Selinexor trans-isomer

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MedKoo CAT#: 540260

CAS#: 1421923-86-5 (E-isomer)

Description: Selinexor trans-isomer is a trans-isomer of Selinexor or KPT-330, which is a CRM1-selective inhibitor of nuclear export. It inhibits protein trafficking from the nucleus and induces cell cycle arrest and apoptosis in mesothelioma cells.

Chemical Structure

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Selinexor trans-isomer
CAS# 1421923-86-5 (E-isomer)
Instruction

Theoretical Analysis

MedKoo Cat#: 540260
Name: Selinexor trans-isomer
CAS#: 1421923-86-5 (E-isomer)
Chemical Formula: C17H11F6N7O
Exact Mass: 443.09
Molecular Weight: 443.310
Elemental Analysis: C, 46.06; H, 2.50; F, 25.71; N, 22.12; O, 3.61

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 1393477-72-9 (free base)   1421923-86-5 (E-isomer)   1621865-82-4 (E-isomer)   Unknown (HCl)    

Synonym: KPT-330 E-isomer; KPT330 trans isomer; E-KPT 330; Selinexor E-isomer; Selinexor trans-isomer

IUPAC/Chemical Name: O=C(NNC1=NC=CN=C1)/C=C/N2N=C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)N=C2

InChi Key: DEVSOMFAQLZNKR-DAFODLJHSA-N

InChi Code: InChI=1S/C17H11F6N7O/c18-16(19,20)11-5-10(6-12(7-11)17(21,22)23)15-26-9-30(29-15)4-1-14(31)28-27-13-8-24-2-3-25-13/h1-9H,(H,25,27)(H,28,31)/b4-1+

SMILES Code: O=C(NNC1=NC=CN=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

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 443.31 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Ben-Barouch S, Kuruvilla J. Selinexor (KTP-330) - a selective inhibitor of nuclear export (SINE): anti-tumor activity in diffuse large B-cell lymphoma (DLBCL). Expert Opin Investig Drugs. 2019 Dec 17. doi: 10.1080/13543784.2020.1706087. [Epub ahead of print] PubMed PMID: 31847605.

2: Azmi AS, Khan HY, Muqbil I, Aboukameel A, Neggers JE, Daelemans D, Mahipal A, Dyson G, Kamgar M, Al Hallak MN, Tesfaye A, Kim S, Shidham V, Ramzi M, Philip PA. Preclinical assessment with clinical validation of Selinexor with gemcitabine and nab-paclitaxel for the treatment of pancreatic ductal adenocarcinoma. Clin Cancer Res. 2019 Dec 12. pii: clincanres.1728.2019. doi: 10.1158/1078-0432.CCR-19-1728. [Epub ahead of print] PubMed PMID: 31831564.

3: Vergote IB, Lund B, Peen U, Umajuridze Z, Mau-Sorensen M, Kranich A, Van Nieuwenhuysen E, Haslund C, Nottrup T, Han SN, Concin N, Unger TJ, Chai Y, Au N, Rashal T, Joshi A, Crochiere M, Landesman Y, Shah J, Shacham S, Kauffman M, Mirza MR. Phase 2 study of the Exportin 1 inhibitor selinexor in patients with recurrent gynecological malignancies. Gynecol Oncol. 2019 Dec 7. pii: S0090-8258(19)31663-4. doi: 10.1016/j.ygyno.2019.11.012. [Epub ahead of print] PubMed PMID: 31822399.

4: Peterson TJ, Orozco J, Buege M. Selinexor: A First-in-Class Nuclear Export Inhibitor for Management of Multiply Relapsed Multiple Myeloma. Ann Pharmacother. 2019 Dec 2:1060028019892643. doi: 10.1177/1060028019892643. [Epub ahead of print] PubMed PMID: 31793336.

5: Abboud R, Chendamarai E, Rettig MP, Trinkaus KM, Riedell PA, Abboud CN, Ghobadi A, Pusic I, Stockerl-Goldstein K, Schroeder MA, Vij R, Westervelt P, DiPersio JF, Uy GL. Selinexor combined with cladribine, cytarabine, and filgrastim in relapsed or refractory acute myeloid leukemia. Haematologica. 2019 Nov 21. pii: haematol.2019.236810. doi: 10.3324/haematol.2019.236810. [Epub ahead of print] PubMed PMID: 31753931.

6: Chari A, Vogl DT, Jagannath S. Selinexor for Refractory Multiple Myeloma. Reply. N Engl J Med. 2019 Nov 14;381(20):1977-1978. doi: 10.1056/NEJMc1912625. PubMed PMID: 31722163.

7: Jhaveri KD, Wanchoo R. Selinexor for Refractory Multiple Myeloma. N Engl J Med. 2019 Nov 14;381(20):1977. doi: 10.1056/NEJMc1912625. PubMed PMID: 31722162.

8: Sweet K, Komrokji R, Padron E, Cubitt CL, Turner JG, Zhou J, List AF, Sallman DA, Dawson JL, Sullivan DM, Chavez J, Shah BD, Lancet JE. Phase I Clinical Trial of Selinexor in Combination with Daunorubicin and Cytarabine in Previously Untreated Poor-Risk Acute Myeloid Leukemia. Clin Cancer Res. 2019 Oct 21. doi: 10.1158/1078-0432.CCR-19-2169. [Epub ahead of print] PubMed PMID: 31636097.

