| Identification | Back Directory | [Name]
CD532 | [CAS]
1639009-81-6 | [Synonyms]
CD532
Urea, N-[4-[[4-[(5-cyclopentyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]amino]phenyl]-N'-[3-(trifluoromethyl)phenyl]-
1-[4-({4-[(5-cyclopentyl-1H-pyrazol-3-yl)imino]-1,4-dihydropyrimidin-2-yl}amino)phenyl]-3-[3-(trifluoromethyl)phenyl]urea | [Molecular Formula]
C26H25F3N8O | [MOL File]
1639009-81-6.mol | [Molecular Weight]
522.52 |
| Chemical Properties | Back Directory | [density ]
1.464±0.06 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Ethanol: soluble | [form ]
A solid | [pka]
13.86±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer[1][2]. | [Definition]
ChEBI: CD532 is a member of the class of phenylureas that is urea with 4-[[4-[(5-cyclopentylpyrazol-3-yl)amino]pyrimidin-2-yl]amino]phenyl and 3-[3-(trifluoromethyl)phenyl substituents at positions N1 and N3. It has a role as an antineoplastic agent. It is an aminopyrimidine, a secondary amino compound, a member of pyrazoles, a member of cyclopentanes and a member of phenylureas. | [Biological Activity]
Cell permeable: yes''Primary Target
Aurora A''Reversible: yes''Secondary Target
MYCN | [in vivo]
CD532 (25 mg/kg; i.p. twice weekly for 3 weeks) decreases the tumor volume and increases survival in mice with subcutaneous sonic hedgehog (SHH)-subtype medulloblastoma[1].
CD532 (60 mg/kg; i.p. for 2 days) decreases the level of MYCN protein in MYCN-amplified neuroblastoma xenografts[1].
CD532 (20 mg/kg; i.p.) shows a serum half-life of ~1.5 hours and AUC0-24 of 27 μM?h in mice[1]. | Animal Model: | Homozygous nu/nu mice with SHH-subtype MYCN-expressing medulloblastoma[1] | | Dosage: | 25 mg/kg | | Administration: | I.p. twice weekly for 3 weeks | | Result: | Decreased the level of MYCN protein and tumor volume and increases survival. |
| [IC 50]
Aurora A: 45 nM (IC50) | [storage]
-20°C | [References]
[1] Gustafson WC, et, al. Drugging MYCN through an allosteric transition in Aurora kinase A. Cancer Cell. 2014 Sep 8;26(3):414-427. DOI:10.1016/j.ccr.2014.07.015
[2] Lee JK, et, al. N-Myc Drives Neuroendocrine Prostate Cancer Initiated from Human Prostate Epithelial Cells. Cancer Cell. 2016 Apr 11;29(4):536-547. DOI:10.1016/j.ccell.2016.03.001 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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