Bosutinib (SKI-606)

Licensed by Pfizer Catalog No.S1014

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.

Cited by 16 Publications

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

PubMed: 27231123

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

PubMed: 21680801

Cancer Res, 2010, 70(19):7489-99

PubMed: 20709760

Mol Cancer Ther, 2017, pii: molcanther.0669

PubMed: 28223426

Mol Cancer Ther, 2016, 10.1158/1535-7163

PubMed: 27196758

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

PubMed: 21177802

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

PubMed: 27913209

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

PubMed: 20068039

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

PubMed: 22037769

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

PubMed: 25165131

Mol Hum Reprod, 2014, 10.1093/molehr/gau073

PubMed: 25180269

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

PubMed: 27120977
Neurotox Res, 2015, 27(4):384-98

PubMed: 25782580

PLoS One, 2014, 9(1):e87014

PubMed: 24466315

PLoS One, 2014, 9(10):e111534

PubMed: 25356636

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

PubMed: 24692691

5 Customer Reviews

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.

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	Activity Description	PMID
NB7	NHroPZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3f2PGlEPTB;MD6wPFI{OSBizszN	MnfJV2FPT0WU
SW756	NXzzOWZTT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYXzeZdRUUN3ME2wMlE1ODJ2IDFOwG0>	MWjTRW5ITVJ?
CTV-1	M2ruOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlyxTWM2OD1yLkG2N\|k5KCEQvF2=	NWPKTGU5W0GQR1XS
HSC-4	M2i5dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NU\oO3FMUUN3ME2wMlE4OTV6IDFOwG0>	NWrOTZU3W0GQR1XS
LAMA-84	M{nmeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnjSTWM2OD1yLkK4OlY1KCEQvF2=	NH3PcVNUSU6JRWK=
KU812	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYTJR\|UxRTBwM{SwOlghKM7:TR?=	NWHUcpJYW0GQR1XS
HCC1806	MlnjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2[1cmlEPTB;MD6zOVIyPiBizszN	M1PmV3NCVkeHUh?=
DOK	MlTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWnZbXRoUUN3ME2wMlM4Pzh4IDFOwG0>	MX\TRW5ITVJ?
NCI-H209	NU\pbo14T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYm1bXFjUUN3ME2wMlQxQDB6IDFOwG0>	NF;5UIlUSU6JRWK=
EoL-1-cell	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MX;JR\|UxRTBwNEG1O\|YhKM7:TR?=	MXzTRW5ITVJ?
H9	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYLQbHhNUUN3ME2wMlQ{PDZ2IDFOwG0>	M1PocHNCVkeHUh?=
EM-2	MkTZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Ml3RTWM2OD1yLkSzPFkhKM7:TR?=	M3u1fXNCVkeHUh?=
NCI-H292	Ml3wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NEPVN\|RKSzVyPUCuOFQyODhiIN88US=>	MmLuV2FPT0WU
697	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M{PFbmlEPTB;MD60OVY{OyBizszN	NIPTbmtUSU6JRWK=
BHT-101	MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYrJR\|UxRTBwNE[1PUAh\|ryP	M4C1fnNCVkeHUh?=
BE-13	MmGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVXJR\|UxRTBwNEi1O\|IhKM7:TR?=	M1frRXNCVkeHUh?=
RS4-11	NGXBWZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1:zZ2lEPTB;MD60PFU5PCBizszN	M335d3NCVkeHUh?=
IGROV-1	NU\UTHhOT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3zy[mlEPTB;MD60PFc6PyBizszN	NIfqO4RUSU6JRWK=
KE-37	M2rR[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUDJR\|UxRTBwNEm1NFkhKM7:TR?=	MY\TRW5ITVJ?
BV-173	NWfmeZNDT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NEO3cG9KSzVyPUCuOVA4QTJiIN88US=>	M1fiXXNCVkeHUh?=
MEG-01	MmrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnrjTWM2OD1yLkWxNlE1KCEQvF2=	MnW5V2FPT0WU
LB2241-RCC	NUDOZ\|dET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MW\JR\|UxRTBwNUO3NVghKM7:TR?=	M2\KOHNCVkeHUh?=
