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  2. Parasite
  3. AN3661

AN3661 

Cat. No.: HY-128204 Purity: 99.66%
Handling Instructions

AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains (mean IC50=32 nM), Ugandan field isolates (mean ex vivo IC50=64 nM), and murine P. berghei and P. falciparum infections.

For research use only. We do not sell to patients.

AN3661 Chemical Structure

AN3661 Chemical Structure

CAS No. : 1268335-33-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 116 In-stock
Estimated Time of Arrival: December 31
5 mg USD 105 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains (mean IC50=32 nM), Ugandan field isolates (mean ex vivo IC50=64 nM), and murine P. berghei and P. falciparum infections[1].

In Vitro

AN3661 is active at nanomolar (IC50=20-56 nM) concentrations against P. falciparum laboratory strains known to be sensitive (3D7) or resistant (W2, Dd2, K1, HB3, FCR3 and TM90C2B), and AN3661 is similarly active in ex vivo studies of fresh Ugandan field isolates (mean ex vivo IC50=64 nM). AN3661 shows minimal cytotoxicity against mammalian cell lines, with the CC50 60.5 μM against Jurkat cells, and all other CC50 values greater than the highest concentrations tested (25 μM or above)[1].
AN3661 inhibits the stability of P. falciparum transcripts[1].

In Vivo

AN3661 (50-200 mg.kg; p.o.; daily for 4 days) inhibits murine P. berghei infections with ED90 (4 days) 0.34 mg/kg[1].
AN3661 is administered orally for 4 days, beginning on the third day of infection, the ED90 4 days after initiation of treatment is 0.57 mg/kg[1].

Animal Model: P. berghei-infected mice (malaria model)[1]
Dosage: 50, 100, 200 mg/kg
Administration: Orally; daily for 4 days
Result: Rapidly controlled parasitemias, with an ED90 of 0.34 mg/kg. Daily dosages of 50 mg/kg and 100 mg/kg extended survival, and mice treated with 200 mg/kg per day demonstrated long-term cures.
Molecular Weight

206.00

Formula

C₁₀H₁₁BO₄

CAS No.

1268335-33-6

SMILES

O=C(O)CCC1=C(B(O)OC2)C2=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (1213.59 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.8544 mL 24.2718 mL 48.5437 mL
5 mM 0.9709 mL 4.8544 mL 9.7087 mL
10 mM 0.4854 mL 2.4272 mL 4.8544 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (10.10 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (10.10 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (10.10 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AN3661AN 3661AN-3661ParasitePfCPSF3antimalarialcytotoxicityP. falciparuminfectionmalariasurvivalInhibitorinhibitorinhibit

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AN3661
Cat. No.:
HY-128204
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