PHA-680632 Chemical Structure
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 is an Aurora inhibitor, Aurora A (IC50 = 0.004 uM) over Aurora B (IC50 = 0.172 uM).
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) 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) is a selective Aurora kinase A inhibitor with a median IC50 of 61 nM.
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) is a highly potent and selective inhibitor of Aurora B (Ki, 0.36 nM)
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 is an Aurora kinase/VEGFR2 inhibitor
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.
PHA-680632 is the first representative of a new class of Aurora inhibitors (Aurora A/B/C IC50 at 27, 135 and 120 nM, respectively). This agent has a high potential for further development as an anticancer therapeutic.
PHA-680632 is active on a wide range of cancer cell lines and shows significant tumor growth inhibition in different animal tumor models at well-tolerated doses. The IC50 of PHA-680632 for cell anti-proliferation ranged from 0.11 µM to 5.6 µM. [1]
| Molecular Weight (WM): | 501.62 |
|---|---|
| Formula: | C28H35N7O2 |
| CAS No.: | 398493-79-3 |
| Synonyms: |
N/A
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| Dissolve in (25°C): | DMSO ≥100mg/mL |
| Water <1mg/mL | |
| Ethanol ≥100mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
A collection of 426 FDA approved drugs
A collection of 139 natural products
A collection of 40 chemotherapeutic agents
A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules

Western blot analysis of Histone H3 and Aurora. 0-5μM PHA 680632 was added.
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Western blot analysis of Histone H3 and Aurora. 0-5μM PHA 680632 was added.
Data independently produced by Dr. Zhang of Tianjin Medical University PHA-680632 purchased from Selleck
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