KPT-251 | CAS#1388841-50-6 | SINE

MedKoo Cat#: 562707 | Name: KPT-251

Description:

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

KPT-251 is a selective inhibitor of nuclear export (SINE).

Chemical Structure

KPT-251

CAS#1388841-50-6

Theoretical Analysis

MedKoo Cat#: 562707

Name: KPT-251

CAS#: 1388841-50-6

Chemical Formula: C14H7F6N5O

Exact Mass: 375.0555

Molecular Weight: 375.23

Elemental Analysis: C, 44.81; H, 1.88; F, 30.38; N, 18.66; O, 4.26

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 450.00	2 Weeks
10mg	USD 950.00	2 Weeks

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Related CAS #

No Data

Synonym

KPT-251; KPT 251; KPT251;

IUPAC/Chemical Name

(Z)-2-{2-[3-(3,5-Bis-trifluoromethyl-phenyl)-[1,2,4]triazol-1-yl]-vinyl}-[1,3,4]oxadiazole

InChi Key

LDFXTRYMMZGKIC-UPHRSURJSA-N

InChi Code

InChI=1S/C14H7F6N5O/c15-13(16,17)9-3-8(4-10(5-9)14(18,19)20)12-21-6-25(24-12)2-1-11-23-22-7-26-11/h1-7H/b2-1-

SMILES Code

FC(C1=CC(C(F)(F)F)=CC(C2=NN(/C=C\C3=NN=CO3)C=N2)=C1)(F)F

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 375.23 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, Mancini A, Colapietro A, Marampon F, Sferra R, Pompili S, Biordi LA, Iorio R, Flati V, Argueta C, Landesman Y, Kauffman M, Shacham S, Festuccia C. Pharmacological treatment with inhibitors of nuclear export enhances the antitumor activity of docetaxel in human prostate cancer. Oncotarget. 2017 Nov 30;8(67):111225-111245. doi: 10.18632/oncotarget.22760. eCollection 2017 Dec 19. PubMed PMID: 29340049; PubMed Central PMCID: PMC5762317. 2: Muqbil I, Aboukameel A, Elloul S, Carlson R, Senapedis W, Baloglu E, Kauffman M, Shacham S, Bhutani D, Zonder J, Azmi AS, Mohammad RM. Anti-tumor activity of selective inhibitor of nuclear export (SINE) compounds, is enhanced in non-Hodgkin lymphoma through combination with mTOR inhibitor and dexamethasone. Cancer Lett. 2016 Dec 28;383(2):309-317. doi: 10.1016/j.canlet.2016.09.016. Epub 2016 Sep 28. PubMed PMID: 27693556; PubMed Central PMCID: PMC5584550. 3: Gravina GL, Mancini A, Sanita P, Vitale F, Marampon F, Ventura L, Landesman Y, McCauley D, Kauffman M, Shacham S, Festuccia C. KPT-330, a potent and selective exportin-1 (XPO-1) inhibitor, shows antitumor effects modulating the expression of cyclin D1 and survivin [corrected] in prostate cancer models. BMC Cancer. 2015 Dec 1;15:941. doi: 10.1186/s12885-015-1936-z. Erratum in: BMC Cancer. 2016;16:8. PubMed PMID: 26620414; PubMed Central PMCID: PMC4666032. 4: De Cesare M, Cominetti D, Doldi V, Lopergolo A, Deraco M, Gandellini P, Friedlander S, Landesman Y, Kauffman MG, Shacham S, Pennati M, Zaffaroni N. Anti-tumor activity of selective inhibitors of XPO1/CRM1-mediated nuclear export in diffuse malignant peritoneal mesothelioma: the role of survivin. Oncotarget. 2015 May 30;6(15):13119-32. PubMed PMID: 25948791; PubMed Central PMCID: PMC4537003. 5: Green AL, Ramkissoon SH, McCauley D, Jones K, Perry JA, Hsu JH, Ramkissoon LA, Maire CL, Hubbell-Engler B, Knoff DS, Shacham S, Ligon KL, Kung AL. Preclinical antitumor efficacy of selective exportin 1 inhibitors in glioblastoma. Neuro Oncol. 2015 May;17(5):697-707. doi: 10.1093/neuonc/nou303. Epub 2014 Nov 2. PubMed PMID: 25366336; PubMed Central PMCID: PMC4482855. 6: Gravina GL, Tortoreto M, Mancini A, Addis A, Di Cesare E, Lenzi A, Landesman Y, McCauley D, Kauffman M, Shacham S, Zaffaroni N, Festuccia C. XPO1/CRM1-selective inhibitors of nuclear export (SINE) reduce tumor spreading and improve overall survival in preclinical models of prostate cancer (PCa). J Hematol Oncol. 2014 Oct 5;7:46. doi: 10.1186/1756-8722-7-46. PubMed PMID: 25284315; PubMed Central PMCID: PMC4283114. 7: Mendonca J, Sharma A, Kim HS, Hammers H, Meeker A, De Marzo A, Carducci M, Kauffman M, Shacham S, Kachhap S. Selective inhibitors of nuclear export (SINE) as novel therapeutics for prostate cancer. Oncotarget. 2014 Aug 15;5(15):6102-12. PubMed PMID: 25026284; PubMed Central PMCID: PMC4171616. 8: Gao J, Azmi AS, Aboukameel A, Kauffman M, Shacham S, Abou-Samra AB, Mohammad RM. Nuclear retention of Fbw7 by specific inhibitors of nuclear export leads to Notch1 degradation in pancreatic cancer. Oncotarget. 2014 Jun 15;5(11):3444-54. PubMed PMID: 24899509; PubMed Central PMCID: PMC4116494. 9: Cheng Y, Holloway MP, Nguyen K, McCauley D, Landesman Y, Kauffman MG, Shacham S, Altura RA. XPO1 (CRM1) inhibition represses STAT3 activation to drive a survivin-dependent oncogenic switch in triple-negative breast cancer. Mol Cancer Ther. 2014 Mar;13(3):675-86. doi: 10.1158/1535-7163.MCT-13-0416. Epub 2014 Jan 15. PubMed PMID: 24431073; PubMed Central PMCID: PMC3954411. 10: Salas Fragomeni RA, Chung HW, Landesman Y, Senapedis W, Saint-Martin JR, Tsao H, Flaherty KT, Shacham S, Kauffman M, Cusack JC. CRM1 and BRAF inhibition synergize and induce tumor regression in BRAF-mutant melanoma. Mol Cancer Ther. 2013 Jul;12(7):1171-9. doi: 10.1158/1535-7163.MCT-12-1171. Epub 2013 Apr 24. PubMed PMID: 23615632. 11: Inoue H, Kauffman M, Shacham S, Landesman Y, Yang J, Evans CP, Weiss RH. CRM1 blockade by selective inhibitors of nuclear export attenuates kidney cancer growth. J Urol. 2013 Jun;189(6):2317-26. doi: 10.1016/j.juro.2012.10.018. Epub 2012 Oct 16. PubMed PMID: 23079374; PubMed Central PMCID: PMC4593314. 12: Etchin J, Sun Q, Kentsis A, Farmer A, Zhang ZC, Sanda T, Mansour MR, Barcelo C, McCauley D, Kauffman M, Shacham S, Christie AL, Kung AL, Rodig SJ, Chook YM, Look AT. Antileukemic activity of nuclear export inhibitors that spare normal hematopoietic cells. Leukemia. 2013 Jan;27(1):66-74. doi: 10.1038/leu.2012.219. Epub 2012 Jul 31. PubMed PMID: 22847027; PubMed Central PMCID: PMC3542631.