Tozasertib (VX-680, MK-0457)

Name: Tozasertib (VX-680, MK-0457)
Brand: Selleck Chemicals
SKU: S1048
Rating: 5 (99 reviews)

For research use only.

Catalog No.S1048

99 publications

Tozasertib (VX-680, MK-0457) Chemical Structure

CAS No. 639089-54-6

Tozasertib (VX-680, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with K_i_app of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2.

Selleck's Tozasertib (VX-680, MK-0457) has been cited by 99 publications

Nature, 2018, 559(7713):211-216.

PubMed: 29973724 ( click the link to review the publication )

Cancer Cell, 2014, 26(3):414-427

PubMed: 25175806 ( click the link to review the publication )

Cell Stem Cell, 2012, 11(2):179-94

PubMed: 22862944 ( click the link to review the publication )

Cell, 2010, 6;142(3):444-55.

PubMed: 20691903 ( click the link to review the publication )

J Cell Biol, 2021, 220(2)e202008029

PubMed: 33355621 ( click the link to review the publication )

PLoS Biol, 2021, 19(1):e3001029

PubMed: 33395410 ( click the link to review the publication )

Breast Cancer, 2021, 10.1007/s12282-021-01242-z

PubMed: 33813687 ( click the link to review the publication )

J Clin Invest, 2020, 139080

PubMed: 33016928 ( click the link to review the publication )

EMBO Rep, 2020, 3;21(4):e49700

PubMed: 32030856 ( click the link to review the publication )

Cancer Res, 2020, 80(18):3841-3854

PubMed: 32690724 ( click the link to review the publication )

Cancers (Basel), 2020, 12(11)E3172

PubMed: 33126775 ( click the link to review the publication )

Cancers (Basel), 2020, 12(9)E2697

PubMed: 32967224 ( click the link to review the publication )

Mol Cancer Ther, 2020, 10.1158/1535-7163.MCT-19-1017

PubMed: 32847978 ( click the link to review the publication )

Mol Cancer Ther, 2020, 19(4):1008-1017

PubMed: 31848297 ( click the link to review the publication )

Sci Adv, 2020, 6(29):eaba1941

PubMed: 32832623 ( click the link to review the publication )

Toxicol Sci, 2020, kfaa103

PubMed: 32617558 ( click the link to review the publication )

Cancer Res, 2019, 79(1):209-219

PubMed: 30389701 ( click the link to review the publication )

Cell Death Differ, 2019, 26(3):548-564

PubMed: 30050055 ( click the link to review the publication )

Cancers (Basel), 2019, 11(10)

PubMed: 31652588 ( click the link to review the publication )

Cell Death Dis, 2019, 10(6):385

PubMed: 31097686 ( click the link to review the publication )

Cell Death Dis, 2019, 10(6):432

PubMed: 31160567 ( click the link to review the publication )

Cell Chem Biol, 2019, 26(3):390-399.e5

PubMed: 30612951 ( click the link to review the publication )

FEBS J, 2019, 286(5):963-974

PubMed: 30600590 ( click the link to review the publication )

Antiviral Res, 2019, 170:104572

PubMed: 31376425 ( click the link to review the publication )
Toxicol Sci, 2019, 10.1093/toxsci/kfz123

PubMed: 31132080 ( click the link to review the publication )

Sci Rep, 2019, 9(1):1897

PubMed: 30760778 ( click the link to review the publication )

Analyst, 2019, 145(1):97-106

PubMed: 31746831 ( click the link to review the publication )

J Pharm Biomed Anal, 2019, doi: 101016/jjpba2019112962

PubMed: 31711864 ( click the link to review the publication )

Environ Mol Mutagen, 2019, 60(6):513-533

PubMed: 30702769 ( click the link to review the publication )

J Pediatr Hematol Oncol, 2019, 41(6):e359-e370

PubMed: 30702467 ( click the link to review the publication )

Int J Mol Sci, 2018, 19(12)

PubMed: 30544932 ( click the link to review the publication )

Cell Signal, 2018, 52:137-146

PubMed: 30223016 ( click the link to review the publication )

SLAS Discov, 2018, 23(2):132-143

PubMed: 28957641 ( click the link to review the publication )

Anticancer Drugs, 2018, 29(10):1004-1010

PubMed: 30080692 ( click the link to review the publication )

Oncotarget, 2018,

PubMed: 29560108 ( click the link to review the publication )

Neuron, 2017, 94(6):1142-1154

PubMed: 28641113 ( click the link to review the publication )

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

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

Cancer Res, 2017, 77(2):494-508

PubMed: 28069801 ( click the link to review the publication )

Oncogene, 2017, 36(44):6177-6189

PubMed: 28869606 ( click the link to review the publication )

Toxicol Sci, 2017, 162(1):146-166

PubMed: 29106658 ( click the link to review the publication )

J Biol Chem, 2017, 292(36):15028-15038

PubMed: 28739871 ( click the link to review the publication )

Cell Signal, 2017, 39:74-83

PubMed: 28780319 ( click the link to review the publication )

Nat Chem Biol, 2016, 10.1038/nchembio.2017

PubMed: 26829474 ( click the link to review the publication )

Nat Commun, 2016, 7:10180

PubMed: 26782714 ( click the link to review the publication )

EMBO J, 2016, 35(8):803-19

PubMed: 26929011 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2016, 113(50):14366-14371

PubMed: 28182563 ( click the link to review the publication )

Elife, 2016, 5:e11402

PubMed: 26878753 ( click the link to review the publication )

Arch Toxicol, 2016, 291(10):4939-54

PubMed: 26404763 ( click the link to review the publication )
J Biol Chem, 2016, 10.1074/jbc.M116.722751

PubMed: 27226586 ( click the link to review the publication )

Exp Cell Res, 2016, 344(2):153-66

PubMed: 27138904 ( click the link to review the publication )

Cell Cycle, 2016, 15(15):2009-18

PubMed: 27249336 ( click the link to review the publication )

Oncol Rep, 2016, 36(2):819-26

PubMed: 27373675 ( click the link to review the publication )

Biochem Biophys Res Commun, 2016, 473(1):212-8

PubMed: 27003257 ( click the link to review the publication )

Exp Hematol, 2016, 44(3):189-93

PubMed: 26706195 ( click the link to review the publication )

Tumour Biol, 2016, 37(11):14745-14755

PubMed: 27629142 ( click the link to review the publication )

Oncotarget, 2016, 7(18):26580-92

PubMed: 27058891 ( click the link to review the publication )

Nat Cell Biol, 2015, 17(1):31-43

PubMed: 25503564 ( click the link to review the publication )

Nat Commun, 2015, 6:7935

PubMed: 26228240 ( click the link to review the publication )

Clin Cancer Res, 2015, 21(23):5338-48

PubMed: 26152738 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2015, 112(19):5875-82

PubMed: 25883264 ( click the link to review the publication )

