WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406241
Description: UA62784 is a specific inhibitor of centromere protein E (CENPE) kinesin-like protein; mitotic inhibitor. CENP-E is a kinesin-like motor protein that localizes to the kinetochore during mitosis and is essential for bipolar spindle formation. UA62784 is a novel specific inhibitor of CENP-E, which likely binds within the motor domain of CENP-E. UA62784 causes reversible cell cycle arrest in mitosis before metaphase, which leads to apoptosis. The compound is not interacting with microtubules directly.
MedKoo Cat#: 406241
Chemical Formula: C23H15NO3
Exact Mass: 353.10519
Molecular Weight: 353.37
Elemental Analysis: C, 78.17; H, 4.28; N, 3.96; O, 13.58
This product is not in stock, which may be available by custom synthesis.
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Synonym: UA62784, UA62784, UA 62784
IUPAC/Chemical Name: 4-(5-(4-methoxyphenyl)oxazol-2-yl)-9H-fluoren-9-one
InChi Key: SVICLWPFAQYZLX-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H15NO3/c1-26-15-11-9-14(10-12-15)20-13-24-23(27-20)19-8-4-7-18-21(19)16-5-2-3-6-17(16)22(18)25/h2-13H,1H3
SMILES Code: O=C1C2=C(C3=C1C=CC=C3)C(C4=NC=C(C5=CC=C(OC)C=C5)O4)=CC=C2
Appearance: Light yellow to yellow solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 353.37 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Maiato H, Logarinho E. Motor-dependent and -independent roles of CENP-E at kinetochores: the cautionary tale of UA62784. Chem Biol. 2011 Jun 24;18(6):679-80. doi: 10.1016/j.chembiol.2011.06.002. PubMed PMID: 21700202.
2: Tcherniuk S, Deshayes S, Sarli V, Divita G, Abrieu A. UA62784 Is a cytotoxic inhibitor of microtubules, not CENP-E. Chem Biol. 2011 May 27;18(5):631-41. doi: 10.1016/j.chembiol.2011.03.006. PubMed PMID: 21609844.
3: Calligaris D, Lafitte D. Chemical inhibitors: the challenge of finding the right target. Chem Biol. 2011 May 27;18(5):555-7. doi: 10.1016/j.chembiol.2011.05.003. PubMed PMID: 21609834.
4: Shaw AY, Henderson MC, Flynn G, Samulitis B, Han H, Stratton SP, Chow HH, Hurley LH, Dorr RT. Characterization of novel diaryl oxazole-based compounds as potential agents to treat pancreatic cancer. J Pharmacol Exp Ther. 2009 Nov;331(2):636-47. doi: 10.1124/jpet.109.156406. Epub 2009 Aug 5. PubMed PMID: 19657049; PubMed Central PMCID: PMC2775253.
5: Wang H, Stephens B, Von Hoff DD, Han H. Identification and characterization of a novel anticancer agent with selectivity against deleted in pancreatic cancer locus 4 (DPC4)-deficient pancreatic and colon cancer cells. Pancreas. 2009 Jul;38(5):551-7. doi: 10.1097/MPA.0b013e31819d7415. PubMed PMID: 19276868.
6: Henderson MC, Shaw YJ, Wang H, Han H, Hurley LH, Flynn G, Dorr RT, Von Hoff DD. UA62784, a novel inhibitor of centromere protein E kinesin-like protein. Mol Cancer Ther. 2009 Jan;8(1):36-44. doi: 10.1158/1535-7163.MCT-08-0789. PubMed PMID: 19139111; PubMed Central PMCID: PMC2634858.
UA62784 Is a cytotoxic inhibitor of microtubules. UA62784 inhibits microtubule polymerization in vitro. UA62784 interacts with tubulin dimers ten times more potently than colchicine, vinblastine, or nocodazole. UA62784 interacts with tubulin at or near the colchicine-binding site. Nanomolar doses of UA62784 promote the accumulation of mammalian cells in mitosis, due to aberrant mitotic spindles. ( Chem Biol. 2011 May 27;18(5):631-41. doi: 10.1016/j.chembiol.2011.03.006.).