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;Polo-like Kinase (PLK),cell,cancer,proliferation,Inhibitor,mitosis,TAK960,TAK 960,leukemia,inhibit,phosphorylation,lines,TAK-960;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;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)-
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
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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

Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
Advantage
55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
Wuhan Kaymke Chemical Co., Ltd.,
Tel
027-027-87342388 18086026008
Fax
027-87342388
Email
sales@kaymke.com
Country
China
ProdList
3870
Advantage
55
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4861
Advantage
58
AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Fax
+1 (866) 333-9607
Email
info@adooq.com
Country
United States
ProdList
2782
Advantage
58
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4456
Advantage
55

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
  • 1137868-52-0
  • C27H34F3N7O3