Mol Cancer Ther, 2015, 14(2):419-28

PubMed: 25522764 ( click the link to review the publication )

Oncol Rep, 2015, 34(2):803-10

PubMed: 26044736 ( click the link to review the publication )

PLoS One, 2015, 10(7):e0134306

PubMed: 26218638 ( click the link to review the publication )

BMC Res Notes, 2015, 8:484

PubMed: 26415506 ( click the link to review the publication )

Mol Cancer Ther, 2015, 14(6):1354-64

PubMed: 25873592 ( click the link to review the publication )

J Mol Cell Biol, 2014, 6(3):240-54

PubMed: 24847103 ( click the link to review the publication )

Biochim Biophys Acta, 2014, 1843(5):934-44

PubMed: 24480460 ( click the link to review the publication )

Hum Gene Ther, 2014, 25(7):599-608

PubMed: 24568341 ( click the link to review the publication )

Am J Physiol Lung Cell Mol Physiol, 2014, 307(2):L173-85

PubMed: 24838752 ( click the link to review the publication )

Cell Cycle, 2014, 13(12):1885-901

PubMed: 24739512 ( click the link to review the publication )

PLoS One, 2014, 9(9):e108758

PubMed: 25268132 ( click the link to review the publication )

PLoS One, 2014, 9(7):e102741

PubMed: 25048812 ( click the link to review the publication )
Oncol Lett, 2014, 7(1):121-124

PubMed: 24348832 ( click the link to review the publication )

Oncotarget, 2014, 5(17):7498-511

PubMed: 25115395 ( click the link to review the publication )

Cancer Res, 2013, 73(22):6722-33

PubMed: 24101154 ( click the link to review the publication )

Cancer Res, 2013, 73(20):6310-22

PubMed: 24067506 ( click the link to review the publication )

Arthritis Rheum, 2013,

PubMed: 23653330 ( click the link to review the publication )

Mol Cancer Res, 2013, 12(3):433-9

PubMed: 24336958 ( click the link to review the publication )

Mol Cancer Res, 2013, 11(11):1326-36

PubMed: 24008673 ( click the link to review the publication )

J Cell Sci, 2013, 126(Pt 5):1235-46

PubMed: 23321637 ( click the link to review the publication )

J Cell Mol Med, 2013, 17(2):265-76

PubMed: 23301855 ( click the link to review the publication )

Vet Comp Oncol, 2013, 10.1111/vco.12018

PubMed: 23410058 ( click the link to review the publication )

Oncotarget, 2013,

PubMed: 23328114 ( click the link to review the publication )

Eur J Cancer, 2012, 48(15):2417-30

PubMed: 22244830 ( click the link to review the publication )

Oncogene, 2012, 31(31):3584-96

PubMed: 22120720 ( click the link to review the publication )

J Med Chem, 2012, 55(17):7392-416

PubMed: 22803810 ( click the link to review the publication )

Brain Pathol, 2012, 23(3):244-53

PubMed: 22971244 ( click the link to review the publication )

J Neurosci, 2012, 32(32):11050-66

PubMed: 22875938 ( click the link to review the publication )

Biochem Pharmacol, 2012, 83(9):1217-28

PubMed: 22306067 ( click the link to review the publication )

Biochem J, 2012, 447(1):93-102

PubMed: 22784093 ( click the link to review the publication )

Exp Cell Res, 2012, 318(4):336-49

PubMed: 22197704 ( click the link to review the publication )

Cytoskeleton, 2012, 69(10):840-53

PubMed: 22887753 ( click the link to review the publication )

J Biomol Screen, 2012, 18(4):388-99

PubMed: 23134735 ( click the link to review the publication )

Pediatr Surg Int, 2012, 28(6):579-89

PubMed: 22526548 ( click the link to review the publication )

Curr Biol, 2011, 21(16):1356-65

PubMed: 21820309 ( click the link to review the publication )

Cancer Res, 2011, 71(23):7207-15

PubMed: 21978935 ( click the link to review the publication )
J Biol Chem, 2011, 286(42):36304-15

PubMed: 21878642 ( click the link to review the publication )

Biochem J, 2011, 440(1):85-93

PubMed: 21774789 ( click the link to review the publication )

Mol Cancer Ther, 2010, 9(5):1318-27

PubMed: 20388735 ( click the link to review the publication )

Purity & Quality Control

Choose Selective Aurora Kinase Inhibitors

Biological Activity

Description

Targets

Aurora A ^[1] (Cell-free assay)	Aurora C ^[1] (Cell-free assay)	Aurora B ^[1] (Cell-free assay)	FLT3 ^[4] (Cell-free assay)	Bcr-Abl ^[4] (Cell-free assay)
0.6 nM(Ki app)	4.6 nM(Ki app)	18 nM(Ki app)	30 nM(Ki)	30 nM(Ki)

In vitro

Although its multi-kinase profile, VX-680 induces similar cytotoxicity with IC50 of approximately 300 nM and exhibits an AUR B-like inhibitory phenotype of G2/M arrest, endoreduplication and apoptosis in BaF3 cells transfected with ABL or FLT-3 (mutant and wild type) kinases. VX-680 prevents the CAL-62 proliferation in a time-dependent manner. VX-680 treatment for 14 days significantly decreases the number and size of colonies by approximately 70% in the 8305C and 90% in the CAL-62, 8505C and BHT-101. Treatment of the different ATC cells with VX-680 inhibits proliferation with the IC50 between 25 and 150 nM. The VX-680 significantly impairs the ability of the different cell lines to form colonies in soft agar. Analysis of caspase-3 activity indicates that VX-680 induces apoptosis in the different cell lines. CAL-62 cells exposed for 12 hours to VX-680 showed an accumulation of cells with ≥4N DNA content. Time-lapse analysis demonstrates that VX-680-treated CAL-62 cells exit metaphase without dividing. Moreover, histone H3 phosphorylation is abrogated following VX-680 treatment. ^[2] VX-680 has significant inhibitory activity against BCR-Abl bearing the T315I mutation in patient-derived samples. ^[3]

