Bulk Inquiry
VX 680
- MK 0457 - Tozasertib
- Soluble in DMSO
- MF: C23H28N8OS
- MW: 464.59
Description
VX 680 (Tozasertib, MK-0457) is a potent pan-Aurora kinase inhibitor with reported Ki values of 0.6 nM for Aurora A, 18 nM for Aurora B and 4.6 nM for Aurora C.
Aurora kinases regulate centrosome maturation, chromosome alignment and cytokinesis. VX 680 is useful for studying mitotic catastrophe, spindle checkpoint failure and the contribution of Aurora, ABL and FLT3 kinase signaling to cancer cell growth.
Key Features
- Potent inhibitor of Aurora A, Aurora B and Aurora C
- Reported Ki: 0.6 nM, 18 nM and 4.6 nM for Aurora A/B/C
- Also inhibits clinically relevant kinases including ABL and FLT3
- Induces mitotic defects and antiproliferative responses
Applications
- Aurora kinase pharmacology
- Mitosis and cytokinesis research
- Cancer cell-cycle inhibition studies
- Leukemia and kinase-addiction models
More Information
| Parent CAS No. | 639089-54-6 |
|---|---|
| Chemical Name | Cyclopropanecarboxylic acid {4-[4-(4-methyl-piperazin-1-yl)-6-(5-methyl-1H-pyrazol-3-ylamino)-pyrimidin-2 -ylsulfanyl]-phenyl}-amide |
| SMILES | C1C(NC2C=C(C)NN=2)=NC(SC2C=CC(NC(=O)C3CC3)=CC=2)=NC=1N1CCN(C)CC1 |
| MFCD | MFCD10565966 |
| InChi | InChI=1S/C23H28N8OS/c1-15-13-20(29-28-15)25-19-14-21(31-11-9-30(2)10-12-31)27-23(26-19)33-18-7-5-17(6-8-18)24-22(32)16-3-4-16/h5-8,13-14,16H,3-4,9-12H2,1-2H3,(H,24,32)(H2,25,26,27,28,29) |
| InChiKey | GCIKSSRWRFVXBI-UHFFFAOYSA-N |
| CID | 5494449 |
| Short Description | Aurora inhibitor |
References
- EA Harrington et al. VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nature Medicine 10, 262 - 267 (2004)
- GM Cheetham et al. Structural basis for potent inhibition of the aurora kinases and a T315I multi-drug resistant mutant form of Abl kinase by VX-680. Cancer Lett. 2007, 251, 323-329.
- FJ Giles et al. MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation. Blood 2007, 109, 500-502.
Related Products
| AXON ID | NAME | FROM PRICE |
|---|---|---|
| 1541 | ZM 447439 |
From $93.50 |
| 1580 | AZD1152-HQPA |
From $77.00 |
| 1597 | Aurora A inhibitor I |
From $137.50 |
| 1630 | Aurora A inhibitor II |
From $137.50 |
| 1783 | AMG 900 |
From $121.00 |
| 1836 | CCT 137690 |
From $126.50 |
| 1961 | MK 5108 |
From $121.00 |
| 2003 | MLN8237 |
From $99.00 |
| 2023 | PF 03814735 |
From $132.00 |
| 2096 | Hesperadin |
From $104.50 |
| 2219 | AT 9283 |
From $99.00 |
| 2474 | SPL-B |
From $137.50 |
| 2570 | FG-2216 |
From $88.00 |
| 2906 | SNS 314 mesylate |
From $99.00 |
| 3408 | AKI603 |
From $159.50 |
| 3758 | LY-3295668 |
From Inquiry |
| 3920 | GSK1070916 |
From $121.00 |
| 3973 | XL-228 |
From Inquiry |
| 4073 | CYC-116 |
From Inquiry |
| 4112 | LXY18 |
From $143.00 |
