| Identification | Back Directory | [Name]
AS703569 | [CAS]
871357-89-0 | [Synonyms]
R763
AS703569
Cenisertib
R763(AS-703569)
AS 703569
(R763
CENISERTIB (AS-703569)
(1S,2S,3R,4R)-3-((5-fluoro-2-((3-Methyl-4-(4-Methylpiperazin-1-yl)phenyl)aMino)pyriMidin-4-yl)aMino)bicyclo[2.2.1]hept-5-ene-2-carboxaMide
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)- | [Molecular Formula]
C24H30FN7O | [MOL File]
871357-89-0.mol | [Molecular Weight]
451.54 |
| Chemical Properties | Back Directory | [Boiling point ]
708.3±70.0 °C(Predicted) | [density ]
1.335±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 250 mg/mL (553.66 mM) | [form ]
Solid | [pka]
16.24±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Cenisertib (AS-703569) is an ATP-competitive 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). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia[1][2][3]. | [in vivo]
Cenisertib (AS-703569) (orally; 7 or 10 mg/kg/day; for 3 days followed by a 4-day rest period; for 4 weeks) 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 followed by a 4-day rest period; for 4 weeks | | Result: | Suppressed significantly tumor growth.
|
| [IC 50]
Aurora-A; Aurora-B; ABL1; STAT5 | [storage]
Store at -20°C | [References]
[1] Peter B, et al. Drug-induced inhibition of phosphorylation of STAT5 overrides drug resistance in neoplastic mast cells. Leukemia. 2018 Apr;32(4):1016-1022. DOI:10.1038/leu.2017.338
[2] McLaughlin J, et al. Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen. J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113. DOI:10.1007/s00432-009-0641-1
[3] Maryam Shariati, et al. Targeting AKT for cancer therapy. Expert Opin Investig Drugs. 2019 Nov;28(11):977-988. DOI:10.1080/13543784.2019.1676726 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
NCE Biomedical Co.,Ltd.
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| Tel: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
m.approvedhomemanagement.com/ShowSupplierProductsList15748/0.htm |
| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
| Company Name: |
cjbscvictory
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| Tel: |
13348960310 13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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