UA62784

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406241

CAS#: 313367-92-9

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.


Price and Availability

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UA62784 is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406241
Name: UA62784
CAS#: 313367-92-9
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


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


Technical Data

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).

Harmonized System Code:
293490


Additional Information

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.).


References

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.