ACHN	M{HvTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MVnJR\|UxRTBwNUSwOlkhKM7:TR?=	M4XC[nNCVkeHUh?=
CTB-1	MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MX\JR\|UxRTBwNUS4NkAh\|ryP	NGjBWGFUSU6JRWK=
HT-1080	M1;5T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGDLSXZKSzVyPUCuOVU{PDliIN88US=>	Mm\sV2FPT0WU
CHL-1	NUjMcItvT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MkC5TWM2OD1yLkW1OFY2KCEQvF2=	MWLTRW5ITVJ?
EW-3	MljDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1ryRWlEPTB;MD61OVk{PSBizszN	MVrTRW5ITVJ?
ES1	MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MlTpTWM2OD1yLk[3OFk5KCEQvF2=	MV3TRW5ITVJ?
KASUMI-1	M2fncmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUfJR\|UxRTBwN{KzN{Ah\|ryP	MmDKV2FPT0WU
SW13	MmX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MoW1TWM2OD1yLkezO\|k5KCEQvF2=	MmfjV2FPT0WU
A3-KAW	MoTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYHJR\|UxRTBwN{myNFghKM7:TR?=	MVnTRW5ITVJ?
LB771-HNC	NI\weFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NV3sXG04UUN3ME2wMlg{OTB2IDFOwG0>	M{LkUHNCVkeHUh?=
OC-314	NYW5dIt2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MUDJR\|UxRTBwOE[5OlUhKM7:TR?=	NFXBeGtUSU6JRWK=
MLMA	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFj0S2VKSzVyPUCuPVA3PzViIN88US=>	MlS2V2FPT0WU
KARPAS-45	NHfsSXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4\1UGlEPTB;MD65NlQ3PiBizszN	MXLTRW5ITVJ?
CAL-27	MmW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MkTQTWM2OD1yLkmyPVA3KCEQvF2=	M1zJPHNCVkeHUh?=
SK-NEP-1	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Ml;PTWM2OD1yLkm3NlQ5KCEQvF2=	NUm4[HZzW0GQR1XS
COR-L105	NXrJfXVWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVrJR\|UxRTFwMECzPVQhKM7:TR?=	M3jGU3NCVkeHUh?=
TI-73	NWL0UYZNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFH2VYVKSzVyPUGuNFE3PSBizszN	MYHTRW5ITVJ?
JVM-3	NYr3WVNDT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NV6x[YpLUUN3ME2xMlA2ODF5IDFOwG0>	M1XY[HNCVkeHUh?=
HAL-01	NF\1[VlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlrvTWM2OD1zLkC4PFEhKM7:TR?=	MYnTRW5ITVJ?
QIMR-WIL	M1f4T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmnnTWM2OD1zLkC5NFU5KCEQvF2=	MUfTRW5ITVJ?
HSC-3	M3PvUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{DtPGlEPTB;MT6xNVc5OyBizszN	M13Ec3NCVkeHUh?=
KY821	NV\ySnE4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MXHJR\|UxRTFwMUOzOVEhKM7:TR?=	NGn4N5BUSU6JRWK=
5637	NXjrdXloT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NH;HWHlKSzVyPUGuNVM5ODNiIN88US=>	NVrEeJZWW0GQR1XS
CAL-33	MknsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MULJR\|UxRTFwMUmzNFIhKM7:TR?=	M2fjW3NCVkeHUh?=
ES4	MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXPJR\|UxRTFwMkC3PUAh\|ryP	NYDmbo5OW0GQR1XS
BHY	MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVzJfJppUUN3ME2xMlIzQDl{IDFOwG0>	M1r1dXNCVkeHUh?=
LB1047-RCC	Mm\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MoPLTWM2OD1zLkKzO\|g2KCEQvF2=	MWfTRW5ITVJ?
H4	NESwOlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MUTJR\|UxRTFwMkSyOVUhKM7:TR?=	MlroV2FPT0WU
RPMI-8866	M{i1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmmwTWM2OD1zLkK2NVA3KCEQvF2=	MmCyV2FPT0WU
HO-1-N-1	NEjENplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYm2[Hd3UUN3ME2xMlI3OzZ7IDFOwG0>	NVPkfFhzW0GQR1XS
BB30-HNC	M4XucWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYn4NFJbUUN3ME2xMlI5PzF2IDFOwG0>	M4nLSHNCVkeHUh?=
PC-14	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NGnlTpVKSzVyPUGuNlkzODViIN88US=>	MmqwV2FPT0WU
NUGC-3	MnPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYrJR\|UxRTFwMkmzOVYhKM7:TR?=	M2Hpe3NCVkeHUh?=
A4-Fuk	NV7kS5dTT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NUH5bY51UUN3ME2xMlMxPzB2IDFOwG0>	MWXTRW5ITVJ?
