AWZ1066S
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MedKoo CAT#: 555646

CAS#: 2239272-16-1

Description: AWZ1066S is a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis. AWZ1066S shows superior efficacy to existing anti-Wolbachia therapies in validated preclinical models of infection and has DMPK characteristics that are compatible with a short therapeutic regimen of 7 days or less. This candidate molecule is well-positioned for onward development and has the potential to make a significant impact on communities affected by filariasis.

Chemical Structure

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AWZ1066S
CAS# 2239272-16-1
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 555646
Name: AWZ1066S
CAS#: 2239272-16-1
Chemical Formula: C19H19F3N6O
Exact Mass: 404.16
Molecular Weight: 404.397
Elemental Analysis: C, 56.43; H, 4.74; F, 14.09; N, 20.78; O, 3.96

Price and Availability

Size Price Availability Quantity
100mg USD 1450 2 Weeks
200mg USD 1950 2 Weeks
500mg USD 3650 2 Weeks
1g USD 5250 2 Weeks
2g USD 7850 2 Weeks
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Related CAS #: 2239272-16-1  

Synonym: AWZ1066S; AWZ-1066S; AWZ 1066S; AWZ106S; AWZ-1066; AWZ 1066;

IUPAC/Chemical Name: (S)-2-(3-methylmorpholino)-N-((2-(trifluoromethyl)pyridin-3-yl)methyl)pyrido[2,3-d]pyrimidin-4-amine

InChi Key: IZFVCNUAPFSNCO-LBPRGKRZSA-N

InChi Code: InChI=1S/C19H19F3N6O/c1-12-11-29-9-8-28(12)18-26-16-14(5-3-7-24-16)17(27-18)25-10-13-4-2-6-23-15(13)19(20,21)22/h2-7,12H,8-11H2,1H3,(H,24,25,26,27)/t12-/m0/s1

SMILES Code: FC(C1=NC=CC=C1CNC2=C(C=CC=N3)C3=NC(N4[C@@H](C)COCC4)=N2)(F)F

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).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
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Biological target: AWZ1066S is an anti-Wolbachia drug candidate for a short-course treatment of filariasis, with an EC50 of 2.5 nM in cell assay.
In vitro activity: AWZ1066 (racemic mixture) was active against Wolbachia in a cell-based assay with an EC50 of 2.6 ± 0.5 nM (Fig. 1B). In an orthogonal secondary in vitro assay utilizing microfilariae (mf) of the human parasite B. malayi, AWZ1066 reduced Wolbachia within the mf with an EC50 of 150 nM while having no effect on the viability and motility of the mf at up to the top testing concentration of 5 µM. Reference: Proc Natl Acad Sci U S A. 2019 Jan 22; 116(4): 1414–1419. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6347715/
In vivo activity: After 7 d of twice-daily treatment of AWZ1066S at either 100 or 50 mg/kg orally, Wolbachia load was reduced by >99% compared with control untreated animals, 18 wk post treatment (Kruskal–Wallis statistic 43.5, P < 0.0001; Fig. 2B). After AWZ1066S treatment, the peripheral blood microfilaremia began to decline from 6 wk post treatment. A state of amicrofilaremia (absence of mf in the blood) was evident from 14 wk post treatment in the 7-d AWZ1066S treatment groups, a state that was sustained until the end of the experiment at 18 wk post treatment. Thus, treatment with AWZ1066S for 7 d leads to sterilization and gradual depletion of mf with the assumption, based on extensive clinical trial data with doxycycline, that this will result in a “slow” killing of adult worms alongside an improved safety profile. Reference: Proc Natl Acad Sci U S A. 2019 Jan 22; 116(4): 1414–1419. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6347715/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 125.0 309.10

Preparing Stock Solutions

The following data is based on the product molecular weight 404.40 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: 1. Hong WD, Benayoud F, Nixon GL, Ford L, Johnston KL, Clare RH, Cassidy A, Cook DAN, Siu A, Shiotani M, Webborn PJH, Kavanagh S, Aljayyoussi G, Murphy E, Steven A, Archer J, Struever D, Frohberger SJ, Ehrens A, Hübner MP, Hoerauf A, Roberts AP, Hubbard ATM, Tate EW, Serwa RA, Leung SC, Qie L, Berry NG, Gusovsky F, Hemingway J, Turner JD, Taylor MJ, Ward SA, O'Neill PM. AWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis. Proc Natl Acad Sci U S A. 2019 Jan 22;116(4):1414-1419. doi: 10.1073/pnas.1816585116. Epub 2019 Jan 7. PMID: 30617067; PMCID: PMC6347715.
In vitro protocol: 1. Hong WD, Benayoud F, Nixon GL, Ford L, Johnston KL, Clare RH, Cassidy A, Cook DAN, Siu A, Shiotani M, Webborn PJH, Kavanagh S, Aljayyoussi G, Murphy E, Steven A, Archer J, Struever D, Frohberger SJ, Ehrens A, Hübner MP, Hoerauf A, Roberts AP, Hubbard ATM, Tate EW, Serwa RA, Leung SC, Qie L, Berry NG, Gusovsky F, Hemingway J, Turner JD, Taylor MJ, Ward SA, O'Neill PM. AWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis. Proc Natl Acad Sci U S A. 2019 Jan 22;116(4):1414-1419. doi: 10.1073/pnas.1816585116. Epub 2019 Jan 7. PMID: 30617067; PMCID: PMC6347715.
In vivo protocol: 1. Hong WD, Benayoud F, Nixon GL, Ford L, Johnston KL, Clare RH, Cassidy A, Cook DAN, Siu A, Shiotani M, Webborn PJH, Kavanagh S, Aljayyoussi G, Murphy E, Steven A, Archer J, Struever D, Frohberger SJ, Ehrens A, Hübner MP, Hoerauf A, Roberts AP, Hubbard ATM, Tate EW, Serwa RA, Leung SC, Qie L, Berry NG, Gusovsky F, Hemingway J, Turner JD, Taylor MJ, Ward SA, O'Neill PM. AWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis. Proc Natl Acad Sci U S A. 2019 Jan 22;116(4):1414-1419. doi: 10.1073/pnas.1816585116. Epub 2019 Jan 7. PMID: 30617067; PMCID: PMC6347715.

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1: Hong WD, Benayoud F, Nixon GL, Ford L, Johnston KL, Clare RH, Cassidy A, Cook
DAN, Siu A, Shiotani M, Webborn PJH, Kavanagh S, Aljayyoussi G, Murphy E, Steven
A, Archer J, Struever D, Frohberger SJ, Ehrens A, Hübner MP, Hoerauf A, Roberts
AP, Hubbard ATM, Tate EW, Serwa RA, Leung SC, Qie L, Berry NG, Gusovsky F,
Hemingway J, Turner JD, Taylor MJ, Ward SA, O'Neill PM. AWZ1066S, a highly
specific anti-Wolbachia drug candidate for a short-course treatment of
filariasis. Proc Natl Acad Sci U S A. 2019 Jan 22;116(4):1414-1419. doi:
10.1073/pnas.1816585116. Epub 2019 Jan 7. PubMed PMID: 30617067; PubMed Central
PMCID: PMC6347715.