Cell Data

Cell Lines	Assay Type	Activity Description	PMID
BE-13	M1LjNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWTBeWszUUN3ME2wMlAxOzN6IN88US=>	NVWzSZZyW0GQR2LFVi=>
RS4-11	M{PJZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mmf3TWM2OD1yLkCwOFA1KM7:TR?=	M3vuZXNCVkeURWK=
MFH-ino	M37qTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3XZVGlEPTB;MD6wNFk6KM7:TR?=	M33DUHNCVkeURWK=
NTERA-S-cl-D1	NV[0T\|d1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MW\JR\|UxRTBwMEG0N\|Qh\|ryP	NIH1bplUSU6JUlXS
697	NGj3OolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVLKOFl[UUN3ME2wMlAzPDdzIN88US=>	M3HkdHNCVkeURWK=
NALM-6	NEG3eJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Ml\ZTWM2OD1yLkCyOVUzKM7:TR?=	M3XlOXNCVkeURWK=
ES8	NXXjTFJWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHTsN3lKSzVyPUCuNFQ3OTNizszN	MnG0V2FPT1KHUh?=
HUTU-80	NUOwO\|k6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NEfrXZdKSzVyPUCuNFUzQTlizszN	MlPZV2FPT1KHUh?=
MV-4-11	NYD3fFNGT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1LQR2lEPTB;MD6wO\|c5OiEQvF2=	NWPNNpFlW0GQR2LFVi=>
MONO-MAC-6	MoTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1XPXGlEPTB;MD6wO\|g4QSEQvF2=	NWiwNmJYW0GQR2LFVi=>
LC-2-ad	MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYqw[IJTUUN3ME2wMlA5Pzh7IN88US=>	MYTTRW5IWkWU
BL-41	NVnlNJJDT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHnncHhKSzVyPUCuNVA1PDVizszN	NILC[HFUSU6JUlXS
A4-Fuk	MmfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NI\4b3FKSzVyPUCuNVE2PjNizszN	MX;TRW5IWkWU
SW954	M2GwV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYXJR\|UxRTBwMUKyNlkh\|ryP	NHuzfVRUSU6JUlXS
BV-173	MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVLOPXFYUUN3ME2wMlEzPjRzIN88US=>	M2nwVHNCVkeURWK=
TE-11	NGfWWJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYHC[nhjUUN3ME2wMlE1QTh{IN88US=>	M4LKeXNCVkeURWK=
SK-UT-1	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1zGSWlEPTB;MD6xOVk3PSEQvF2=	MXnTRW5IWkWU
SIG-M5	NUfYSGM1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MonUTWM2OD1yLkG2O\|A4KM7:TR?=	MUHTRW5IWkWU
OCUB-M	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3r0SWlEPTB;MD6xOlk5OyEQvF2=	Mm\SV2FPT1KHUh?=
K052	Mnn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFvaXWZKSzVyPUCuNVk1QCEQvF2=	MWPTRW5IWkWU
VA-ES-BJ	MnrkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXnJR\|UxRTBwMkCwPFYh\|ryP	M2OzT3NCVkeURWK=
SW982	NXH3ZVlST3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NEnBV5lKSzVyPUCuNlE{QCEQvF2=	M4jBcnNCVkeURWK=
LB647-SCLC	NF[x[o1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NUTuO5VoUUN3ME2wMlIyPTJ\|IN88US=>	M{\3XXNCVkeURWK=
PSN1	NF7p[4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXfEdJd{UUN3ME2wMlIzODJ4IN88US=>	M2\PTnNCVkeURWK=
BB30-HNC	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXTJR\|UxRTBwMkK1PVEh\|ryP	Mnu1V2FPT1KHUh?=
ST486	Ml7FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXLJR\|UxRTBwMkOwPFch\|ryP	NGLEdG1USU6JUlXS
MOLT-4	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHv2PVRKSzVyPUCuNlM{OzdizszN	NV;JfI9zW0GQR2LFVi=>
EW-16	M2DhdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXOyW4ZCUUN3ME2wMlI{PzZ6IN88US=>	MnHTV2FPT1KHUh?=
KS-1	NGi2ZnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MV\JR\|UxRTBwMkO3PFUh\|ryP	MVrTRW5IWkWU
SR	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVTt[GpMUUN3ME2wMlI1PTZ2IN88US=>	M1;4cHNCVkeURWK=
KM12	M{DnOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUXJR\|UxRTBwMk[zOkDPxE1?	M3jRXHNCVkeURWK=
EM-2	NWDEfHN6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWnJR\|UxRTBwMk[2OFEh\|ryP	MmnZV2FPT1KHUh?=
MEG-01	NGfQbpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MkT4TWM2OD1yLkK3PFQ6KM7:TR?=	M2frRnNCVkeURWK=
NB13	NF\rTI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MX7JR\|UxRTBwMke5PFQh\|ryP	MkPHV2FPT1KHUh?=
RKO	NV;pXFkyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MV;JR\|UxRTBwM{C4NVMh\|ryP	NFLBSHRUSU6JUlXS
CESS	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUnNfVF[UUN3ME2wMlMyOzJ6IN88US=>	NYLTTG5[W0GQR2LFVi=>
EoL-1-cell	MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3vGbWlEPTB;MD6zN\|Q2QSEQvF2=	NHXwdo1USU6JUlXS
DOHH-2	MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYfJR\|UxRTBwM{O3PFEh\|ryP	MkDxV2FPT1KHUh?=
A388	MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MX;JR\|UxRTBwM{SwPFYh\|ryP	MnvuV2FPT1KHUh?=
LAMA-84	NVW4co5FT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHrnXVRKSzVyPUCuN\|UyPzhizszN	MkfZV2FPT1KHUh?=
IMR-5	Mn\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MoW1TWM2OD1yLkO1OVQh\|ryP	M1:2eHNCVkeURWK=
KARPAS-422	MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFe5RplKSzVyPUCuN\|czPzJizszN	M2fW[3NCVkeURWK=
MRK-nu-1	Mo\qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXHJR\|UxRTBwM{ixN{DPxE1?	NFr6WVhUSU6JUlXS
BL-70	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NEXwXlBKSzVyPUCuN\|g6PzRizszN	NULaPVB6W0GQR2LFVi=>
LXF-289	M4PBOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoXPTWM2OD1yLkSwOFA3KM7:TR?=	MUTTRW5IWkWU
RL95-2	NX;KfI16T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVXJR\|UxRTBwNEC1Olch\|ryP	MYrTRW5IWkWU
QIMR-WIL	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXvVWZg2UUN3ME2wMlQzPjd4IN88US=>	M4D2UnNCVkeURWK=
K-562	MlTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M4DJ[WlEPTB;MD60N\|Q4OiEQvF2=	NFjyXZFUSU6JUlXS
NCI-H510A	Ml;jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFTUdIpKSzVyPUCuOFM5OjNizszN	NE\CSnBUSU6JUlXS
NCI-H524	NGHKR29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Ml\DTWM2OD1yLkWxNVQ4KM7:TR?=	MYnTRW5IWkWU
KE-37	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHTWcXVKSzVyPUCuOVIyODJizszN	NWnsUmI4W0GQR2LFVi=>
KP-N-YS	M2jQb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYXMe4M3UUN3ME2wMlU1Ozl{IN88US=>	MkPVV2FPT1KHUh?=
LS-411N	MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MUHJR\|UxRTBwNUe3OVIh\|ryP	M{\NNXNCVkeURWK=
CTV-1	MnruS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUTJR\|UxRTBwNUi3O\|Mh\|ryP	MWnTRW5IWkWU
NCI-SNU-16	NHjHTJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NIqweHFKSzVyPUCuOlM2PzFizszN	Mly2V2FPT1KHUh?=
HT-144	M33ifmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NV;Y[ZpOUUN3ME2wMlY{Pzl6IN88US=>	NHjES4JUSU6JUlXS
NCI-H187	NHHqbXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4XKO2lEPTB;MD62OFE{KM7:TR?=	MYjTRW5IWkWU
OCI-AML2	NEnSbXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NUf4cYhuUUN3ME2wMlY1PDB\|IN88US=>	M2PXcnNCVkeURWK=
CCRF-CEM	NILubJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MV\JR\|UxRTBwNkWzOFYh\|ryP	MX\TRW5IWkWU
