製品番号: HY-139481

TL-895

1 Cited Publications

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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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.86%
CAS 番号: 1415823-49-2
分子式: C₂₅H₂₆FN₅O₂
分子量:447.50

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

TL-895 構造式

CAS 番号: 1415823-49-2

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数量

Amount: USD 0.00

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Use of MCE Products

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (1)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[3]

IL-1β

IL-8

IL-6

Interleukin Related アイソフォーム固有の製品をすべて表示 :

TNF Receptor アイソフォーム固有の製品をすべて表示 :

体外実験

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) (EC_₅₀ 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.

体内実験

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.

Animal Model:

BXSB-Yaa model established in C57BL/6mice^[1]
Dosage:

25 mg/kg feed, average 3.7 mg/kg daily
Administration:

Oral administration (p.o.), for 11 weeks
Result:

Significantly reduced the urine albumin/creatinine ratio (UACR).
Significantly increased survival rate.
Significantly reduced the scores of glomerular crescents, protein casts, interstitial inflammation and vasculitis.
Significantly reduced the levels of anti-dsDNA, anti-histone, and anti-Ro/SSA antibodies.
Reduced the expression of CD69 on B and T cells, and decreased the number of plasma cells (B220⁻).

Animal Model:

Pristane-DBA/1 model established in C57BL/6mice^[1]
Dosage:

25 mg/kg feed, average 3.7 mg/kg daily
Administration:

Oral administration (p.o.), for 4 months
Result:

Significantly reduced the clinical arthritis score and the paw inflammation and injury score.
Reduced some of the autoantibodies (anti-dsDNA, anti-histone, anti-Ro/SSA).
Did not significantly affect the expression of IFN-regulating genes.
Partially reduced anti-dsDNA, anti-histone, and anti-Ro/SSA antibodies, but did not affect anti-Sm/RNP antibodies.
Increased the expression of CD69 on B cells, significantly reducing B220⁺ cells.

Animal Model:

MCL xenograft model induced by Maver-1, Granta519, Mino, Jeko-1 established in 6-week-old female nude (NMRI:nu/nu) or CB17-SCID mice^[3]
Dosage:

25 mg/kg
Administration:

Oral gavage (i.g.), once daily for 14 (Maver-1 and Granta519), 20 (Jeko-1) and 27 (Mino) days
Result:

Showed significant anti-tumor activity in a specific MCL model.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1415823-49-2
性状 Solid
分子量 447.50
分子式 C₂₅H₂₆FN₅O₂
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
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Cancer Res Commun

Drug-drug interaction liabilities with BTK inhibitor TL-895. [Abstract]

2025 Aug 22. PMID: 40844833

溶剤 & 溶解度

体外:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2346 mL

11.1732 mL

22.3464 mL

5 mM

0.4469 mL

2.2346 mL

4.4693 mL

10 mM

0.2235 mL

1.1173 mL

2.2346 mL

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.

モル濃度計算機

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

Mass Mass

濃度濃度

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分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

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体内:

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

Stock Solution Working Solution

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.

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.

Protocol 3

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

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

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
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+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

TL-895

1 Cited Publications

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TL-895

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MedChemExpress（MCE）の使用を引用している文献 TL-895

Interleukin Related アイソフォーム固有の製品をすべて表示

TNF Receptor アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

Help & FAQs

Complete Stock Solution Preparation Table

TL-895 関連分類

HY-139481 関連分類