MHH-NB-11	MlfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MkGzTWM2OD1zLkOxN\|g{KCEQvF2=	M{Hz[3NCVkeHUh?=
KOSC-2	M2\DRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NV[4NJl7UUN3ME2xMlMyPzd3IDFOwG0>	NUDWNHd3W0GQR1XS
A498	M1vpcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NInqdmpKSzVyPUGuOFAyOTNiIN88US=>	MoLpV2FPT0WU
KG-1	MmHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlfsTWM2OD1zLkSxNlc{KCEQvF2=	NVXReVl1W0GQR1XS
DEL	NGPEUHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NEHWVVBKSzVyPUGuOFM3PTdiIN88US=>	Mmi4V2FPT0WU
EW-16	MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MkL6TWM2OD1zLkSzPVc{KCEQvF2=	NXLOfJRHW0GQR1XS
BPH-1	M13hVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHu1SVhKSzVyPUGuOFQ5ODViIN88US=>	NIfoR5RUSU6JRWK=
JAR	M3jN[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHK4ZlBKSzVyPUGuOFk{PiBizszN	MlP5V2FPT0WU
J-RT3-T3-5	M1PHbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MorsTWM2OD1zLkWxO\|IzKCEQvF2=	MWDTRW5ITVJ?
A375	Mmj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVrJR\|UxRTFwNUG3O\|IhKM7:TR?=	MmK1V2FPT0WU
SW954	MlT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MV3JR\|UxRTFwNUWwNFchKM7:TR?=	NEHXTlhUSU6JRWK=
Ca9-22	NXzifZpNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NE\tdHJKSzVyPUGuOVYzPiBizszN	M1L5XXNCVkeHUh?=
D-566MG	MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYHyZlAxUUN3ME2xMlU4OTV3IDFOwG0>	MXHTRW5ITVJ?
SCC-15	NIO2V4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MoLKTWM2OD1zLk[xPFA1KCEQvF2=	NFHmd4RUSU6JRWK=
HD-MY-Z	MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWLOXGlzUUN3ME2xMlY{PTh2IDFOwG0>	M4HhZXNCVkeHUh?=
HT-1376	MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVnDS4ZrUUN3ME2xMlY1OzZiIN88US=>	NF;qO4RUSU6JRWK=
CAL-54	NH3xPFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFPXfG1KSzVyPUGuOlU4ODliIN88US=>	NXSwZndPW0GQR1XS
ONS-76	NUXWZZUzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mke1TWM2OD1zLk[3OVUyKCEQvF2=	M{f5O3NCVkeHUh?=
EFO-27	MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4qwbGlEPTB;MT62PFkzKCEQvF2=	M3K5bnNCVkeHUh?=
769-P	Mo\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlzNTWM2OD1zLk[5OVk3KCEQvF2=	M1LhcHNCVkeHUh?=
MV-4-11	MnzFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MkjzTWM2OD1zLk[5PFU3KCEQvF2=	M{TMXHNCVkeHUh?=
NKM-1	NVm2bXp2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NV;Y[WhoUUN3ME2xMlcyQDB{IDFOwG0>	M1jyN3NCVkeHUh?=
LOXIMVI	M4PkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUXJR\|UxRTFwN{S1PVkhKM7:TR?=	NFO5TlZUSU6JRWK=
KYSE-140	NWS0[4E5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mmr5TWM2OD1zLke1OlU2KCEQvF2=	MUPTRW5ITVJ?
ES5	MmrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3TBT2lEPTB;MT64Olc1PyBizszN	MX\TRW5ITVJ?
BB65-RCC	MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVLJR\|UxRTFwOEm4OFkhKM7:TR?=	Mn7NV2FPT0WU
HN	NHKydJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NV\ZcJE{UUN3ME2xMlg6QDd2IDFOwG0>	NHr5[oxUSU6JRWK=
A101D	M4ThT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NF3oT2RKSzVyPUGuPVM3OjhiIN88US=>	MXjTRW5ITVJ?
LoVo	NES0NlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVjJR\|UxRTFwOUe2O\|khKM7:TR?=	M1GwPHNCVkeHUh?=
NCI-H526	NY\VUII3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1zYfmlEPTB;MT65PVMzPSBizszN	MUjTRW5ITVJ?
NCI-H1693	NVO1Z4Z{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1\JZWlEPTB;MT65PVg5QCBizszN	NUnzSpI6W0GQR1XS
OVCAR-4	MlrhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFvrUFNKSzVyPUKuNFA1OzViIN88US=>	MkPpV2FPT0WU
SK-HEP-1	NXf3SXp5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYTQ[IpJUUN3ME2yMlAxPzR3IDFOwG0>	NYDFV\|J4W0GQR1XS
C2BBe1	MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NH7FbVRKSzVyPUKuNFM{PzJiIN88US=>	MUPTRW5ITVJ?