ONS-76	MmjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWHhcGN4UUN3ME2wMlY3PDV6IN88US=>	NHTTRpRUSU6JUlXS
IST-SL2	M1;6S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3fBR2lEPTB;MD63NVk5OiEQvF2=	M17NVHNCVkeURWK=
NB6	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NH\wWXJKSzVyPUCuO\|czPTRizszN	MWfTRW5IWkWU
SK-PN-DW	MkfTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NEntSZRKSzVyPUCuO\|kyPCEQvF2=	M3HYTHNCVkeURWK=
HCC1599	NIWyRnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmGyTWM2OD1yLkiwPFc1KM7:TR?=	MWfTRW5IWkWU
MC116	NGHjeI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M3ixRmlEPTB;MD64OVAyOSEQvF2=	Ml:yV2FPT1KHUh?=
TE-15	M1PrU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnnqTWM2OD1yLki1NFk5KM7:TR?=	MUHTRW5IWkWU
HOP-62	MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4i5bGlEPTB;MD64OlMzQSEQvF2=	M2XCUnNCVkeURWK=
TGBC24TKB	M1KwNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3r5TGlEPTB;MD64OlM5PSEQvF2=	MYnTRW5IWkWU
HCE-4	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2frTWlEPTB;MD64PFA3OyEQvF2=	M2nSTnNCVkeURWK=
ALL-PO	MofYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MmL0TWM2OD1yLki4NVc2KM7:TR?=	NXi5Uol3W0GQR2LFVi=>
KGN	M4PlUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MY\JR\|UxRTBwOEm5PVUh\|ryP	NH;MfnBUSU6JUlXS
ML-2	MnG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1i4TGlEPTB;MD65NFI2QSEQvF2=	MX7TRW5IWkWU
ES4	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXPP[mZyUUN3ME2wMlkyOTJ6IN88US=>	MmLFV2FPT1KHUh?=
SF126	M4PicGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkHiTWM2OD1yLkm0PFE6KM7:TR?=	M4TDXHNCVkeURWK=
SK-N-DZ	NH;Kem1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmfLTWM2OD1yLkm2NVg6KM7:TR?=	MlHWV2FPT1KHUh?=
HCC1187	NIX1cZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MV;JR\|UxRTFwMEC1NFUh\|ryP	MoTmV2FPT1KHUh?=
DU-4475	MmjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MonjTWM2OD1zLkCxO\|U3KM7:TR?=	NHXLc5ZUSU6JUlXS
NKM-1	MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUHWRpBMUUN3ME2xMlAzPzd3IN88US=>	NEH1OGZUSU6JUlXS
HL-60	M1jIdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MofkTWM2OD1zLkC2OVc1KM7:TR?=	NH30U5RUSU6JUlXS
SBC-1	NHvWO2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHflUopKSzVyPUGuNVI2PDJizszN	MonGV2FPT1KHUh?=
TE-10	M{DtW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1jSPGlEPTB;MT6xNlk1PiEQvF2=	Mn\IV2FPT1KHUh?=
ETK-1	NI\DPItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYDJR\|UxRTFwMUO2NVMh\|ryP	Ml3oV2FPT1KHUh?=
HAL-01	NYrH[FNKT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3vHbmlEPTB;MT6xOlcxQSEQvF2=	M1nlenNCVkeURWK=
BB65-RCC	M2[yXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoPSTWM2OD1zLkG4NFA2KM7:TR?=	MnfGV2FPT1KHUh?=
EW-1	NYnBVmc2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3nJSmlEPTB;MT6xPFU3OiEQvF2=	MnTGV2FPT1KHUh?=
SK-NEP-1	MkfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NHrsU2pKSzVyPUGuNlEyOTFizszN	M2PRO3NCVkeURWK=
SK-LMS-1	M2Lncmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1fDPGlEPTB;MT6yNlIyOiEQvF2=	NGjKbGpUSU6JUlXS
DEL	NFvTdWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NGjhdJBKSzVyPUGuNlU3PDNizszN	NV\BN3hiW0GQR2LFVi=>
GT3TKB	M1m3[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NH\IOFdKSzVyPUGuNlgxPTdizszN	NI\SeYlUSU6JUlXS
MOLT-16	M3G1PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1XGUmlEPTB;MT6zOVQxPSEQvF2=	MWDTRW5IWkWU
CMK	MnzGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MoPQTWM2OD1zLkSyNVE4KM7:TR?=	NVTpRZVCW0GQR2LFVi=>
NB5	NIj3SmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NUHlZ5RbUUN3ME2xMlY1OjJ7IN88US=>	NVLrfHRDW0GQR2LFVi=>
NCI-H1963	NFfIZ3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXTJR\|UxRTFwN{C1PFMh\|ryP	MVjTRW5IWkWU
KURAMOCHI	MlLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXnJR\|UxRTFwN{i5NVEh\|ryP	NYrLUGt[W0GQR2LFVi=>
TE-8	Mo[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWj0d\|d3UUN3ME2xMlgxOzZ6IN88US=>	MnzVV2FPT1KHUh?=
NCI-H1304	NXPIXWc3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MV7JR\|UxRTFwOEOwO\|Mh\|ryP	MUXTRW5IWkWU
A101D	Ml7yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnT5TWM2OD1zLki3N\|k2KM7:TR?=	NHS0OmhUSU6JUlXS
SCLC-21H	NXv5XpJCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXLFdIZyUUN3ME2xMlk4ODV5IN88US=>	MWXTRW5IWkWU
GB-1	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MlS2TWM2OD1{LkCxOlQ4KM7:TR?=	NX\tTZBbW0GQR2LFVi=>
KARPAS-45	NI\Jb4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MlzSTWM2OD1{LkCyOlU1KM7:TR?=	NW\IZnNMW0GQR2LFVi=>
ATN-1	M4jEbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MonYTWM2OD1{LkCyPFU5KM7:TR?=	MnjFV2FPT1KHUh?=
NCI-H720	MnX5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MWTJR\|UxRTJwME[yOFQh\|ryP	M{G2PXNCVkeURWK=
RPMI-6666	NFL5[21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MV3JR\|UxRTJwMU[yNFch\|ryP	Ml7JV2FPT1KHUh?=
NB17	M3jSXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoT4TWM2OD1{LkK5Nlch\|ryP	NFzlPVdUSU6JUlXS
IST-SL1	NVLvcVlVT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYn4fnB3UUN3ME2yMlI6PzZ3IN88US=>	NVnFbWF3W0GQR2LFVi=>
SH-4	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	Mlv1TWM2OD1{LkOyOFY6KM7:TR?=	MlfrV2FPT1KHUh?=
K5	M1:yO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{f1dGlEPTB;Mj60NFMyQSEQvF2=	M2fSUnNCVkeURWK=
OVCAR-4	MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3OyOGlEPTB;Mj60OlE{KM7:TR?=	MnniV2FPT1KHUh?=
ACN	NFTyfYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVPWSVB{UUN3ME2yMlUxOjF\|IN88US=>	NV\GbWg1W0GQR2LFVi=>
TGW	NFm4fVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXfJR\|UxRTJwNkW4N\|Ih\|ryP	M1\FdnNCVkeURWK=
NCI-H2107	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M{DyUmlEPTB;Mj64N\|cyOSEQvF2=	MUTTRW5IWkWU
NCI-H82	MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUi0PG1{UUN3ME2yMlg{QDN6IN88US=>	MUfTRW5IWkWU
SK-N-FI	M{CzVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYjJR\|UxRTJwOE[4Olgh\|ryP	NHqxVYxUSU6JUlXS
LB1047-RCC	M{jGbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVy1OWxbUUN3ME2yMlg5OTJ4IN88US=>	NUPsT3ZIW0GQR2LFVi=>
LU-134-A	M3HOPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M17aOmlEPTB;Mj64PVI3KM7:TR?=	M4jv[HNCVkeURWK=
NCI-H209	M4i3WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXfHfoNkUUN3ME2yMlkyOjV\|IN88US=>	Mo\tV2FPT1KHUh?=
NOMO-1	MoftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUfJR\|UxRTNwMEKyO\|Qh\|ryP	NFK4O2dUSU6JUlXS
RH-1	NFrXOJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYTJR\|UxRTNwMUeyPVEh\|ryP	MYLTRW5IWkWU
