Deferitazole

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

MedKoo CAT#: 319691

CAS#: 945635-15-4 (free acid)

Description: Deferitazole, also known as FBS-0701 and SPD-602, is a new orally active Antimalarial iron chelator for the treatment of transfusional iron overload. Deferitazole displays a high affinity and selectivity for iron(III) as demonstrated by the log β2 = 33.39 ± 0.03 and the pFe(3+) value of 22.3. Deferitazole scavenges iron from labile sources such as citrate and albumin with efficiencies comparable with those of other therapeutic iron chelators, including deferasirox, deferiprone and desferrioxamine. FBS0701 blocks transmission by Plasmodium falciparum gametocyte.

Chemical Structure

Deferitazole

CAS# 945635-15-4 (free acid)

Instruction

Theoretical Analysis

MedKoo Cat#: 319691
Name: Deferitazole
CAS#: 945635-15-4 (free acid)
Chemical Formula: C18H25NO7S
Exact Mass: 399.14
Molecular Weight: 399.458
Elemental Analysis: C, 54.12; H, 6.31; N, 3.51; O, 28.04; S, 8.03

Price and Availability

Size	Price	Availability	Quantity
10mg	USD -2
25mg	USD -2
50mg	USD -2
100mg	USD -2
200mg	USD -2
500mg	USD -2
1g	USD -1
2g	USD -1
5g	USD -1
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: FBS-0701; FBS0701; FBS 0701; SPD-602; SPD 602; SPD602; Deferitazole

IUPAC/Chemical Name: (S)-2-(2-hydroxy-3-(2-(2-(2-methoxyethoxy)ethoxy)ethoxy)phenyl)-4-methyl-4,5-dihydrothiazole-4-carboxylic acid

InChi Key: AWHIMFSHNAAMBM-GOSISDBHSA-N

InChi Code: InChI=1S/C18H25NO7S/c1-18(17(21)22)12-27-16(19-18)13-4-3-5-14(15(13)20)26-11-10-25-9-8-24-7-6-23-2/h3-5,20H,6-12H2,1-2H3,(H,21,22)/t18-/m1/s1

SMILES Code: O=C([C@]1(C)N=C(C2=CC=CC(OCCOCCOCCOC)=C2O)SC1)O

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

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 399.46 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

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Hider RC, Kong X, Abbate V, Harland R, Conlon K, Luker T. Deferitazole, a new orally active iron chelator. Dalton Trans. 2015 Mar 21;44(11):5197-204. doi: 10.1039/c5dt00063g. PubMed PMID: 25687725.

2: Ferrer P, Vega-Rodriguez J, Tripathi AK, Jacobs-Lorena M, Sullivan DJ Jr. Antimalarial iron chelator FBS0701 blocks transmission by Plasmodium falciparum gametocyte activation inhibition. Antimicrob Agents Chemother. 2015 Mar;59(3):1418-26. doi: 10.1128/AAC.04642-14. Epub 2014 Dec 15. PubMed PMID: 25512427; PubMed Central PMCID: PMC4325789.

3: Gumienna-Kontecka E, Pyrkosz-Bulska M, Szebesczyk A, Ostrowska M. Iron chelating strategies in systemic metal overload, neurodegeneration and cancer. Curr Med Chem. 2014;21(33):3741-67. Review. PubMed PMID: 25005181.

4: Ferrer P, Tripathi AK, Clark MA, Hand CC, Rienhoff HY Jr, Sullivan DJ Jr. Antimalarial iron chelator, FBS0701, shows asexual and gametocyte Plasmodium falciparum activity and single oral dose cure in a murine malaria model. PLoS One. 2012;7(5):e37171. doi: 10.1371/journal.pone.0037171. Epub 2012 May 21. PubMed PMID: 22629364; PubMed Central PMCID: PMC3357340.

5: Ma Y, Zhou T, Kong X, Hider RC. Chelating agents for the treatment of systemic iron overload. Curr Med Chem. 2012;19(17):2816-27. Review. PubMed PMID: 22455586.

6: Neufeld EJ, Galanello R, Viprakasit V, Aydinok Y, Piga A, Harmatz P, Forni GL, Shah FT, Grace RF, Porter JB, Wood JC, Peppe J, Jones A, Rienhoff HY Jr. A phase 2 study of the safety, tolerability, and pharmacodynamics of FBS0701, a novel oral iron chelator, in transfusional iron overload. Blood. 2012 Apr 5;119(14):3263-8. doi: 10.1182/blood-2011-10-386268. Epub 2012 Jan 17. PubMed PMID: 22251482; PubMed Central PMCID: PMC3321852.

7: Rienhoff HY Jr, Viprakasit V, Tay L, Harmatz P, Vichinsky E, Chirnomas D, Kwiatkowski JL, Tapper A, Kramer W, Porter JB, Neufeld EJ. A phase 1 dose-escalation study: safety, tolerability, and pharmacokinetics of FBS0701, a novel oral iron chelator for the treatment of transfusional iron overload. Haematologica. 2011 Apr;96(4):521-5. doi: 10.3324/haematol.2010.034405. Epub 2010 Dec 20. PubMed PMID: 21173101; PubMed Central PMCID: PMC3069228.

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