9: Depping R, von Fallois M, Landesman Y, Kosyna FK. The Nuclear Export Inhibitor Selinexor Inhibits Hypoxia Signaling Pathways And 3D Spheroid Growth Of Cancer Cells. Onco Targets Ther. 2019 Oct 11;12:8387-8399. doi: 10.2147/OTT.S213208. eCollection 2019. PubMed PMID: 31632086; PubMed Central PMCID: PMC6793465.

10: Bhatnagar B, Zhao Q, Mims AS, Vasu S, Behbehani GK, Larkin K, Blachly JS, Blum W, Klisovic RB, Ruppert AS, Orwick S, Oakes C, Ranganathan P, Byrd JC, Walker AR, Garzon R. Selinexor in combination with decitabine in patients with acute myeloid leukemia: results from a phase 1 study. Leuk Lymphoma. 2019 Sep 23:1-10. doi: 10.1080/10428194.2019.1665664. [Epub ahead of print] PubMed PMID: 31545113.

11: Romero D. Responses to selinexor in multiple myeloma. Nat Rev Clin Oncol. 2019 Nov;16(11):661. doi: 10.1038/s41571-019-0275-4. PubMed PMID: 31485030.

12: Stirrups R. Selinexor-dexamethasone for refractory multiple myeloma. Lancet Oncol. 2019 Oct;20(10):e560. doi: 10.1016/S1470-2045(19)30566-2. Epub 2019 Aug 30. PubMed PMID: 31477451.

13: Chari A, Vogl DT, Gavriatopoulou M, Nooka AK, Yee AJ, Huff CA, Moreau P, Dingli D, Cole C, Lonial S, Dimopoulos M, Stewart AK, Richter J, Vij R, Tuchman S, Raab MS, Weisel KC, Delforge M, Cornell RF, Kaminetzky D, Hoffman JE, Costa LJ, Parker TL, Levy M, Schreder M, Meuleman N, Frenzel L, Mohty M, Choquet S, Schiller G, Comenzo RL, Engelhardt M, Illmer T, Vlummens P, Doyen C, Facon T, Karlin L, Perrot A, Podar K, Kauffman MG, Shacham S, Li L, Tang S, Picklesimer C, Saint-Martin JR, Crochiere M, Chang H, Parekh S, Landesman Y, Shah J, Richardson PG, Jagannath S. Oral Selinexor-Dexamethasone for Triple-Class Refractory Multiple Myeloma. N Engl J Med. 2019 Aug 22;381(8):727-738. doi: 10.1056/NEJMoa1903455. PubMed PMID: 31433920.

14: Syed YY. Selinexor: First Global Approval. Drugs. 2019 Sep;79(13):1485-1494. doi: 10.1007/s40265-019-01188-9. Review. PubMed PMID: 31429063.

15: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK544627/ PubMed PMID: 31369222.

16: Jakubowiak AJ, Jasielec JK, Rosenbaum CA, Cole CE, Chari A, Mikhael J, Nam J, McIver A, Severson E, Stephens LA, Tinari K, Rosebeck S, Zimmerman TM, Hycner T, Turowski A, Karrison T, Zonder JA. Phase 1 study of selinexor plus carfilzomib and dexamethasone for the treatment of relapsed/refractory multiple myeloma. Br J Haematol. 2019 Aug;186(4):549-560. doi: 10.1111/bjh.15969. Epub 2019 May 24. PubMed PMID: 31124580; PubMed Central PMCID: PMC6772147.

17: Shafique M, Ismail-Khan R, Extermann M, Sullivan D, Goodridge D, Boulware D, Hogue D, Soliman H, Khong H, Han HS. A Phase II Trial of Selinexor (KPT-330) for Metastatic Triple-Negative Breast Cancer. Oncologist. 2019 Jul;24(7):887-e416. doi: 10.1634/theoncologist.2019-0231. Epub 2019 Apr 17. PubMed PMID: 30996012; PubMed Central PMCID: PMC6656474.

18: Ming M, Wu W, Xie B, Sukhanova M, Wang W, Kadri S, Sharma S, Lee J, Shacham S, Landesman Y, Maltsev N, Lu P, Wang YL. XPO1 Inhibitor Selinexor Overcomes Intrinsic Ibrutinib Resistance in Mantle Cell Lymphoma via Nuclear Retention of IκB. Mol Cancer Ther. 2018 Dec;17(12):2564-2574. doi: 10.1158/1535-7163.MCT-17-0789-ATR. PubMed PMID: 30510142.

19: Bahlis NJ, Sutherland H, White D, Sebag M, Lentzsch S, Kotb R, Venner CP, Gasparetto C, Del Col A, Neri P, Reece D, Kauffman M, Shacham S, Unger TJ, Jeha J, Saint-Martin JR, Shah J, Chen C. Selinexor plus low-dose bortezomib and dexamethasone for patients with relapsed or refractory multiple myeloma. Blood. 2018 Dec 13;132(24):2546-2554. doi: 10.1182/blood-2018-06-858852. Epub 2018 Oct 23. PubMed PMID: 30352784; PubMed Central PMCID: PMC6302280.

20: Baek HB, Lombard AP, Libertini SJ, Fernandez-Rubio A, Vinall R, Gandour-Edwards R, Nakagawa R, Vidallo K, Nishida K, Siddiqui S, Wettersten H, Landesman Y, Weiss RH, Ghosh PM, Mudryj M. XPO1 inhibition by selinexor induces potent cytotoxicity against high grade bladder malignancies. Oncotarget. 2018 Oct 2;9(77):34567-34581. doi: 10.18632/oncotarget.26179. eCollection 2018 Oct 2. PubMed PMID: 30349650; PubMed Central PMCID: PMC6195388.