LOUCY	NH2yUGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MljVTWM2OD1\|LkG4Olk{KM7:TR?=	NH7rd3FUSU6JUlXS
TE-9	NYL5U2Q3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVf5VHVLUUN3ME2zMlI3PzN4IN88US=>	MWHTRW5IWkWU
PF-382	M3\Nb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHzyOppKSzVyPUOuN\|U4PzhizszN	MWnTRW5IWkWU
RPMI-8402	NUTkd5VMT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MknKTWM2OD1\|LkW4OlA{KM7:TR?=	NUf2XlhSW0GQR2LFVi=>
HEL	NGi5WGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Ml22TWM2OD1\|Lk[zNkDPxE1?	NFLoOYZUSU6JUlXS
NOS-1	NUS0XYhjT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MVjJR\|UxRTNwOES3OVQh\|ryP	MWHTRW5IWkWU
ES1	NFHXO4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYOwOJBiUUN3ME2zMlkzOjl\|IN88US=>	NXSwcmFKW0GQR2LFVi=>
NCI-H2171	M33Edmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NXiwXWFbUUN3ME2zMlkzPDJ\|IN88US=>	NYLERlREW0GQR2LFVi=>
NCI-H747	MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2TOXmlEPTB;Mz65OFIzOSEQvF2=	MoXmV2FPT1KHUh?=
MHH-NB-11	NVjtfoF6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MXnJR\|UxRTNwOUWzNVIh\|ryP	Mny5V2FPT1KHUh?=
MZ1-PC	M1fl[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYXoRlJEUUN3ME2zMlk6OjRizszN	NVK1RmpuW0GQR2LFVi=>
MMAC-SF	MmjRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVOzTIlZUUN3ME20MlAzPDZ5IN88US=>	M3OyeXNCVkeURWK=
NMC-G1	Mn73S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1PzR2lEPTB;ND6yNlczOyEQvF2=	NIHISY1USU6JUlXS
SW872	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NVq2c2NYUUN3ME20MlM1OzRizszN	M3jaenNCVkeURWK=
TE-12	NXj6TXluT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MmPsTWM2OD12LkW2N\|k1KM7:TR?=	MXvTRW5IWkWU
LU-139	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MUjJR\|UxRTRwNkG4N\|Uh\|ryP	MoPCV2FPT1KHUh?=
HC-1	M3TVPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M3f6U2lEPTB;ND62PVQ6PCEQvF2=	MW\TRW5IWkWU
COR-L279	M2HBTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYjLRWROUUN3ME20Mlc2QDlzIN88US=>	NV7WSIRnW0GQR2LFVi=>
SF268	M{fnRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkTtTWM2OD12Lke5PVE3KM7:TR?=	M3uyXHNCVkeURWK=
MC-CAR	M1LyUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MX;JR\|UxRTVwME[3OVch\|ryP	MULTRW5IWkWU
TK10	M2LIfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGPBd3BKSzVyPUWuN\|U1PjlizszN	MnrOV2FPT1KHUh?=
TE-1	MmrzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWmxc\|JPUUN3ME21MlQ6ODB2IN88US=>	NXvFdW9qW0GQR2LFVi=>
NCI-H2126	MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MUPJR\|UxRTVwNkS1O\|Qh\|ryP	MVjTRW5IWkWU
Daudi	NELVe5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmTiTWM2OD13Lk[5NVIh\|ryP	NFHvdVRUSU6JUlXS
NCI-H1648	M3[0PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYHNOYptUUN3ME21MlgyPDV2IN88US=>	Mn7sV2FPT1KHUh?=
OS-RC-2	NVLHb4x[T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NF73WmFKSzVyPUWuPVg2QTdizszN	NXrlbWlwW0GQR2LFVi=>
DJM-1	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYXJR\|UxRTZwM{S2OlYh\|ryP	NH\wUIxUSU6JUlXS
LS-1034	M33FSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NF7rUY5KSzVyPU[uO\|U3PiEQvF2=	MWHTRW5IWkWU
NCI-H1581	NHz5OYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NE\S[IZKSzVyPU[uO\|g1ODVizszN	MXXTRW5IWkWU
UACC-257	MnL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MnHlTWM2OD15LkC0OVEzKM7:TR?=	NXPRU\|BZW0GQR2LFVi=>
KM-H2	M2H1XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NFXue2lKSzVyPUeuNVg1PTdizszN	MXzTRW5IWkWU
NCI-H1436	NWDUUmtNT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MnjZTWM2OD15Lk[5PVMzKM7:TR?=	MkDDV2FPT1KHUh?=
IA-LM	MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NX2zcmVEUUN3ME23Mlg2QSEQvF2=	M4TvZnNCVkeURWK=
NCI-H526	MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MV7JR\|UxRThwMkW2N\|ch\|ryP	NVG3ZoZYW0GQR2LFVi=>
GCIY	NWCwXmJnT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MXjJR\|UxRThwM{[5OlUh\|ryP	MnXlV2FPT1KHUh?=
CP67-MEL	MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVfJR\|UxRThwNUOyOkDPxE1?	NUnXVJoxW0GQR2LFVi=>
KALS-1	M{LEVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmflTWM2OD16LkizPFUyKM7:TR?=	NV\nb\|N{W0GQR2LFVi=>
NCI-H1770	M2LzTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUfJR\|UxRThwOUCyOlUh\|ryP	MlPlV2FPT1KHUh?=
8-MG-BA	NEDS[nFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MXTJR\|UxRTlwM{K4OFQh\|ryP	NWnPVFJ{W0GQR2LFVi=>
KY821	NGnBSGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYO0dldQUUN3ME25Mlc4PDh2IN88US=>	NVfqfpJtW0GQR2LFVi=>
SNB75	NIfVZVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1LJXWlEPTB;MUCuNFc3KM7:TR?=	NF\MbXFUSU6JUlXS
NCCIT	M4nFRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mk\6TWM2OD1zMT6wOVgzKM7:TR?=	NHXpO4xUSU6JUlXS
SJSA-1	NUTBfVlCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NIm5VlJKSzVyPUGxMlI5QTFizszN	NVfiRYhsW0GQR2LFVi=>
LB373-MEL-D	MojHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M{DhRmlEPTB;MUGuN\|gzPyEQvF2=	MljDV2FPT1KHUh?=
TALL-1	MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NH23WnpKSzVyPUGxMlQxPThizszN	NGjsTVBUSU6JUlXS
NB69	NVTJZ5l3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MV7JR\|UxRTFzLke3NFUh\|ryP	M4DtcnNCVkeURWK=
NCI-H1355	MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYK5dGdpUUN3ME2xNU46PDJ4IN88US=>	NGXHTZpUSU6JUlXS
DMS-153	NH;QWIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{LPbGlEPTB;MUKuNFQzPiEQvF2=	MV3TRW5IWkWU
OPM-2	MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHzUT3NKSzVyPUGyMlE2QTZizszN	M4TTRnNCVkeURWK=
NB1	NF7wN4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmL4TWM2OD1zMj6yPUDPxE1?	M2PHbHNCVkeURWK=
A3-KAW	NVHJRWpbT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NIq3[XhKSzVyPUGyMlMzOzZizszN	MlW2V2FPT1KHUh?=
NCI-H1882	NV\MWYVVT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXO5XmhCUUN3ME2xNk41ODZ4IN88US=>	M{m0fXNCVkeURWK=
KG-1	M3j5TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mk\KTWM2OD1zMj62OVQ2KM7:TR?=	NEPsXZBUSU6JUlXS
LC4-1	NHvmN25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{[0[mlEPTB;MUKuO\|cxPiEQvF2=	NH32fVZUSU6JUlXS
HCE-T	M{X5[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlO0TWM2OD1zMz6wNFQ6KM7:TR?=	M3rWOnNCVkeURWK=
NEC8	NYHoXmp{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2HhTGlEPTB;MUOuNVA{QCEQvF2=	MlTtV2FPT1KHUh?=
IST-MEL1	M3THdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHTCUXJKSzVyPUGzMlU4QDhizszN	MkfMV2FPT1KHUh?=
EW-3	NVKzbFd{T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MlTBTWM2OD1zMz63OFAzKM7:TR?=	NG\VWHZUSU6JUlXS
