871357-89-0
871357-89-0 structure
- Name: Cenisertib
- Chemical Name: (1S,2S,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
- CAS Number: 871357-89-0
- Molecular Formula: C24H30FN7O
- Molecular Weight: 451.540
- Catalog: Signaling Pathways Cell Cycle/DNA Damage Aurora Kinase
- Create Date: 2016-05-28 12:02:41
- Modify Date: 2025-08-22 22:23:19
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Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC)[1]. Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia[2].
| Name | (1S,2S,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 |
Cenisertib
UNII-5277GPA358 Bicyclo[2.2.1]hept-5-ene-2-carboxamide, 3-[[5-fluoro-2-[[3-methyl-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]-, (1S,2S,3R,4R)- (1S,2S,3R,4R)-3-[(5-Fluoro-2-{[3-methyl-4-(4-methyl-1-piperazinyl)phenyl]amino}-4-pyrimidinyl)amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide |
| Description | Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC)[1]. Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia[2]. |
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| Related Catalog | |
| Target |
Aurora-A Aurora-B ABL1 Akt STAT5 |
| In Vitro | Cenisertib (AS-703569) (1-1000 nM; for 48 hours) induces dose-dependent inhibition of proliferation in primary neoplastic mast cells (MC) [1]. Cenisertib (5-100 nM; for 24 hours) induces a substantial G2/M cell cycle arrest at low nanomolar concentrations in all MC lines[1]. Cenisertib (1-1000 nM; for 24 hours)induces apoptosis in HMC-1.1, HMC-1.2, C2, and NI-1 cells in a dose-dependent manner[1]. Cenisertib (5-500 nM; for 24 hours) induces cleavage of caspase 3 in both HMC-1 sub-clones as well as in C2 and NI-1 cells[1]. Cell Proliferation Assay[1] Cell Line: HMC-1.1, HMC-1.2, ROSAKIT WT, ROSAKIT D816V and MCPV-1.1 mast cells Concentration: 1, 5, 10, 50, 100, 500, 1000 nM Incubation Time: 48 hours Result: Induced dose-dependent inhibition of proliferation in primary neoplastic MC. Cell Cycle Analysis[1] Cell Line: HMC-1.1, HMC-1.2, C2 and NI-1 cells Concentration: 5, 10, 50, 100 nM Incubation Time: 24 hours Result: Induced a substantial G2/M cell cycle arrest at low nanomolar concentrations in all MC lines. Apoptosis Analysis[1] Cell Line: HMC-1.1, HMC-1.2, C2 and NI-1 cells Concentration: 1, 5, 10, 50, 100, 500, 1000 nM Incubation Time: 24 hours Result: Induced apoptosis in HMC-1.1, HMC-1.2, C2, and NI-1 cells in a dose-dependent manner. Western Blot Analysis[1] Cell Line: HMC-1.1, HMC-1.2, C2 and NI-1 cells Concentration: 50, 100, 500 nM Incubation Time: 24 hours Result: Induced cleavage of caspase 3 in both HMC-1 sub-clones as well as in C2 and NI-1 cells. |
| In Vivo | Cenisertib (AS-703569) (orally; 7 or 10 mg/kg/day; for 3 days) significantly suppresses tumor growth. Animal Model: Female CB17 Severe Combined Immunodeficiency (SCID) mice bearing NCI-MDR tumors[2] Dosage: 7 and 10 mg/kg Administration: Orally; daily; for 3 days Result: Suppressed significantly tumor growth. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 708.3±70.0 °C at 760 mmHg |
| Molecular Formula | C24H30FN7O |
| Molecular Weight | 451.540 |
| Flash Point | 382.2±35.7 °C |
| Exact Mass | 451.249573 |
| PSA | 103.63000 |
| LogP | 0.76 |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Index of Refraction | 1.669 |