MedKoo Cat#: 206782 | Name: Eltanexor
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Description:

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

Eltanexor, also known as KPT-8602, is a second-generation exportin-1 inhibitor. KPT-8602 demonstrates potent activity against acute lymphoblastic leukemia. KPT-8602 is well tolerated and highly active against AML blasts and leukemia-initiating cells. Eltanexor shows improved efficacy and in vivo tolerability in hematological malignancies.

Chemical Structure

Eltanexor
Eltanexor
CAS#1642300-52-4

Theoretical Analysis

MedKoo Cat#: 206782

Name: Eltanexor

CAS#: 1642300-52-4

Chemical Formula: C17H10F6N6O

Exact Mass: 428.0820

Molecular Weight: 428.30

Elemental Analysis: C, 47.67; H, 2.35; F, 26.61; N, 19.62; O, 3.74

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 Weeks
25mg USD 650.00 2 Weeks
50mg USD 950.00 2 Weeks
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Related CAS #
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Synonym
KPT-8602; KPT8602; KPT 8602; Eltanexor; Eltanexorum; NSC794443; NSC 794443; NSC-794443
IUPAC/Chemical Name
(2E)-3-{3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl}-2-(pyrimidin-5-yl)prop-2-enamide
InChi Key
JFBAVWVBLRIWHM-AWNIVKPZSA-N
InChi Code
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+
SMILES Code
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
Appearance
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
Shelf Life
>2 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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 428.30 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.

Recalculate based on batch purity %
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: 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.