ChemicalBook > CAS DataBase List > TAK-960

TAK-960

Product Name
TAK-960
CAS No.
1137868-52-0
Chemical Name
TAK-960
Synonyms
CS-554;TAK-960;CS-1725;TAK 960;TAK960;TAK-960 TAK-960,S1239;TAK-960, 10 mM in DMSO;Polo-like Kinase (PLK),cell,cancer,proliferation,Inhibitor,mitosis,TAK960,TAK 960,leukemia,inhibit,phosphorylation,lines,TAK-960;4-((9-cyclopentyl-5,7,7-trimethyl-6-oxo-6,7,8,9-tetrahydro-5h-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-2-fluoro-5-methoxy-n-(1-methylpiperidin-4-yl)benzamide;4-[(9-Cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-N-(1-methyl-4-piperidinyl)benzamide;4-((9-Cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide
CBNumber
CB62628442
Molecular Formula
C27H34F3N7O3
Formula Weight
561.6
MOL File
1137868-52-0.mol
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TAK-960 Property

Density 
1.39±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
≥28.05 mg/mL in DMSO; insoluble in H2O; ≥12.3 mg/mL in EtOH
form 
solid
pka
13.21±0.20(Predicted)
color 
White to light yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
17701
Product name
TAK-960
Purity
≥95%
Packaging
1mg
Price
$62
Updated
2024/03/01
Cayman Chemical
Product number
17701
Product name
TAK-960
Purity
≥95%
Packaging
5mg
Price
$270
Updated
2024/03/01
Cayman Chemical
Product number
17701
Product name
TAK-960
Purity
≥95%
Packaging
10mg
Price
$419
Updated
2024/03/01
Cayman Chemical
Product number
17701
Product name
TAK-960
Purity
≥95%
Packaging
50mg
Price
$1189
Updated
2024/03/01
TRC
Product number
T004940
Product name
TAK-960
Packaging
50mg
Price
$1050
Updated
2021/12/16
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TAK-960 Chemical Properties,Usage,Production

Uses

TAK-960 is a potent and selective inhibitor of polo-like kinase 1 (PLK1), a serine/threonine protein kinase involved in key processes during mitosis. TAK-960 has shown activity in several tumor cell lines, including those that express multidrug-resistant protein 1 (MDR1). TAK-960 treatments has shown significant efficacy against multiple tumor xenografts and is a potential chemotherapeutic agent for patients with advanced tumors.

Biological Activity

polo-like kinase 1 (plk1) is a serine/threonine protein kinase involved in key mitosis processes. human plk1 has been shown to be overexpressed in various human cancers. elevated levels of plk1 have been associated with poor prognosis, making it an attractive target for anticancer therapy. tak-960 is a novel, investigational, orally bioavailable, potent, and selective plk1 inhibitor.

in vitro

tak-960 treatment caused accumulation of g2–m cells, aberrant polo mitosis morphology, and increased the phosphorylation of histone h3. tak-960 inhibited proliferation of multiple cancer cell lines, with mean ec50 ranging from 8.4 to 46.9 nmol/l, but not in nondividing normal cells [1].

in vivo

in animal models, oral administration of tak-960 increased phh3 in a dose-dependent manner and significantly inhibited the growth of ht-29 colorectal cancer xenografts. once daily treatment tak-960 exhibited significant efficacy against multiple tumor xenografts, including an adriamycin/paclitaxel-resistant xenograft model and a disseminated leukemia model [1].

IC 50

8.4 to 46.9 nmol/l for multiple cancer cell lines

References

[1] hikichi y, honda k, hikami k, miyashita h, kaieda i, murai s, uchiyama n, hasegawa m, kawamoto t, sato t, ichikawa t, cao s, nie z, zhang l, yang j, kuida k, kupperman e. tak-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens. mol cancer ther. 2012 mar;11(3):700-9.
[2]
[3]

TAK-960 Preparation Products And Raw materials

Raw materials

Preparation Products

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TAK-960 Suppliers

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1137868-52-0, TAK-960Related Search:


  • TAK-960
  • 4-((9-Cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide
  • 4-[(9-Cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-N-(1-methyl-4-piperidinyl)benzamide
  • CS-1725
  • TAK 960;TAK960
  • CS-554
  • Benzamide, 4-[(9-cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-N-(1-methyl-4-piperidinyl)-
  • Polo-like Kinase (PLK),cell,cancer,proliferation,Inhibitor,mitosis,TAK960,TAK 960,leukemia,inhibit,phosphorylation,lines,TAK-960
  • TAK-960, 10 mM in DMSO
  • TAK-960 TAK-960,S1239
  • 4-((9-cyclopentyl-5,7,7-trimethyl-6-oxo-6,7,8,9-tetrahydro-5h-pyrimido[4,5-b][1,4]diazepin-2-yl)amino)-2-fluoro-5-methoxy-n-(1-methylpiperidin-4-yl)benzamide
  • 1137868-52-0
  • C27H34F3N7O3