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
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
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..…
N-Bromosuccinimide Price
- Product number
- 17701
- Product name
- TAK-960
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 17701
- Product name
- TAK-960
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $270
- Updated
- 2024/03/01
- Product number
- 17701
- Product name
- TAK-960
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $419
- Updated
- 2024/03/01
- Product number
- 17701
- Product name
- TAK-960
- Purity
- ≥95%
- Packaging
- 50mg
- Price
- $1189
- Updated
- 2024/03/01
- Product number
- T004940
- Product name
- TAK-960
- Packaging
- 50mg
- Price
- $1050
- Updated
- 2021/12/16
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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