CTB-1	NHy0OJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYrJR\|UxRTF2LkCzNlkh\|ryP	NWe4eFFPW0GQR2LFVi=>
LS-123	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUfnUJpHUUN3ME2xOE4yPTh6IN88US=>	NIrrU\|lUSU6JUlXS
NCI-H1417	M{LKTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MV\JR\|UxRTF2LkOwOVIh\|ryP	NF3uXppUSU6JUlXS
MZ7-mel	M{e2Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkL0TWM2OD1zND60OFM{KM7:TR?=	MmXYV2FPT1KHUh?=
JiyoyeP-2003	NGTibnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NVqxPWVvUUN3ME2xOU43OzJ4IN88US=>	MVvTRW5IWkWU
ES6	M2TFUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYT2VW1WUUN3ME2xOk4zOzZzIN88US=>	NWrOU4RLW0GQR2LFVi=>
HH	MkPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NX;wZ25qUUN3ME2xO{4yQTZ\|IN88US=>	MkTzV2FPT1KHUh?=
SF539	M4PCUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MXvJR\|UxRTF5Lkm5NlIh\|ryP	MoXMV2FPT1KHUh?=
Calu-6	NFHXb5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NGHVZlJKSzVyPUG5MlI{QSEQvF2=	MmH3V2FPT1KHUh?=
SK-MM-2	NYnkV4QyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NX;iU2tGUUN3ME2xPU42PTVizszN	NVzrWpZlW0GQR2LFVi=>
IST-MES1	NXr2TnFzT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGD2XoJKSzVyPUG5MlY3PjNizszN	NX3jVItLW0GQR2LFVi=>
GI-ME-N	MlK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mm\STWM2OD1zOT64NlI4KM7:TR?=	NU\5TldYW0GQR2LFVi=>
CAL-148	NVW4[VJWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXGybZVPUUN3ME2yNE46QTN2IN88US=>	NY\H[Wd2W0GQR2LFVi=>
EVSA-T	MmC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MWTJR\|UxRTJzLkG0PVkh\|ryP	MVXTRW5IWkWU
LP-1	M3;EfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUXJR\|UxRTJzLkO0N\|Ih\|ryP	MWDTRW5IWkWU
BOKU	NVzJbG1XT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MljkTWM2OD1{MT60OVM{KM7:TR?=	NFTaRZlUSU6JUlXS
KLE	NYW4VWlZT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHzpVnlKSzVyPUKyMlE6ODNizszN	M2TYWnNCVkeURWK=
LB831-BLC	MoSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUjJR\|UxRTJ3LkG1NlYh\|ryP	MVjTRW5IWkWU
NCI-H889	M1;aUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MUHJR\|UxRTJ3LkG5N\|Eh\|ryP	NES2RpdUSU6JUlXS
REH	M1rId2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYm3[2ZYUUN3ME2yOU41PjdzIN88US=>	NWq0XXdHW0GQR2LFVi=>
KP-N-RT-BM-1	NYL5VXBwT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NF;DRYdKSzVyPUK1MlQ4PTJizszN	MmC5V2FPT1KHUh?=
MPP-89	NXnuNllHT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NUTFS5l{UUN3ME2yOU42OzF2IN88US=>	NUTXVYpsW0GQR2LFVi=>
no-11	MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MW\JR\|UxRTJ3Lke0O{DPxE1?	M{XRdHNCVkeURWK=
NCI-H748	NV\iUY5tT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NF2xPIVKSzVyPUK1Mlc3OjdizszN	MWXTRW5IWkWU
LB2518-MEL	NFzNcllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MULJR\|UxRTJ5LkG3O\|Mh\|ryP	MWPTRW5IWkWU
TGBC1TKB	MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NH62S2pKSzVyPUK3MlU2QDVizszN	NVryT5lxW0GQR2LFVi=>
MHH-PREB-1	NYHIcYwxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M1L2SWlEPTB;MkiuNFc{PCEQvF2=	MlHXV2FPT1KHUh?=
MZ2-MEL	M1e0[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWTJR\|UxRTJ6Lk[xOFMh\|ryP	MVfTRW5IWkWU
U-266	NEPzOWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYDJR\|UxRTJ6Lk[zOlYh\|ryP	NG[0T3pUSU6JUlXS
SNU-C1	NV\HbFFlT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mn\yTWM2OD1{OD65OFMh\|ryP	MUXTRW5IWkWU
SW962	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MYHJR\|UxRTNyLkK3OFch\|ryP	MWjTRW5IWkWU
Raji	NXq1WlJ6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGfDWWRKSzVyPUOwMlU2QTJizszN	M3[ySnNCVkeURWK=
KNS-42	NUK1XGlYT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4P0eWlEPTB;M{CuPFk2PiEQvF2=	MnHCV2FPT1KHUh?=
LB996-RCC	NVW5Zo1yT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFTwb\|lKSzVyPUOxMlE4ODJizszN	NVzBboJKW0GQR2LFVi=>
CHP-126	NUfsXY1FT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NYDORpN6UUN3ME2zNU4yQTh2IN88US=>	MkmzV2FPT1KHUh?=
RXF393	NH\0ZW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnnQTWM2OD1\|Mj60PVch\|ryP	M2G1PHNCVkeURWK=
COLO-684	NFLWbHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHTSZXBKSzVyPUOyMlY1OzhizszN	M17HVnNCVkeURWK=
A704	MkOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Moq2TWM2OD1\|Mz61OVM5KM7:TR?=	NUKwXYV[W0GQR2LFVi=>
A253	M1LNTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NFT5b4hKSzVyPUOzMlU5PTJizszN	MUXTRW5IWkWU
KNS-81-FD	MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NEn0XY5KSzVyPUO0MlU1PTZizszN	NHvFcJdUSU6JUlXS
TE-441-T	Mn3RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1TnVGlEPTB;M{SuOlM4OSEQvF2=	NYPWd4twW0GQR2LFVi=>
HCC2157	MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHTBSJFKSzVyPUO1MlQ3OTlizszN	MXfTRW5IWkWU
ES3	NXvBNWFRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M37ZU2lEPTB;M{[uOlc2KM7:TR?=	NF3oWpBUSU6JUlXS
NCI-H1155	MmT0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NVjH[mZ[UUN3ME2zO{45OTVizszN	MkP6V2FPT1KHUh?=
SNU-C2B	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUPBN2tZUUN3ME2zPE4yPjV2IN88US=>	MWTTRW5IWkWU
JAR	NEHo[GxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4m4N2lEPTB;M{iuNlQ1QSEQvF2=	MoqxV2FPT1KHUh?=
GDM-1	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHHNNoNKSzVyPUO4MlkyOTZizszN	M1PDOXNCVkeURWK=
KU812	Mm[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NX7vboh5UUN3ME20NU42ODdizszN	Ml7IV2FPT1KHUh?=
BC-1	MlLXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MonyTWM2OD12Mj62O\|MyKM7:TR?=	M13xbHNCVkeURWK=
GI-1	NV\RVmM4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHvvOWJKSzVyPUSyMlkyQTJizszN	NXPHSG9bW0GQR2LFVi=>
NCI-H1694	NGrRU4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4G1OmlEPTB;NESuPVQ4OiEQvF2=	MVzTRW5IWkWU
DG-75	M163dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlHCTWM2OD12NT6xOVc4KM7:TR?=	NInCeolUSU6JUlXS
COR-L88	M3n6NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGrWToRKSzVyPUS1MlI4PzhizszN	NFjUSmdUSU6JUlXS
LS-513	MnPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVTJR\|UxRTR3LkmxOVYh\|ryP	M3HybnNCVkeURWK=
HD-MY-Z	NHrVelJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mn7nTWM2OD12Nj60OlEzKM7:TR?=	MWDTRW5IWkWU
L-363	NXnSR\|VCT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M2S0ZmlEPTB;NE[uPFgyKM7:TR?=	NUXRNllrW0GQR2LFVi=>
TE-6	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXjze\|JxUUN3ME20PE41PDZizszN	MkDqV2FPT1KHUh?=
NCI-H345	NU\KeIs3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MYjJR\|UxRTR6LkS2PEDPxE1?	M4H4d3NCVkeURWK=
TE-5	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NIizNphKSzVyPUS5MlcyOThizszN	NIrpWZNUSU6JUlXS

