A) H1650 and (B) H1975. IC50; PubMed: 27903968 Oncotarget 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]	- Collapse 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]	- Collapse 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]	- Collapse Animal Models: Nude female mice injected with K562 cells Dosages: ~150 mg/kg/day Administration: Oral gavage (Only for Reference)

References

- Collapse

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 Download Bosutinib (SKI-606) SDF

Molecular Weight	530.45
Formula	C₂₆H₂₉Cl₂N₅O₃
CAS No.	380843-75-4
Storage	3 years-20°C powder 2 years-80°C 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)

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Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

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

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

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

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The Serial Dilution Calculator Equation

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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):
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Molecular Weight Calculator

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

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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

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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

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-09-06)

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.

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

Src Inhibitors with Unique Features

Most Potent Src Inhibitor

Dasatinib : Src, IC50=0.8 nM.
FDA-approved Src Inhibitor

Dasatinib : Approved by FDA for CML and Ph+ ALL.
Newest Src Inhibitor

PP1 : Potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.
Classic Src Inhibitor

KX2-391 : The first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

Related Src Products

Dasatinib Monohydrate ^New

Dasatinib Monohydrate (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
SU6656 ^New

SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.
PX-478 2HCl ^New

PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.
Saracatinib (AZD0530)

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.

Features:The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.
Dasatinib (BMS-354825)

Dasatinib (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
KX2-391 (Tirbanibulin)

KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.
PP1

PP1 (AGL 1872, EI 275) is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.
PP2

PP2 (AG 1879, AGL 1879), a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.
WH-4-023

WH-4-023 (KIN001-112, KIN112, Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases.
Ibrutinib (PCI-32765)

Ibrutinib (PCI-32765) is a potent and highly selective Brutons tyrosine kinase (Btk) inhibitor with IC50 of 0.5 nM in cell-free assays, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc. Ibrutinib is applicable as a Btk ligand in the synthesis of a series of PROTACs including P13I.

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Bosutinib (SKI-606)