WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206583
Description: Verdinexor, also known as KPT-335, is an orally bioavailable Selective Inhibitor of Nuclear Export (SINE). KPT-335 inhibited proliferation, blocked colony formation, and induced apoptosis of treated cells at biologically relevant concentrations of drug. Additionally, KPT-335 downregulated XPO1 protein while inducing a concomitant increase in XPO1 messenger RNA. KPT-335 treatment of cell lines upregulated the expression of both protein and mRNA for the tumor suppressor proteins p53 and p21, and promoted their nuclear localization.
MedKoo Cat#: 206583
Chemical Formula: C18H12F6N6O
Exact Mass: 442.0977
Molecular Weight: 442.3254
Elemental Analysis: C, 48.88; H, 2.73; F, 25.77; N, 19.00; O, 3.62
Synonym: KPT-335; KPT 335; KPT335; Verdinexor
IUPAC/Chemical Name: (Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyridin-2-yl)acrylohydrazide
InChi Key: OPAKEJZFFCECPN-XQRVVYSFSA-N
InChi Code: InChI=1S/C18H12F6N6O/c19-17(20,21)12-7-11(8-13(9-12)18(22,23)24)16-26-10-30(29-16)6-4-15(31)28-27-14-3-1-2-5-25-14/h1-10H,(H,25,27)(H,28,31)/b6-4-
SMILES Code: O=C(NNC1=NC=CC=C1)/C=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, not in water
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
The following data is based on the product molecular weight 442.3254 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: Gravina GL, Senapedis W, McCauley D, Baloglu E, Shacham S, Festuccia C. Nucleo-cytoplasmic transport as a therapeutic target of cancer. J Hematol Oncol. 2014 Dec 5;7:85. doi: 10.1186/s13045-014-0085-1. Review. PubMed PMID: 25476752; PubMed Central PMCID: PMC4272779.
2: Tan M, Wettersten HI, Chu K, Huso DL, Watnick T, Friedlander S, Landesman Y, Weiss RH. Novel inhibitors of nuclear transport cause cell cycle arrest and decrease cyst growth in ADPKD associated with decreased CDK4 levels. Am J Physiol Renal Physiol. 2014 Dec 1;307(11):F1179-86. doi: 10.1152/ajprenal.00406.2014. Epub 2014 Sep 18. PubMed PMID: 25234309; PubMed Central PMCID: PMC4254973.
3: Breit MN, Kisseberth WC, Bear MD, Landesman Y, Kashyap T, McCauley D, Kauffman MG, Shacham S, London CA. Biologic activity of the novel orally bioavailable selective inhibitor of nuclear export (SINE) KPT-335 against canine melanoma cell lines. BMC Vet Res. 2014 Jul 15;10:160. doi: 10.1186/1746-6148-10-160. PubMed PMID: 25022346; PubMed Central PMCID: PMC4105800.
4: Perwitasari O, Johnson S, Yan X, Howerth E, Shacham S, Landesman Y, Baloglu E, McCauley D, Tamir S, Tompkins SM, Tripp RA. Verdinexor, a novel selective inhibitor of nuclear export, reduces influenza a virus replication in vitro and in vivo. J Virol. 2014 Sep 1;88(17):10228-43. doi: 10.1128/JVI.01774-14. Epub 2014 Jun 25. PubMed PMID: 24965445; PubMed Central PMCID: PMC4136318.
5: London CA, Bernabe LF, Barnard S, Kisseberth WC, Borgatti A, Henson M, Wilson H, Jensen K, Ito D, Modiano JF, Bear MD, Pennell ML, Saint-Martin JR, McCauley D, Kauffman M, Shacham S. Preclinical evaluation of the novel, orally bioavailable Selective Inhibitor of Nuclear Export (SINE) KPT-335 in spontaneous canine cancer: results of a phase I study. PLoS One. 2014 Feb 4;9(2):e87585. doi: 10.1371/journal.pone.0087585. eCollection 2014. PubMed PMID: 24503695; PubMed Central PMCID: PMC3913620.