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	DLK / p-MKK7 / MKK7 / p-JNK / JNK ; PubMed: 23431148 Proc Natl Acad Sci U S A Western blot of the DLK pathway members in RGCs (retinal ganglion cells) 4 h after immunopanning in the presence of 0, 0.03, 0.06, 0.125, 0.25, 0.5, 1, or 2 μM tozasertib. p-AURKA / AURKA / Survivin ; PubMed: 28218735 Oncogenesis BGC823 cells were incubated with indicated doses of VX-680 for 24 h before subjected to western blotting with the indicated antibodies. Densitometry was used to quantify the Survivin and GAPDH levels. The relative expression shown (right panel) are means±s.e.m. of the ratios of Survivin to GAPDH. YAP; PubMed: 31160567 Cell Death Dis Western blot analysis of YAP protein level in A549 cells treated with indicated doses of VX-680 for 24 h. p-AKT / p-GSK3β / Cleaved caspase-3 / Cleaved PARP ; PubMed: 21600017 J Transl Med NB4-R2 cells were collected, lysed and subjected to Western blot analysis with cleaved caspase-3, cleaved-PARP, pAkt-1 (Ser473), pGSK-3β (Ser9) specific antibodies. GAPDH was used as a loading control. Data shown is a representative of three independent experiments.	23431148 28218735 31160567 21600017
Immunofluorescence	α-tubulin / Aurora-A ; PubMed: 21600017 J Transl Med The morphology of mitotic spindle was shown by immunofluorescence staining with anti-α-tubulin antibody and anti-Aur-A antibodies. Microtubules were stained as green, Aur-A protein as red, and nucleus as blue.	21600017
Growth inhibition assay	Cell viability; PubMed: 21600017 J Transl Med VX-680 significantly suppresses the proliferation in a number of leukemic cell types. OCI-AML3, NB4, HL-60 and ML-1 cells were incubated with increasing doses of VX-680 (1, 2, 5 and 10 nM) for 24 hr. Cell viability was measured by MTT assay. Data summarized three independent experiments, p < 0.05, *p < 0.01, compared to control.	21600017

