| Size | Price | Stock | Qty |
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| ln Vitro |
Mast cell (MC) proliferation in primary tumors is dose-dependently inhibited by ceneretib (AS-703569) (1-1000 nM; 48 hours) [1]. At low nanomolar concentrations, ceneritibibe (5-100 nM) significantly arrests the G2/M cell cycle in all MC lines over the course of 24 hours [1]. In HMC-1.1, HMC-1.2, C2, and NI-1 cells, ceneretib (1-1000 nM) causes apoptosis in a dose-dependent manner over the course of 24 hours [1]. In HMC-1 subclones, C2 and NI-1 cells, ceneretib (5-500 nM) causes caspase 3 cleavage for a duration of 24 hours [1].
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| ln Vivo |
Tumor growth was markedly suppressed by ceneritib (AS-703569) (oral; 7 or 10 mg/kg/day; for 3 days followed by 4 days of rest; for 4 weeks).
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: HMC-1.1, HMC-1.2, ROSAKIT WT, ROSAKIT D816V and MCPV-1.1 Mast cell Tested Concentrations: 1, 5, 10, 50, 100, 500, 1000 nM Incubation Duration: 48 hrs (hours) Experimental Results: Dose-dependent inhibition of primary tumor MC proliferation. Cell cycle analysis[1] Cell Types: HMC-1.1, HMC-1.2, C2 and NI-1 Cell Tested Concentrations: 5, 10, 50, 100 nM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of massive G2/M cell cycle at 7 The nanomolar concentrations of stasis were low in all MC lines. Apoptosis analysis[1] Cell Types: HMC-1.1, HMC-1.2, C2 and NI-1 Cell Tested Concentrations: 1, 5, 10, 50, 100, 500, 1000 nM Incubation Duration: 24 hrs (hours) Experimental Results: In HMC- Induced apoptosis in 1.1, HMC-1.2, C2 and NI-1 cells in a dose-dependent manner. Western Blot Analysis[1] Cell Types: HMC-1.1, HMC-1.2, C2 and NI-1 Cell Tested Concentrations: 50, 100, 500 nM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of caspase 3 cleaved clones in HMC-1 subcells and in C2 and NI-1 cells. |
| Animal Protocol |
Animal/Disease Models: NCI-MDR tumor-bearing female CB17 severe combined immunodeficiency (SCID) mice [2]
Doses: 7 and 10 mg/kg Route of Administration: Oral; daily; 3 days followed by 4 days rest; continuous 4-week Experimental Results: Dramatically inhibited tumor growth. |
| References | |
| Additional Infomation |
Cenisertib is an aurora kinase inhibitor.
Cenisertib is a water-soluble, synthetic small molecule with potential antineoplastic activity. Cenisertib selectively binds to and inhibits aurora kinases (AKs), a family of serine-threonine kinases which are important regulators of cell division and proliferation, and which are overexpressed in certain types of cancer. Inhibition of aurora kinases inhibits cell division and proliferation and induces apoptosis in tumor cells overexpressing AKs. Drug Indication Investigated for use/treatment in solid tumors, leukemia (myeloid), myelodysplastic syndrome, and cancer/tumors (unspecified). Mechanism of Action R763 is a highly potent and specific inhibitor of Aurora kinase, which has been shown to block proliferation and trigger apoptosis (cell death) in several tumor cell lines including cervical, colon, lung, pancreas and prostate. The over-expression of Aurora kinase can cause cells to rapidly develop an abnormal number of chromosomes. Elevated levels of Aurora kinase are frequently associated with various human cancers and inhibition of this enzyme disrupts cell division and promotes apoptosis. [Rigel Pharmaceuticals Press Release] A probable target for R763 is Aurora kinase A (serine/threonine protein kinase 6). |
| Molecular Formula |
C24H30FN7O
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|---|---|
| Molecular Weight |
451.54
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| Exact Mass |
451.249
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| CAS # |
871357-89-0
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| PubChem CID |
11569967
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
708.3±70.0 °C at 760 mmHg
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| Flash Point |
382.2±35.7 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.669
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| LogP |
0.76
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
33
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| Complexity |
730
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC1=C(C=CC(=C1)NC2=NC=C(C(=N2)N[C@@H]3[C@@H]4C[C@H]([C@@H]3C(=O)N)C=C4)F)N5CCN(CC5)C
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| InChi Key |
KSOVGRCOLZZTPF-QMKUDKLTSA-N
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| InChi Code |
InChI=1S/C24H30FN7O/c1-14-11-17(5-6-19(14)32-9-7-31(2)8-10-32)28-24-27-13-18(25)23(30-24)29-21-16-4-3-15(12-16)20(21)22(26)33/h3-6,11,13,15-16,20-21H,7-10,12H2,1-2H3,(H2,26,33)(H2,27,28,29,30)/t15-,16+,20+,21-/m1/s1
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| Chemical Name |
(1S,2S,3R,4R)-3-[[5-fluoro-2-[3-methyl-4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide
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| Synonyms |
R-763; R 763; R763
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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 |
| 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) |
DMSO : ~250 mg/mL (~553.66 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.61 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 20.8 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: ≥ 2.08 mg/mL (4.61 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 20.8 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: ≥ 2.08 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2146 mL | 11.0732 mL | 22.1464 mL | |
| 5 mM | 0.4429 mL | 2.2146 mL | 4.4293 mL | |
| 10 mM | 0.2215 mL | 1.1073 mL | 2.2146 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.
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