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SH-4	NG\CcJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MoP2TWM2OD1{Mj63NFQ2KCEQvF2=	MUDTRW5ITVJ?
DoTc2-4510	NGL6NGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYrJR\|UxRTJ\|Lk[0O\|IhKM7:TR?=	NGfy[2pUSU6JRWK=
MMAC-SF	NF3YVmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MX\JR\|UxRTJ\|Lk[5NVEhKM7:TR?=	NIX3Z\|dUSU6JRWK=
NCI-H510A	M4Pzemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NUXZdXNYUUN3ME2yN{44QTN7IDFOwG0>	MWfTRW5ITVJ?
HDLM-2	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M{XNe2lEPTB;MkSuNVQ3KCEQvF2=	NYTrOGE5W0GQR1XS
KINGS-1	Mk\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MljBTWM2OD1{ND6yOFIhKM7:TR?=	M2HCenNCVkeHUh?=
NCI-H1648	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnTwTWM2OD1{ND60NFI1KCEQvF2=	MW\TRW5ITVJ?
HCC1187	NVe5ZWZzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mn7pTWM2OD1{NT6wNlM2KCEQvF2=	M16yZ3NCVkeHUh?=
BALL-1	NVfFPXhRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NWCzdpV7UUN3ME2yOU4zODZ{IDFOwG0>	M3e1SnNCVkeHUh?=
SBC-1	NXvYSYZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MmLDTWM2OD1{NT6yPVk{KCEQvF2=	NFLUNldUSU6JRWK=
BFTC-909	NF7IVJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mn;FTWM2OD1{NT6zOVUyKCEQvF2=	MXTTRW5ITVJ?
MOLT-13	M3jYbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mo\oTWM2OD1{NT62O\|Q1KCEQvF2=	M4DVZXNCVkeHUh?=
SW1990	NYC0fVZRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1;nZWlEPTB;MkWuPVY2PSBizszN	M3ruT3NCVkeHUh?=
DK-MG	NGXWdJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnnkTWM2OD1{Nj6wOFQ{KCEQvF2=	NI\PTHVUSU6JRWK=
TE-8	Mnq3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFzPNItKSzVyPUK2MlA3PjhiIN88US=>	NYHheY1kW0GQR1XS
Becker	M2PXOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M2nHUGlEPTB;Mk[uNVU4PCBizszN	NVL1Xnd[W0GQR1XS
KYSE-70	NGi5[29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{TLS2lEPTB;Mk[uOVMyPyBizszN	NHXIR25USU6JRWK=
MKN7	M{DiO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVq2RlBuUUN3ME2yO{44PDd7IDFOwG0>	M1Tu[XNCVkeHUh?=
D-392MG	NFTXeJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MUnJR\|UxRTJ5Lke2PVQhKM7:TR?=	MnK5V2FPT0WU
NH-12	MoHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHjYV4FKSzVyPUK4MlEzOjliIN88US=>	MoCyV2FPT0WU
EW-18	MlT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYDJR\|UxRTJ6LkKyNVghKM7:TR?=	NF7hT\|VUSU6JRWK=
LCLC-97TM1	MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUTWRWJpUUN3ME2yPE4zPzZ{IDFOwG0>	NYTWVpVNW0GQR1XS
NCI-H1770	NV;0T\|BLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NULvZ2pyUUN3ME2yPE4{PTZ4IDFOwG0>	NEXOWodUSU6JRWK=
BT-20	Mkj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGPqUmNKSzVyPUK4MlM3QDViIN88US=>	NWfGb3o2W0GQR1XS
DBTRG-05MG	NXXodXZsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXPZR3REUUN3ME2yPE41QDN6IDFOwG0>	MlXGV2FPT0WU
HPAF-II	MoLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVfJR\|UxRTJ6Lke3PUAh\|ryP	MUjTRW5ITVJ?
SW837	MknTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NEHXSnlKSzVyPUK5MlM{QDViIN88US=>	M4LMfXNCVkeHUh?=
647-V	NXvnPJpQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWTJR\|UxRTJ7LkewNFMhKM7:TR?=	M{Hz[3NCVkeHUh?=
J82	NHHxV2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NIK2dYlKSzVyPUK5MlgxOTNiIN88US=>	NVTVR204W0GQR1XS
MC116	NVr3RlBMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MUPJR\|UxRTNyLkC3N\|MhKM7:TR?=	Ml[wV2FPT0WU
NCI-H69	NWDBUnViT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MX;JR\|UxRTNyLk[wPVMhKM7:TR?=	NX24fFYyW0GQR1XS
NB6	M4Dwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{\4Z2lEPTB;M{GuN\|YzQSBizszN	NYHk[nNNW0GQR1XS
CAL-120	M3;lemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlLBTWM2OD1\|Mj60N\|E4KCEQvF2=	MYjTRW5ITVJ?
