2. Protein Tyrosine Kinase/RTK Immunology/Inflammation Apoptosis
  3. Btk BMX Kinase Interleukin Related TNF Receptor
  4. TL-895

TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor. TL-895 is active against recombinant BTK (average IC50: 1.5 nM) and inhibits only three additional kinases BLK, BMX (IC50 = 1.6 nM) and TXK with IC50 within tenfold of BTK activity. TL-895 inhibits BTK auto-phosphorylation at the Y223 phosphorylation site (IC50: 1-10 nM). The TL-895 effectively inhibits the production of inflammatory factors such as IL-8, IL-1β, MCP-1 and TNF-α by monocytes or macrophages, and reduces the chemotactic migration of MF cells towards SDF-1. TL-895 is used be for studies of chronic lymphocytic leukemia (CLL), myelofibrosis (MF), and B-cell malignancies.

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

TL-895

TL-895 Chemical Structure

CAS No. : 1415823-49-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

TL-895 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE TL-895

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

  • Biological Activity

  • Purity & Documentation

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Description

TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor. TL-895 is active against recombinant BTK (average IC50: 1.5 nM) and inhibits only three additional kinases BLK, BMX (IC50 = 1.6 nM) and TXK with IC50 within tenfold of BTK activity. TL-895 inhibits BTK auto-phosphorylation at the Y223 phosphorylation site (IC50: 1-10 nM). The TL-895 effectively inhibits the production of inflammatory factors such as IL-8, IL-1β, MCP-1 and TNF-α by monocytes or macrophages, and reduces the chemotactic migration of MF cells towards SDF-1. TL-895 is used be for studies of chronic lymphocytic leukemia (CLL), myelofibrosis (MF), and B-cell malignancies[1][2][3].

IC50 & Target[3]

IL-1β

 

IL-8

 

IL-6

 

In Vitro

TL-895 in Ramos cells blocks BCR activation with an IC50 of 45.75 nM and also inhibits FcR activation in basophils with an IC50 of 1.01 μM[1].
TL-895 (0-10 μM, 17-24 h) inhibits the production of TNF-α by macrophages, but does not inhibit the production of IFN in PBMCs, and blocks the activation of macrophages activated by FcR stimulation[1].
TL-895 (0.1 nM-10 μM) effectively inhibits pBTK in B cells, Ramos cells, monocytes and Hel-92 cells[2].
TL-895 reduces the chemotaxis of Hel-92 cells and inhibits their migration towards SDF-1[2].
TL-895 reduces the expression of CD69 (an activation marker) on B cells in PBMCs and whole blood stimulated by B-cell receptor (BCR) (EC₅₀ values are 12 nM and 21 nM respectively)[2].
TL-895 inhibits the production of IL-8, IL-1β, MCP-1, MIP-1α and IL-6 in healthy monocytes[2].
TL-895 (0.01-50 μM, 1-4 days) effectively inhibits the proliferation of primary CLL cells, and at the effective concentration, it shows no significant toxicity to primary liver cells and HepG2 cells[3].
TL-895 (0.05-3 μM) does not inhibit antibody-dependent cellular cytotoxicity (ADCC) and is suitable for use in combination with therapeutic antibodies[3].

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

TL-895 Related Antibodies
In Vivo

TL-895 (25 mg/kg feed, average 3.7 mg/kg daily, p.o., for 11 weeks) reduces the production of autoantibodies by inhibiting the BCR signal, and comprehensively improves multiple organ diseases in BXSB-Yaa lupus mice[1].
TL-895 (25 mg/kg feed, average 3.35 mg/kg daily, p.o., for 4 months) alleviates arthritis by inhibiting FcR signaling, and it suppresses local inflammation rather than systemic immune regulation in the Pristane (HY-N7819)-induced DBA/1 lupus model in mice[1].
TL-895 (25 mg/kg, once daily, i.g., for 14-27 days) significantly inhibits tumor growth in the Mino model, but has limited effect in the Jeko-1, Maver-1, and Granta519 models in mice[3].
TL-895 (once daily, i.g., for 13-25 days) shows significant anti-tumor activity in the Diffuse large B-cell lymphoma (DLBCL) patient-derived xenograft (PDX) models mice model[3].

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

447.50

Formula

C25H26FN5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCC(CNC2=NC=NC(N)=C2C3=CC=C(C=C3)OC4=CC=CC=C4)(CC1)F)C=C
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 (558.66 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 2.2346 mL 11.1732 mL 22.3464 mL
5 mM 0.4469 mL 2.2346 mL 4.4693 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.65 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.65 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:

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: 99.86%

SDS (251 KB)

COA (253 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

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. 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 2.2346 mL 11.1732 mL 22.3464 mL 55.8659 mL
5 mM 0.4469 mL 2.2346 mL 4.4693 mL 11.1732 mL
10 mM 0.2235 mL 1.1173 mL 2.2346 mL 5.5866 mL
15 mM 0.1490 mL 0.7449 mL 1.4898 mL 3.7244 mL
20 mM 0.1117 mL 0.5587 mL 1.1173 mL 2.7933 mL
25 mM 0.0894 mL 0.4469 mL 0.8939 mL 2.2346 mL
30 mM 0.0745 mL 0.3724 mL 0.7449 mL 1.8622 mL
40 mM 0.0559 mL 0.2793 mL 0.5587 mL 1.3966 mL
50 mM 0.0447 mL 0.2235 mL 0.4469 mL 1.1173 mL
60 mM 0.0372 mL 0.1862 mL 0.3724 mL 0.9311 mL
80 mM 0.0279 mL 0.1397 mL 0.2793 mL 0.6983 mL
100 mM 0.0223 mL 0.1117 mL 0.2235 mL 0.5587 mL
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TL-895 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:

TL-8951415823-49-2TL895TL 895BtkBMX KinaseInterleukin RelatedTNF ReceptorBruton tyrosine kinaseILTumor Necrosis Factor ReceptorTNFRMyelofibrosisCOVID-19Sars-CoV2CancerSolid TumorCarcinomaAcute Myeloid Leukemiaanti-viralInhibitorinhibitorinhibit

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