2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. ARQ 531

ARQ 531  (Synonyms: MK-1026)

Cat. No.: HY-112215 Purity: 99.24%
COA Handling Instructions

ARQ 531 (MK-1026) is a reversible non-covalent and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.

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

ARQ 531 Chemical Structure

ARQ 531 Chemical Structure

CAS No. : 2095393-15-8

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Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 165 In-stock
Solid
5 mg USD 150 In-stock
10 mg USD 250 In-stock
25 mg USD 550 In-stock
50 mg USD 950 In-stock
100 mg USD 1650 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE ARQ 531

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

ARQ 531 (MK-1026) is a reversible non-covalent and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.

IC50 & Target

IC50: 0.85 nM (WT-BTK), 0.39 nM (C481S-BTK)[1].
In Vitro

ARQ 531 shows strong target inhibition in TMD8 cell line. The IC50 values are 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively, in biochemical assay. Additionally, ARQ 531 also shows strong inhibition of TEK kinases with IC50s of 5.23 nM (BMX), 5.80 nM (TEC), 36.4 nM (TXK). The IC50s of ARQ 531 for SRC kinases are 3.86 nM (LCK), 4.22 nM (YES), 9.71 nM (BLK), 18.3 nM (HCK), 18.8 nM (LYNa), 25.9 nM (FGR), 32.2 nM (FYN), 48.0 nM (FRK) and for TRK kinases are 11.7 nM (TrkB), 13.1 nM (TrkA), 19.1 nM (TrkC). ARQ 531 inhibits proliferation of diverse types of cell lines (TMD8: GI50=0.13 μM, REC1: GI50=0.18 nM) and shows potency in cell lines that are addict to BCR, Src-family kinase and PI3K/AKT pathways.

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

ARQ 531 is efficacious in TMD-8 tumor xenograft model. ARQ 531 causes complete tumor regression after 14 days of treatment. ARQ 531 is also efficacious in collagen induced arthritis model. ARQ 531 demonstrates potent efficacy against arthritis in mouse model. In the BTK driven TMD8 xenograft mouse model, ARQ 531 demonstrates excellent anti-tumor activity with durable response. ARQ 531 demonstrates in vivo efficacy in a mouse collagen-induced arthritis (CIA) model[1].

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

478.93

Appearance

Solid

Formula

C25H23ClN4O4
CAS No.
SMILES

O=C(C1=C(C=C(OC2=CC=CC=C2)C=C1)Cl)C3=CNC4=NC=NC(N[[email protected]@H]5CC[[email protected]@H](CO)OC5)=C34
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 : ≥ 50 mg/mL (104.40 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0880 mL 10.4399 mL 20.8799 mL
5 mM 0.4176 mL 2.0880 mL 4.1760 mL
10 mM 0.2088 mL 1.0440 mL 2.0880 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 (4.34 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.34 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.34 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.24%

COA (246 KB) HNMR (286 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

Biochemical inhibition assay is measured using full length BTK constructs of wild type or C481S mutant. Profiling on 236 kinases identifies 45 kinases with >50% inhibition at 200 nM concentration of ARQ 531. Subsequently, the potency of this ATP competitive inhibitor is determined on such kinases at the physiological 1 mM ATP concentration cells are treated with increasing concentrations of inhibitors in SUDHL-4 for 2 hours, following stimulation with either anti-IgM or growth factors cells are lysed for Western blot analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Six week old female CB-17 SCID mice (1-2 weeks) are used. Mice are housed in sterile micro isolator cages, five mice per cage and receive food and water ad libitum. Female SCID mice are implanted subcutaneously with 8x106 TMD8 cells in 0.2 mL HBSS with 50% standard concentration BD matrigel in the upper right flank area. Mice are monitored and staged on day 14 (post injection of tumor cells) when size reaches approximately 400 mg. Oral daily dosing with ARQ 531 at 100 mg/kg or vehicle began on stage day. Tumor measurements and body weights are collected three times a week. In vivo Target and pathway inhibition is studied in mouse TMD8 xenograft model. Percent inhibition relative to the vehicle control is determined using densitometry analysis and the intensity of actin band is used as a loading control and the percentage of vehicle group is designated as 100%. DBA1/J mice are immunized with collagen to develop the arthritis, following the onset of arthritis, mice are randomized into treatment groups. Treatment is initiated by oral dosing of ARQ 531 at 25, 50 and 75 mg/kg and continued daily through arthritis day 14. Clinical scores are assessed for each of the paws on study arthritis days 1-15[1].

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

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Keywords:

ARQ 5312095393-15-8MK-1026ARQ531ARQ-531MK1026MK 1026BtkBruton tyrosine kinaseInhibitorinhibitorinhibit

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