U-87-MG	MnWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFq3XZpKSzVyPUOzMlAzPTFiIN88US=>	MV7TRW5ITVJ?
NCI-H1304	NHq1TpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVPlOm1LUUN3ME2zN{4xOzV2IDFOwG0>	NFfuNo9USU6JRWK=
YH-13	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3rkNmlEPTB;M{OuNlU{PSBizszN	MoDTV2FPT0WU
RMG-I	NE\tcXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NUDnOFFtUUN3ME2zN{41Ojh3IDFOwG0>	M{LFUnNCVkeHUh?=
LU-65	MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NIm1dlFKSzVyPUO0MlE1ODhiIN88US=>	MU\TRW5ITVJ?
GB-1	MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MX\JR\|UxRTN3LkC3NlkhKM7:TR?=	Mnz6V2FPT0WU
DU-4475	NHHIUolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmG0TWM2OD1\|NT6xOVU{KCEQvF2=	M2jhcnNCVkeHUh?=
SBC-5	MlzLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUnJR\|UxRTN4LkW5NFIhKM7:TR?=	NGP6b\|BUSU6JRWK=
OE33	M{LlTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NULY[4hYUUN3ME2zO{44PTd5IDFOwG0>	M4rOb3NCVkeHUh?=
C8166	MljJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUHJR\|UxRTN6LkWyOlchKM7:TR?=	M2HEZXNCVkeHUh?=
COLO-684	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M13MdmlEPTB;M{iuO\|QzQCBizszN	NVrTNYlpW0GQR1XS
NCI-H1155	NFzpR21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3zKZmlEPTB;M{muNFQ4OSBizszN	M3;qS3NCVkeHUh?=
ATN-1	NFntcXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlG5TWM2OD1\|OT63O\|kzKCEQvF2=	NWLtZ4lvW0GQR1XS
KARPAS-299	NUHNVXlLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYfJR\|UxRTN7LkizPUAh\|ryP	M2GwbnNCVkeHUh?=
KNS-81-FD	MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MlfwTWM2OD12MD6zOlA1KCEQvF2=	NHfSZplUSU6JRWK=
NCI-H1563	M3L0cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWDWdItlUUN3ME20NU42ODN7IDFOwG0>	MlvWV2FPT0WU
NB14	MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1jFOmlEPTB;NEKuO\|I3OyBizszN	M1fGc3NCVkeHUh?=
COLO-800	MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVnJR\|UxRTR{Lki1NVchKM7:TR?=	MVrTRW5ITVJ?
MS-1	M4\x[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWTJR\|UxRTR\|LkC0PFMhKM7:TR?=	NEXoVIJUSU6JRWK=
OVCAR-8	NUHGTY5PT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MlXNTWM2OD12Mz62PFA6KCEQvF2=	NYHiUlFTW0GQR1XS
SK-PN-DW	M3jGdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4DiOWlEPTB;NEOuPFc4PiBizszN	MX7TRW5ITVJ?
G-402	NX2zO2NqT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3LodGlEPTB;NEOuPVAxPiBizszN	NWL4flh4W0GQR1XS
NCI-H2291	NHfpbHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWC5bWdLUUN3ME20OE45ODF5IDFOwG0>	MXzTRW5ITVJ?
PC-3	M3nuemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NF;jco9KSzVyPUS1MlgxOjNiIN88US=>	Moe0V2FPT0WU
NCI-H1581	Mlf4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIDvNHdKSzVyPUS1Mlk5QDliIN88US=>	MmfnV2FPT0WU
SW1116	MoO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M3T3[WlEPTB;NEeuNFE5OiBizszN	NFvLNmJUSU6JRWK=
ZR-75-30	MmPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVj2XZFbUUN3ME20O{4xOjN7IDFOwG0>	Ml3aV2FPT0WU
OCI-AML2	Mln1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVHJR\|UxRTR5LkC5NVghKM7:TR?=	Mn2xV2FPT0WU
MDA-MB-231	NFzkclRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mn3LTWM2OD12Nz62NlQ6KCEQvF2=	NWTpPGo2W0GQR1XS
ES3	NYXGfIEzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1K5dmlEPTB;NEiuN\|UzQSBizszN	Mn32V2FPT0WU
NCI-H630	MoXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnnVTWM2OD12OT6xO\|QzKCEQvF2=	NX;N[o1IW0GQR1XS
OE19	NELQVHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYfJR\|UxRTR7LkK5NFIhKM7:TR?=	NGXSWllUSU6JRWK=
NCI-H1573	NF71[ohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MX;JR\|UxRTR7Lk[4OlEhKM7:TR?=	MnPyV2FPT0WU
EW-1	NWKyXWV7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWLJR\|UxRTR7LkmwPFQhKM7:TR?=	MVjTRW5ITVJ?

