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| 25mg |
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Purity: ≥98%
GSK1070916 (also known as NMI-900 or GSK-1070916A) is a novel, potent, reversible and ATP-competitive inhibitor of Aurora B/C with potential antitumor activity. It inhibits Aurora B/C with IC50 of 3.5 nM/6.5 nM and displays >100-fold selectivity for Aurora B/C over the closely related Aurora A-TPX2 complex. It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. GSK1070916 A binds to and inhibits the activity of Aurora kinases B and C, which may result in inhibition of cellular division and a decrease in the proliferation of tumor cells that overexpress the Aurora kinases B and C. Aurora kinases play essential roles in mitotic checkpoint control during mitosis, and are overexpressed by a wide variety of cancer cell types.
| ln Vitro |
GSK-1070916 has a modest inhibitory impact on Aurora A/TPX2, with a Ki of 492±61 nM, while it significantly inhibits the kinases of Aurora B/INCENP and Aurora C/INCENP, with Ki of 0.38±0.29 and 1.45±0.35 nM, respectively. Additionally, FLT1, TIE2, SIK, FLT4, and FGFR1 are inhibited by GSK-1070916, with IC50 values of 42, 59, 70, 74, and 78 nM, respectively. GSK-1070916 treatment of human lung cancer A549 cells can result in a strong anti-proliferative impact (EC50=7 nM) [1]. GSK-1070916 has been demonstrated to suppress HH3-S10 phosphorylation in all tumor cell lines, with average EC50 values ranging from 8 to 118 nM [2]. The compound also inhibits a panel of tumor cell lines.
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| ln Vivo |
GSK-1070916 injected intraperitoneally (i.p.) suppresses HH3-S10 phosphorylation in a dose-dependent manner in nude mice implanted with human colon tumor (HCT116) xenografts. Upon repeated intraperitoneal (i.p.) administration of GSK-1070916, four out of eight tumor types (lung, A549; colon, HCT116; acute myelogenous leukemia (AML), HL60; and chronic myelogenous leukemia, K562) exhibit complete or partial antitumor activity; three of the eight exhibit stable disease (colon, Colo205; lung, H460; and breast, MCF-7); and one of the eight tumor types (colon, SW620) exhibits tumor growth delay. In general, GSK-1070916 is well tolerated when taken daily[2].
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| References |
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| Additional Infomation |
3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethyl-3-pyrazolyl]phenyl]-1,1-dimethylurea is a member of pyrazoles and a ring assembly.
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| Molecular Formula |
C30H33N7O
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| Molecular Weight |
507.63
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| Exact Mass |
507.274
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| CAS # |
942918-07-2
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| Related CAS # |
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| PubChem CID |
46885626
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.651
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| LogP |
5.19
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
38
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| Complexity |
770
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QTBWCSQGBMPECM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H33N7O/c1-6-37-19-26(28(34-37)21-10-12-23(13-11-21)32-30(38)36(4)5)24-14-15-31-29-25(24)17-27(33-29)22-9-7-8-20(16-22)18-35(2)3/h7-17,19H,6,18H2,1-5H3,(H,31,33)(H,32,38)
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| Chemical Name |
3-[4-[4-[2-[3-[(dimethylamino)methyl]phenyl]-1H-pyrrolo[2,3-b]pyridin-4-yl]-1-ethylpyrazol-3-yl]phenyl]-1,1-dimethylurea
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (3.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (1.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2% Cremophor EL, 2% N,N-dimethylacetamide, pH 5.0:~30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9699 mL | 9.8497 mL | 19.6994 mL | |
| 5 mM | 0.3940 mL | 1.9699 mL | 3.9399 mL | |
| 10 mM | 0.1970 mL | 0.9850 mL | 1.9699 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01118611 | Completed | Drug: Aurora B/C kinase inhibitor GSK1070916A |
Unspecified Adult Solid Tumor, Protocol Specific |
Cancer Research UK | March 2010 | Phase 1 |
Products are for research use only; We do not sell to patients
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