Research Area
Product Type
United States ( Change Country )
CCT129202 Chemical Structure
VX-680 (MK-0457, Tozasertib)
VX-680 (MK-0457, Tozasertib) is the inhibitor of Aurora-A,-B,-C kinases with apparent inhibition constant values of 0.6,18,4.6 nM respectively.
MLN8054
MLN8054 is an Aurora inhibitor, Aurora A (IC50 = 0.004 uM) over Aurora B (IC50 = 0.172 uM).
ZM-447439
ZM-447439 is a poten, selective ATP-competitive Aurora B kinase inhibitor with an IC50 of 50 nM, 1 μM and 250 nM for Aurora B, A and C, respectively.
Danusertib (PHA-739358)
Danusertib (PHA-739358) is a pyrrolo-pyrazole and small molecule aurora kinases and Bcr-Abl kinase inhibitor for aurora A, B, and C with IC50 of 13 nM, 79 nM, and 61 nM, respectively.
MLN8237 (Alisertib)
MLN8237 (Alisertib) is a selective Aurora kinase A inhibitor with a median IC50 of 61 nM.
AT9283
AT9283 is a small molecule a multi-targeted c-ABL, JAK2, Aurora A and B inhibitor with IC50 of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), Jak2 and Jak3, aurora A and B, respectively.
AZD1152-HQPA (Barasertib)
AZD1152-HQPA (Barasertib) is a highly potent and selective inhibitor of Aurora B (Ki, 0.36 nM)
SNS-314
SNS-314 Mesylate is a potent and selective Aurora kinase inhibitor with IC50 of 9, 31, and 3.4 nM for Aurora kinases A, B, and C, respectively.
CYC116
CYC116 is an Aurora kinase/VEGFR2 inhibitor
ENMD-2076
ENMD-2076 is a antiangiogenic and Aurora kinase inhibitor with IC50 of 3, 13, 350, 23, 40, 93 and 120 nM for Flt-3, AurA, AurB, Src, KDR/VEGFR2 and FGFR1.
Biological Activity
CCT129202 is a Aurora kinase inhibitor with IC50 of 0.042 ± 0.022, 0.198 ± 0.05, and 0.227 ± 0.064 μmol/L for Aurora A, Aurora B, and Aurora C, respectively.It showed high selectivity for the Aurora kinases over a panel of other kinases tested and inhibits proliferation in multiple cultured human tumor cell lines. CCT129202 causes the accumulation of human tumor cells with ≥4N DNA content, leading to apoptosis. The results showed that the CCT129202 is an ATP-competitive inhibitor of recombinant Aurora A kinase with a Ki of 49.8 nmol/L. [1][2]
References on CCT129202
- [1] Mol Cancer Ther 2007;6:3147-3157
- [2] Molecular Biology of the Cell August 2003;14：3325–3341
Product Information
| Molecular Weight (WM): | 497.02 |
|---|---|
| Formula: | C23H25ClN8OS |
| CAS No.: | 942947-93-5 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥3mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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T47D Breast cancer cells were pretreated with p-Aurora, Aurora and then treated with the indicated concentrations of CCT129202.
T47D Breast cancer cells were pretreated with p-Aurora, Aurora and then treated with the indicated concentrations of CCT129202.
Data independently produced by Dr Zhang of Tianjin Medical University CCT129202 purchased from Selleck
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T47D Breast cancer cells were pretreated with p-Aurora, Aurora and then treated with the indicated concentrations of CCT129202.
|
Data independently produced by Dr Zhang of Tianjin Medical University
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