... 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)

References

+ Expand

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
Storage	2 years -80°C in solvent
Synonyms	N/A

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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)

*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).

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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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The Serial Dilution Calculator Equation

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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):
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C8=C7/X	C8:	LOG(C8):

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2018-10-19)

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
NCT01903733	Active not recruiting	Chronic Myeloid Leukemia	Pfizer	August 28 2013	Not Applicable
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

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

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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

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.

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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. 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). Phase 2/3.

Features:The 1st Src inhibitor to show inhibition of the Src pathway in human tumor tissue.
Dasatinib

Dasatinib 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.
KX2-391

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 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.
PP2

PP2, 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 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.

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Bosutinib (SKI-606)

Cited by 16 Publications

5 Customer Reviews

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Protocol

References

Solubility (25°C)

Chemical Information Download Bosutinib (SKI-606) SDF

Bio Calculators

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

Dilution Calculator

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

The Serial Dilution Calculator Equation

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Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2018-10-19)

Tech Support

Frequently Asked Questions

Src Signaling Pathway Map

Src Inhibitors with Unique Features

Related Src Products

Choose Your Country or Region

By Signaling Pathways

By product type

Bosutinib (SKI-606)

Cited by 16 Publications

5 Customer Reviews

Purity & Quality Control

Choose Selective Src Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download Bosutinib (SKI-606) SDF

Bio Calculators

Molarity Calculator

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

Dilution Calculator

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

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

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

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

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2018-10-19)

Tech Support

Frequently Asked Questions

Src Signaling Pathway Map

Src Inhibitors with Unique Features

Related Src Products

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