Tinostamustine free base
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MedKoo CAT#: 407990

CAS#: 1236199-60-2 (free base)

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

Size Price Shipping out time Quantity
10mg USD 150 Same day
25mg USD 250 Same day
50mg USD 450 Same day
100mg USD 750 Same day
200mg USD 1250 Same day
500mg USD 1950 Same day
1g USD 2950 Same day
2g USD 5450 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-06-06. Prices are subject to change without notice.

Tinostamustine free base, purity > 98%, is in stock. The same day shipping after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 407990
Name: Tinostamustine free base
CAS#: 1236199-60-2 (free base)
Chemical Formula: C19H28Cl2N4O2
Exact Mass: 414.1589
Molecular Weight: 415.359
Elemental Analysis: C, 54.94; H, 6.80; Cl, 17.07; N, 13.49; O, 7.70


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

Synonym: Tinostamustine free base; EDO-S101; EDO-S 101; EDO-S-101;

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

InChi Key: GISXTRIGVCKQBX-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H28Cl2N4O2/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)

SMILES Code: O=C(NO)CCCCCCC1=NC2=CC(N(CCCl)CCCl)=CC=C2N1C


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

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:
>3 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


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.