2. Protein Tyrosine Kinase/RTK
  3. Btk
  4. Edralbrutinib

Edralbrutinib (TG-1701) is a highly selective, orally available irreversible BTK inhibitor, with an EC50 of 6.70 nM and a Kd of 3 nM against human BTK. Edralbrutinib inhibits downstream signaling of the B cell receptor, induces dephosphorylation of Ikaros Ser442/445, promotes nuclear exclusion of Ikaros, attenuates Ikaros gene signatures, and exerts anti-tumor activity. Edralbrutinib can be used in research related to B-cell non-Hodgkin lymphoma, chronic lymphocytic leukemia, mantle cell lymphoma, follicular lymphoma, and diffuse large B-cell lymphoma.

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Edralbrutinib

Edralbrutinib Chemical Structure

CAS No. : 1858206-58-2

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Edralbrutinib Related Antibodies

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  • Purity & Documentation

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Description

Edralbrutinib (TG-1701) is a highly selective, orally available irreversible BTK inhibitor, with an EC50 of 6.70 nM and a Kd of 3 nM against human BTK. Edralbrutinib inhibits downstream signaling of the B cell receptor, induces dephosphorylation of Ikaros Ser442/445, promotes nuclear exclusion of Ikaros, attenuates Ikaros gene signatures, and exerts anti-tumor activity. Edralbrutinib can be used in research related to B-cell non-Hodgkin lymphoma, chronic lymphocytic leukemia, mantle cell lymphoma, follicular lymphoma, and diffuse large B-cell lymphoma[1][2].

In Vitro

Edralbrutinib (TG-1701) (1 μM) exhibits high selectivity for BTK over 440 other human kinases, with a BTK Kd of 3 nM when tested at 1 μM[1].
Edralbrutinib (TG-1701) inhibits wild-type BTK enzymatic activity with an EC50 of 6.70 nM in a cell-free kinase activity assay[1].
Edralbrutinib (TG-1701) (0.1-100 nM) achieves full BTK occupancy in BTK-sensitive DoHH-2 follicular lymphoma cells at a concentration of 30 nM[1].
Edralbrutinib (TG-1701) (72 h) inhibits viability of 10 parental B-NHL cell lines with a mean GI50 of 6.4 μM after 72-hour incubation, including a mean GI50 of 4.3 μM in MCL cell lines and a GI50 of 3.83 μM in REC-1 MCL cells[1].
Edralbrutinib (TG-1701) (1 μM; 24 h) at 1 μM for 24 hours impairs Ikaros signaling in BTK-sensitive REC-1 MCL cells by downregulating pBTK and MYC, upregulating YES1 (to a greater extent than ibrutinib), and inducing nuclear exclusion of Ikaros[1].
Edralbrutinib (TG-1701) (1 μM; 24 h) at 1 μmol/L for 24 hours induces nuclear exclusion of Ikaros in BTK-sensitive JEKO-1 MCL cells, reducing nuclear Ikaros levels by 50% to 70%[1].

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

Edralbrutinib Related Antibodies
In Vivo

Edralbrutinib (TG-1701) (25-100 mg/kg; p.o.; twice a day; 21 days; 50 mg/kg; p.o.; single dose) dose-dependently inhibits MINO MCL xenograft tumor growth, with 100 mg/kg (orally, twice daily for 21 days) achieving 78% TGI, and a single 50 mg/kg oral dose maintains suppression of BCR pathway kinases for at least 24 hours[1].
Edralbrutinib (25 mg/kg; p.o.; once daily; 17 days) inhibits BTK-sensitive REC-1 MCL xenograft growth by 53% over 17 days and modulates the Ikaros signaling pathway, including reduced MYC expression and increased YES1 expression[1].
Edralbrutinib (25 mg/kg; p.o.; once daily; 17 days) does not significantly inhibit tumor growth in the noncanonical NF-κB-driven BTK inhibitor-resistant UPN-IbruR MCL xenograft model, with no associated modulation of Ikaros signaling pathway components[1].

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

Animal Model: Nude mice (6-7 weeks old; subcutaneous inoculation of MINO MCL cells)[1]
Dosage: 25 mg/kg (TGI); 50 mg/kg (TGI; BCR pathway suppression); 100 mg/kg (TGI)
Administration: p.o.; twice a day; 21 days; p.o.; single dose
Result: Achieved 56% tumor growth inhibition (TGI).
Achieved 72% tumor growth inhibition (TGI).
Achieved 78% tumor growth inhibition (TGI).
Caused rapid dephosphorylation of pBTK within 2 hours and dephosphorylation of pAKT within 4 hours, with both effects maintained for at least 24 hours.
Animal Model: CB17-SCID mice (subcutaneous inoculation of REC-1GFP+LUC+ BTK-sensitive MCL cells)[1]
Dosage: 25 mg/kg
Administration: p.o.; once daily; 17 days
Result: Achieved 53% tumor growth inhibition (TGI) compared to vehicle control.
Reduced pBTK levels by 70% relative to vehicle controls.
Increased YES1 protein levels by 2.25-fold relative to vehicle controls.
Reduced MYC protein levels by 79% relative to vehicle controls.
Reduced Ikaros protein levels by 23% relative to vehicle controls.
Significantly upregulated YES1 mRNA compared to vehicle controls.
Significantly downregulated MYC mRNA compared to vehicle controls.
Showed reduced CD20 expression and nuclear exclusion of Ikaros in treated tumors.
Animal Model: CB17-SCID mice (subcutaneous inoculation of UPN-IbruR noncanonical NF-κB-driven BTK inhibitor-resistant MCL cells)[1]
Dosage: 25 mg/kg
Administration: p.o.; once daily; 17 days
Result: Did not significantly reduce UPN-IbruR tumor volume compared to vehicle control.
Showed no reduction in pBTK levels relative to vehicle controls.
Showed no significant change in YES1 or MYC protein levels relative to vehicle controls.
Showed no significant modulation of YES1 or MYC mRNA levels relative to vehicle controls.
Showed no change in CD20 expression or Ikaros nuclear localization in treated tumors.
Clinical Trial
Molecular Weight

489.47

Formula

C26H21F2N5O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(C(N)=NN1)C(C(C=C3)=CC=C3OC(C(F)=CC=C4)=C4F)=CN2[C@@](CC5)([H])CN5C(C#CC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (25.54 mM; ultrasonic and warming and heat to 60°C; 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 2.0430 mL 10.2151 mL 20.4303 mL
5 mM 0.4086 mL 2.0430 mL 4.0861 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (2.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 1.25 mg/mL (2.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0430 mL 10.2151 mL 20.4303 mL 51.0757 mL
5 mM 0.4086 mL 2.0430 mL 4.0861 mL 10.2151 mL
10 mM 0.2043 mL 1.0215 mL 2.0430 mL 5.1076 mL
15 mM 0.1362 mL 0.6810 mL 1.3620 mL 3.4050 mL
20 mM 0.1022 mL 0.5108 mL 1.0215 mL 2.5538 mL
25 mM 0.0817 mL 0.4086 mL 0.8172 mL 2.0430 mL
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Edralbrutinib 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:

Edralbrutinib1858206-58-2TG-1701TG1701TG 1701BtkBruton tyrosine kinasefollicular lymphomamantle cell lymphomaDoHH-2 follicular lymphoma cellsB-cell non-Hodgkin lymphomaIkarosdiffuse large B-cell lymphomachronic lymphocytic leukemiaREC-1 MCL cellsB-cell receptorInhibitorinhibitorinhibit

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