Eltanexor

• CAT Number: I026800
• CAS Number: 1642300-52-4
• Molecular Formula: C17H10F6N6O
• Molecular Weight: 428.2984
• Purity: 98%
• Synonyms: KPT-8602; KPT8602; KPT 8602. Eltanexor.
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Storage: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
• IUPAC Name: (2E)-3-{3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl}-2-(pyrimidin-5-yl)prop-2-enamide
• InChI: InChI=1S/C17H10F6N6O/c18-16(19,20)11-1-9(2-12(3-11)17(21,22)23)15-27-8-29(28-15)6-13(14(24)30)10-4-25-7-26-5-10/h1-8H,(H2,24,30)/b13-6+
• InChIKey: JFBAVWVBLRIWHM-AWNIVKPZSA-N
• SMILES: O=C(N)/C(C1=CN=CN=C1)=C/N2N=C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)N=C2

Eltanexor(CAT: I026800) referred to as KPT-8602, represents a significant advancement in the field of targeted therapies for hematological malignancies. As a second-generation exportin-1 inhibitor, Eltanexor disrupts the nuclear export of various proteins, influencing critical cellular processes. This compound has demonstrated potent activity against acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML), targeting not only leukemia blasts but also leukemia-initiating cells.

Reference

1: Vercruysse T, De Bie J, Neggers J, Jacquemyn M, Vanstreels E, Schmid-Burgk JL, Hornung V, Baloglu E, Landesman Y, Senapedis W, Shacham S, Dagklis A, Cools J, Daelemans D. The second-generation exportin-1 inhibitor KPT-8602 demonstrates potent activity against acute lymphoblastic leukemia. Clin Cancer Res. 2016 Oct 25. pii: clincanres.1580.2016. [Epub ahead of print] PubMed PMID: 27780859.
2: Etchin J, Berezovskaya A, Conway AS, Galinsky IA, Stone RM, Baloglu E, Senapedis W, Landesman Y, Kauffman M, Shacham S, Wang JC, Look AT. KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells. Leukemia. 2017 Jan;31(1):143-150. doi: 10.1038/leu.2016.145. PubMed PMID: 27211268.
3: Hing ZA, Fung HY, Ranganathan P, Mitchell S, El-Gamal D, Woyach JA, Williams K, Goettl VM, Smith J, Yu X, Meng X, Sun Q, Cagatay T, Lehman AM, Lucas DM, Baloglu E, Shacham S, Kauffman MG, Byrd JC, Chook YM, Garzon R, Lapalombella R. Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies. Leukemia. 2016 Dec;30(12):2364-2372. doi: 10.1038/leu.2016.136. PubMed PMID: 27323910; PubMed Central PMCID: PMC5143172.
4: Taylor-Kashton C, Lichtensztejn D, Baloglu E, Senapedis W, Shacham S, Kauffman MG, Kotb R, Mai S. XPO1 Inhibition Preferentially Disrupts the 3D Nuclear Organization of Telomeres in Tumor Cells. J Cell Physiol. 2016 Dec;231(12):2711-9. doi: 10.1002/jcp.25378. PubMed PMID: 26991404; PubMed Central PMCID: PMC5111786.