In vivo

VX-680 gives rise to a marked decrease in tumor size in a human AML (HL-60) xenograft model. In mude mice treateed with VX-680 at 75 mg/kg, twice a day intraperitoneally (b.i.d. i.p.) for 13 days, mean tumor volumes are reduced by 98%. Tumor growth decrease is dose dependent and significant at a dose of 12.5 mg/kg b.i.d. VX-680 is well tolerated, with a small decrease in body weight observed only at the highest dose. VX-680 also triggers tumor regresson in pancreatic and colon xenograft models. VX-680 also displays potent antitumor activity when infused i.v. in mude rats bearing established HCT116 tumors. A higher dose of VX-680 (2 mg/kg/h) improves efficacy with a 56% decrease in mean tumor volume. ^[1]

Protocol

Kinase Assay: ^[3]	- Collapse Kinase inhibition assays: The consumption of ATP is coupled via the pyruvate kinase/lactic dehydrogenase enzyme pair to the oxidation of NADH, which can be monitored through the decrease in absorption at 340 nm. Reactions contains 100 mM Tris (pH 8), 10 mM MgCl₂, 2.2 mM ATP, 1 mM phosphoenolpyruvate, 0.6 mg/mL NADH, 75 units/mL pyruvate kinase, 105 units/mL lactate dehydrogenase, and 0.5 mM substrate peptide (sequence: EAIYAAPFAKKK). Reactions (75 μL) are started by adding sufficient kinase to bring the reactions to 30 nM kinase concentration and the decrease in absorbance is monitored over 30 minutes at 30°C in a microtiter plate spectrophotometer. Inhibitory constants are obtained through addition of 3.75 μL VX-680 in 100% DMSO or DMSO alone. Ki values are calculated as follows, K _i = IC50 / (1 + [S]/K_d), where [S] = [ATP] = 2.2 mM, and K_d (of ATP to Abl) = 70 μM. These values are calculated assuming a K_d (ATP) of 70 μM for wild type and H396P Abl kinase domain.
Cell Research: ^[2]	- Collapse Cell lines: CAL-62 cells Concentrations: 5-500 nM Incubation Time: 4 days Method: The CAL-62 cells are cultured in the absence (dimethyl sulfoxide, DMSO) or the presence of 500 nM VX-680 for different periods of time (1-5 days). The dose-dependent effects of VX-680 on cell proliferation are evaluated by treating the different ATC cells for 4 days with different concentrations of the Aurora inhibitor (5–500 nM). The cells are pulse labeled with 30 mM BrdU for 2 hours before the end of the incubation time. The BrdU incorporation is analyzed by means of a colorimetric immunoassay using the cell proliferation ELISA kit. The results from VX-680-treated cells are compared with those observed in control cells and expressed as a fold of variation versus control. (Only for Reference)
Animal Research: ^[1]	- Collapse Animal Models: Female athymic NCr-nu mice bearing HL-60 leukemia cells Dosages: 50 mg/kg, 75 mg/kg Administration: Administered via i.p. (Only for Reference)

References

[4] Cheetham GM, et al. Cancer Lett. 2007, 251(2), 323-329.

- Collapse

Solubility (25°C)

In vitro	DMSO	93 mg/mL (200.17 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+30% PEG 300+2% Tween 80+ddH2O For best results, use promptly after mixing.	15mg/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 Tozasertib (VX-680, MK-0457) SDF

Molecular Weight	464.59
Formula	C₂₃H₂₈N₈OS
CAS No.	639089-54-6
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CC1=CC(=NN1)NC2=CC(=NC(=N2)SC3=CC=C(C=C3)NC(=O)C4CC4)N5CCN(CC5)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

Calculate Reset

Calculation results:

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

Molarity Calculator

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

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

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

Dilution Calculator

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

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

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

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

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

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

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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

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

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

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

Molarity Calculator

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.

Aurora Kinase Signaling Pathway Map

Aurora Kinase Inhibitors with Unique Features

Pan Aurora Kinase Inhibitors

Danusertib (PHA-739358) : Pan-Aurora kinase inhibitor, Aurora A/B/C, IC50=13 nM/79 nM/61 nM.
Pan Aurora Kinase Inhibitors

SNS-314 Mesylate : Pan-Aurora kinase inhibitor, Aurora A/B/C, IC50=9 nM/31 nM/3 nM.
Most Potent Aurora Kinase Inhibitor

MK-5108 (VX-689) : Aurora A, IC50=0.064 nM.
Aurora Kinase Inhibitor in Clinical Trial

Alisertib (MLN8237) : Phase III for Relapsed/Refractory Peripheral T-Cell Lymphoma.
Classic Aurora Kinase Inhibitor

Hesperadin : Potently inhibits Aurora B with IC50 of 250 nM.

Related Aurora Kinase Products

Ro-3306 ^New

RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases. RO-3306 enhances p53-mediated Bax activation and mitochondrial apoptosis.
CCG-1423 ^New

CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.
ML141 ^New

ML141 (CID-2950007) is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. ML141 also protects neuroblastoma cells from metformin-induced apoptosis.
Alisertib (MLN8237)

Alisertib (MLN8237) is a selective Aurora A inhibitor with IC50 of 1.2 nM in a cell-free assay. It has >200-fold higher selectivity for Aurora A than Aurora B. Alisertib induces cell cycle arrest, apoptosis and autophagy. Phase 3.

Features:First orally available inhibitor of Aurora A.
Barasertib (AZD1152-HQPA)

Barasertib (AZD1152-HQPA, AZD2811, INH-34) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.
Danusertib (PHA-739358)

Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2.
ZM 447439

ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.

Features:An Aurora selective ATP-competitive inhibitor.
MLN8054

MLN8054 is a potent and selective inhibitor of Aurora A with IC50 of 4 nM in Sf9 insect cell. It is more than 40-fold selective for Aurora A than Aurora B. Phase 1.
MK-5108 (VX-689)

MK-5108 (VX-689) is a highly selective Aurora A inhibitor with IC50 of 0.064 nM in a cell-free assay and is 220- and 190-fold more selective for Aurora A than Aurora B/C, while it inhibits TrkA with less than 100-fold selectivity. MK-5108 (VX-689) induces autophagy. Phase 1.
Aurora A Inhibitor I (TC-S 7010)

Aurora A Inhibitor I (TC-S 7010) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B. Aurora A Inhibitor I (TC-S 7010) triggers apoptosis through the ROS-mediated UPR signaling pathway.

Features:Aurora A Inhibitor I is a novel, potent, and selective inhibitor to Aurora A.

Choose Your Country or Region

By Signaling Pathways

By product type

Tozasertib (VX-680, MK-0457)