TAK-960

CAT: 0013-GTR19157392-01Size: 200 mgDry Ice: NoHazardous: No

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CAT#:0013-GTR19157392-01Size:200 mg

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Description

TAK-960 is an orally bioavailable selective inhibitor of Plks with IC50 values of 0.8 16.9 and 50.2 nM for Plk1 Plk2 and Plk3 respectively. (In Vitro) :TAK-960 treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3) . TAK-960 (2-1000 nM; 72 hours) inhibits proliferation of multiple cancer cell lines, with mean EC50 values ranging from 8.4 to 46.9 nM, but not in nondividing normal cells.TAK-960 (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells. (In Vivo) :TAK-960 exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts.In animal models, TAK-960 (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts.

CAS Number

1137868-52-0

Field of Research

Epigenetics & Chromatin

Purity

>98% (HPLC)

Solubility

DMSO:35 mg/mL (62.32 mM)

Smiles

COc1cc (C (=O) NC2CCN (C) CC2) c (F) cc1Nc1ncc2N (C) C (=O) C (F) (F) CN (C3CCCC3) c2n1

Molecular Formula

C27H34F3N7O3

Molecular Weight

561.6

Storage Conditions

Storage temperature: -20°C. Stability: ≥ 2 years

Notes

For research use only.

Other Product Names

4- ((9-cyclopentyl-77-difluoro-5-methyl-6-oxo-6789-tetrahydro-5H-pyrimido[45-b][14]diazepin-2-yl) amino) -2-fluoro-5-methoxy-N- (1-methylpiperidin-4-yl) benzamide

Chemical Information

Tak-960

PLK1 Inhibitor TAK-960 is an orally available, Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor TAK-960 selectively inhibits PLK1, inducing selective G2/M cell-cycle arrest followed by apoptosis in a variety of tumor cells while causing reversible cell-cycle arrest at the G1 and G2 stages without apoptosis in normal cells. PLK1 inhibition may result in the inhibition of proliferation in PLK1-overexpressed tumor cells. PLK1, named after the polo gene of Drosophila melanogaster, is a serine/threonine kinase crucial in the regulation of mitosis.

CAS Number	1137868-52-0
PubChem CID	53357478
IUPAC Name	4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-8H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide
Molecular Formula	C27H34F3N7O3
Molecular Weight	561.6
XLogP	3.6
Topological Polar Surface Area	103
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	11
Rotatable Bond Count	6
Heavy Atom Count	40
Formal Charge	0
Complexity	903

SMILES

CN1CCC(CC1)NC(=O)C2=CC(=C(C=C2F)NC3=NC=C4C(=N3)N(CC(C(=O)N4C)(F)F)C5CCCC5)OC

InChI

InChI=1S/C27H34F3N7O3/c1-35-10-8-16(9-11-35)32-24(38)18-12-22(40-3)20(13-19(18)28)33-26-31-14-21-23(34-26)37(17-6-4-5-7-17)15-27(29,30)25(39)36(21)2/h12-14,16-17H,4-11,15H2,1-3H3,(H,32,38)(H,31,33,34)

InChIKey

GWRSATNRNFYMDI-UHFFFAOYSA-N

Chemical Structure

2D Structure

CAS: 1137868-52-0

CID: 53357478

Formula: C27H34F3N7O3

MW: 561.6

Interactive 3D Structure

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View on PubChem Raw 3D data

Computed Properties

Property	Value
Molecular Weight	561.6
XLogP3	3.6
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	11
Rotatable Bond Count	6
Exact Mass	561.26752246
Monoisotopic Mass	561.26752246
Topological Polar Surface Area	103 Å²
Heavy Atom Count	40
Formal Charge	0
Complexity	903
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently-Bonded Unit Count	1
Compound Is Canonicalized	Yes

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Catalog	Name
MBS130811-01	TAK-960
MBS132301-01	TAK 960
MVB86896-01	Tak 960 hydrochloride
T39553-01	TAK-960 monohydrochloride
166670	TAK-960-d3
HY-15160B-01	TAK-960 (dihydrochloride)
MBS3846128-01	TAK-960 hydrochloride
MBS5814717	TAK-960 dihydrochloride
A11146-50	TAK-960 50mg
HY-15160C	TAK-960 (monohydrochloride)

TAK-960

Chemical Information

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