Tinostamustine HCl

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MedKoo CAT#: 206504

CAS#: 1793059-58-1 (HCl)

Description: Tinostamustine, also known as EDO-S101, is an alkylatlng histone-deacetylase inhibitor (HDACi) fusion molecule. EDO-S101 is a functional pan-histone-deacetylase inhibitor and is assumed to potentiate the alkylating activity of the compound and/or may help to overcome resistance to other therapeutic agents.


Price and Availability

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Pricing updated 2020-07-07. Prices are subject to change without notice.

Tinostamustine hydrochloride is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 206504
Name: Tinostamustine HCl
CAS#: 1793059-58-1 (HCl)
Chemical Formula: C19H29Cl3N4O2
Exact Mass:
Molecular Weight: 451.82
Elemental Analysis: C, 50.51; H, 6.47; Cl, 23.54; N, 12.40; O, 7.08


Related CAS #: 1793059-58-1 (HCl)   1236199-60-2 (free base)    

Synonym: EDO-S101; EDO-S 101; EDO-S-101; EDO-S101 HCl; EDO-S101 hydrochloride; Tinostamustine hydrochloride

IUPAC/Chemical Name: 7-(5-(bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)-N-hydroxyheptanamide hydrochloride

InChi Key: DWGQFQRWFYIINU-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H28Cl2N4O2.ClH/c1-24-17-9-8-15(25(12-10-20)13-11-21)14-16(17)22-18(24)6-4-2-3-5-7-19(26)23-27;/h8-9,14,27H,2-7,10-13H2,1H3,(H,23,26);1H

SMILES Code: O=C(NO)CCCCCCC1=NC2=CC(N(CCCl)CCCl)=CC=C2N1C.[H]Cl


Technical Data

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


Additional Information

Related CAS#
1793059-58-1 (HCl salt);
1236199-60-2 (free base)


References

1: M'kacher R, Frenzel M, Al Jawhari M, Junker S, Cuceu C, Morat L, Bauchet AL, Stimmer L, Lenain A, Dechamps N, Hempel WM, Pottier G, Heidingsfelder L, Laplagne E, Borie C, Oudrhiri N, Jouni D, Bennaceur-Griscelli A, Colicchio B, Dieterlen A, Girinsky T, Boisgard R, Bourhis J, Bosq J, Mehrling T, Jeandidier E, Carde P. Establishment and Characterization of a Reliable Xenograft Model of Hodgkin Lymphoma Suitable for the Study of Tumor Origin and the Design of New Therapies. Cancers (Basel). 2018 Oct 31;10(11). pii: E414. doi: 10.3390/cancers10110414. PubMed PMID: 30384446; PubMed Central PMCID: PMC6265845.

2: Dooley D, van Timmeren MM, O'Reilly VP, Brady G, O'Brien EC, Fazekas B, Hickey FB, Leacy E, Pusey CD, Tam FWK, Mehrling T, Heeringa P, Little MA. Alkylating histone deacetylase inhibitors may have therapeutic value in experimental myeloperoxidase-ANCA vasculitis. Kidney Int. 2018 Nov;94(5):926-936. doi: 10.1016/j.kint.2018.05.028. Epub 2018 Aug 26. PubMed PMID: 30158055.

3: Qiu Y, Li Z, Copland JA, Mehrling T, Tun HW. Combined alkylation and histone deacetylase inhibition with EDO-S101 has significant therapeutic activity against brain tumors in preclinical models. Oncotarget. 2018 Jun 15;9(46):28155-28164. doi: 10.18632/oncotarget.25588. eCollection 2018 Jun 15. PubMed PMID: 29963268; PubMed Central PMCID: PMC6021334.

4: Festuccia C, Mancini A, Colapietro A, Gravina GL, Vitale F, Marampon F, Delle Monache S, Pompili S, Cristiano L, Vetuschi A, Tombolini V, Chen Y, Mehrling T. The first-in-class alkylating deacetylase inhibitor molecule tinostamustine shows antitumor effects and is synergistic with radiotherapy in preclinical models of glioblastoma. J Hematol Oncol. 2018 Feb 27;11(1):32. doi: 10.1186/s13045-018-0576-6. Erratum in: J Hematol Oncol. 2018 Mar 14;11(1):38. PubMed PMID: 29486795; PubMed Central PMCID: PMC5830080.

5: Besse L, Kraus M, Besse A, Bader J, Silzle T, Mehrling T, Driessen C. The first-in-class alkylating HDAC inhibitor EDO-S101 is highly synergistic with proteasome inhibition against multiple myeloma through activation of multiple pathways. Blood Cancer J. 2017 Jul 28;7(7):e589. doi: 10.1038/bcj.2017.69. PubMed PMID: 28753594; PubMed Central PMCID: PMC5549260.

6: López-Iglesias AA, Herrero AB, Chesi M, San-Segundo L, González-Méndez L, Hernández-García S, Misiewicz-Krzeminska I, Quwaider D, Martín-Sánchez M, Primo D, Paíno T, Bergsagel PL, Mehrling T, González-Díaz M, San-Miguel JF, Mateos MV, Gutiérrez NC, Garayoa M, Ocio EM. Preclinical anti-myeloma activity of EDO-S101, a new bendamustine-derived molecule with added HDACi activity, through potent DNA damage induction and impairment of DNA repair. J Hematol Oncol. 2017 Jun 20;10(1):127. doi: 10.1186/s13045-017-0495-y. PubMed PMID: 28633670; PubMed Central PMCID: PMC5477689.

7: Mehrling T, Chen Y. The Alkylating-HDAC Inhibition Fusion Principle: Taking Chemotherapy to the Next Level with the First in Class Molecule EDO-S101. Anticancer Agents Med Chem. 2016;16(1):20-8. PubMed PMID: 25980817.