2. PI3K/Akt/mTOR Anti-infection
  3. PI4K Parasite
  4. BQR-695

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

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

BQR-695 Chemical Structure

BQR-695 Chemical Structure

CAS No. : 1513879-21-4

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 88 In-stock
Solid
5 mg USD 80 In-stock
10 mg USD 110 In-stock
25 mg USD 240 In-stock
50 mg USD 350 In-stock
100 mg USD 550 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

BQR-695 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE BQR-695

View All PI4K Isoform Specific Products:

View All Isoforms
PI4KIIIβ PI4KIIIα PI4K PI4KII

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View All Isoforms
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target[1]

human PI4KIIIβ

80 nM (IC50)

Plasmodium

 

Plasmodium PI4KIIIβ

3.5 nM (IC50)

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BQR-695 Related Antibodies
Molecular Weight

352.39

Formula

C19H20N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC(C(OC)=C1)=CC=C1C2=CC3=NC(NCC(NC)=O)=CN=C3C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (141.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: 2.5 mg/mL (7.09 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.92%

COA (245 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8378 mL 14.1888 mL 28.3776 mL 70.9441 mL
5 mM 0.5676 mL 2.8378 mL 5.6755 mL 14.1888 mL
10 mM 0.2838 mL 1.4189 mL 2.8378 mL 7.0944 mL
15 mM 0.1892 mL 0.9459 mL 1.8918 mL 4.7296 mL
20 mM 0.1419 mL 0.7094 mL 1.4189 mL 3.5472 mL
25 mM 0.1135 mL 0.5676 mL 1.1351 mL 2.8378 mL
30 mM 0.0946 mL 0.4730 mL 0.9459 mL 2.3648 mL
40 mM 0.0709 mL 0.3547 mL 0.7094 mL 1.7736 mL
50 mM 0.0568 mL 0.2838 mL 0.5676 mL 1.4189 mL
60 mM 0.0473 mL 0.2365 mL 0.4730 mL 1.1824 mL
80 mM 0.0355 mL 0.1774 mL 0.3547 mL 0.8868 mL
100 mM 0.0284 mL 0.1419 mL 0.2838 mL 0.7094 mL
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BQR-695 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BQR-6951513879-21-4NVP-BQR695BQR695BQR 695PI4KParasitePhosphatidylinositol 4 kinasesPI4 kinasesInhibitorinhibitorinhibit

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