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

10mg
USD 150
100mg
USD 750
1g
USD 3050
Size
Price

25mg
USD 250
200mg
USD 1250
2g
USD 5650
Size
Price

50mg
USD 450
500mg
USD 1950
5g
USD 7650

Tinostamustine free base, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week 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)

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).

Harmonized System Code:
2934990300


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.