Danusertib
| Code | Size | Price |
|---|
| SYN-1095-M100 | 100 mg | Enquire |
Quantity:
| SYN-1095-M001 | 1 mg | £133.00 |
Quantity:
| SYN-1095-M005 | 5 mg | £209.00 |
Quantity:
| SYN-1095-M010 | 10 mg | £373.00 |
Quantity:
| SYN-1095-M050 | 50 mg | £1,123.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Documents
Further Information
Alternate Names/Synonyms:
PHA-739358
Appearance:
Solid.
CAS:
827318-97-8
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS07
Hazards:
H303, H317, H333
InChi:
InChI=1S/C26H30N6O3/c1-30-12-14-31(15-13-30)20-10-8-19(9-11-20)25(33)27-24-21-16-32(17-22(21)28-29-24)26(34)23(35-2)18-6-4-3-5-7-18/h3-11,23H,12-17H2,1-2H3,(H2,27,28,29,33)/t23-/m1/s1
InChiKey:
XKFTZKGMDDZMJI-HSZRJFAPSA-N
Long Description:
Chemical. CAS: 827318-97-8. Formula: C26H30N6O3. MW: 474.6. Aurora kinases are key regulators of protein phosphorylation during mitosis, and these serine/threonine kinases interact with other cellular proteins to help control chromosome assembly and segregation during mitosis. Aurora kinases are often highly expressed in malignancies and solid tumors. Danusertib (PHA-739358) is a small molecule pan- Aurora kinase inhibitor that also has activity against other cancer-relevant kinases such as Bcr-Abl tyrosine kinase. Other off target effects of danusertib include inhibition of receptor tyrosine kinases such as FGFR-1, and TrkA. Danusertib demonstrates nanomolar IC(50) values for the Aurora kinases all under 100nM and it also demonstrates potent anti-proliferation effects in cell proliferation assays with IC(50) values ranging from 20nM for A2780 cells to <200nM.
Molecular Formula:
C26H30N6O3
Molecular Weight:
474.6
Package Type:
Plastic Vial
Precautions:
P261, P272, P280, P302, P352, P333, P313, P321, P363, P501
Product Description:
Aurora kinases are key regulators of protein phosphorylation during mitosis, and these serine/threonine kinases interact with other cellular proteins to help control chromosome assembly and segregation during mitosis. Aurora kinases are often highly expressed in malignancies and solid tumors. Danusertib (PHA-739358) is a small molecule pan- Aurora kinase inhibitor that also has activity against other cancer-relevant kinases such as Bcr-Abl tyrosine kinase. Other off target effects of danusertib include inhibition of receptor tyrosine kinases such as FGFR-1, and TrkA. Danusertib demonstrates nanomolar IC(50) values for the Aurora kinases all under 100nM and it also demonstrates potent anti-proliferation effects in cell proliferation assays with IC(50) values ranging from 20nM for A2780 cells to <200nM.
Purity:
>95%
Signal word:
Warning
Solubility Chemicals:
Soluble in DMSO or ethanol.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile: D. Fancelli, et al.; J. Med. Chem. 49, 7247 (2006) | Targeting aurora kinases with danusertib (PHA-739358) inhibits growth of liver metastases from gastroenteropancreatic neuroendocrine tumors in an orthotopic xenograft model: K. Fraedrich, et al.; Clin. Cancer Res. 18, 4621 (2012) | Splice Modulation Synergizes Cell Cycle Inhibition: A. Kelsey, et al.; ACS Chem. Biol. ahead of print (2020)
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