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BQR-695 (NVP-BQR695) (Synonyms: NVP-BQR695)

カタログ番号GC32163

BQR-695 (NVP-BQR695) は PI4KIIIβ です。ヒト PI4KIIIβ に対する IC50 が 80 および 3.5 nM の阻害剤。およびPI4KIIIβのプラスモディウム変異体;、それぞれ。

Products are for research use only. Not for human use. We do not sell to patients.

BQR-695 (NVP-BQR695) 化学構造

Cas No.: 1513879-21-4

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$56.00
在庫あり
5mg
$72.00
在庫あり
10mg
$99.00
在庫あり
50mg
$315.00
在庫あり
100mg
$495.00
在庫あり
200mg
$1,379.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

A clonal population of P. falciparum Dd2 parasites is used to initiate two or three independent parasite cultures under the initial selection pressure of 12 nM KAI407, 1 nM KAI715 or 40 nM BQR695. Stepwise drug evolution continues until the final concentration is at least 3-fold higher than the initial concentration (typically 80 to 120 days). For each of the ten resistant strains, copy number variations (CNVs) and single nucleotide variations (SNVs) are detected using a whole-genome tiling array and analyzed with PfGenominator. The susceptibility of each resistant strain to KAI407, KAI715, KDU691 and BQR695 is determined by the 72-hr SYBR Green cell proliferation assay with four independent experiments assayed in duplicate[2].

References:

[1]. Fowler ML, et al. Using hydrogen deuterium exchange mass spectrometry to engineer optimized constructs for crystallization of protein complexes: Case study of PI4KIIIβ with Rab11. Protein Sci. 2016 Apr;25(4):826-39.
[2]. McNamara CW, et al. Targeting Plasmodium PI(4)K to eliminate malaria. Nature. 2013 Dec 12;504(7479):248-253.

Background

BQR-695 is a PI4KIIIβ inhibitor with IC50s of 80 and 3.5 nM for human PI4KIIIβ and Plasmodium variant of PI4KIIIβ, respectively.

Treatment with 0.5 μM of either KAI407 or BQR695 causes GFP-PHOsh2 to redistribute to the parasite plasma membrane, consistent with depletion of intracellular PI4P upon inhibition of PfPI4K function. BQR695 shows no evidence of toxicity against mature red blood cells (RBCs), induces a schizont-stage arrest indistinguishable from that observed in imidazopyrazine-treated parasites and exhibits cross-resistance with the imidazopyrazine-resistant lines[2].

[1]. Fowler ML, et al. Using hydrogen deuterium exchange mass spectrometry to engineer optimized constructs for crystallization of protein complexes: Case study of PI4KIIIβ with Rab11. Protein Sci. 2016 Apr;25(4):826-39. [2]. McNamara CW, et al. Targeting Plasmodium PI(4)K to eliminate malaria. Nature. 2013 Dec 12;504(7479):248-253.

Chemical Properties

Cas No. 1513879-21-4 SDF
同義語 NVP-BQR695
Canonical SMILES COC(C(OC)=C1)=CC=C1C2=CC3=NC(NCC(NC)=O)=CN=C3C=C2
Formula C19H20N4O3 M.Wt 352.39
溶解度 DMSO : 100 mg/mL (283.78 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.8378 mL 14.1888 mL 28.3776 mL
5 mM 0.5676 mL 2.8378 mL 5.6755 mL
10 mM 0.2838 mL 1.4189 mL 2.8378 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 38 reference(s) in Google Scholar.)

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