Art. -Nr.: HY-18012

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Spebrutinib

(Synonyms: AVL-292; CC-292)

17 Cited Publications

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Based on 17 publication(s) in Google Scholar

Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC₅₀ of 0.5 nM.

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Reinheit: 99.22%
CAS. Nr.: 1202757-89-8
Formel: C₂₂H₂₂FN₅O₃
Molecular Weight:423.44

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Spebrutinib Chemical Structure

CAS. Nr.: 1202757-89-8

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (17)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC₅₀ of 0.5 nM.

IC₅₀ & Target

IC50: <0.5 nM (Btk)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	IC₅₀	14.9 μM Compound: 3	Cytotoxicity against human 786-O cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human 786-O cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
A549	IC₅₀	1.98 μM Compound: 3	Cytotoxicity against human A549 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human A549 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
B-cell	IC₅₀	3.28 nM Compound: 2	Antiproliferative activity against B cells (unknown origin) Antiproliferative activity against B cells (unknown origin)	[PMID: 26976214]
BJ	IC₅₀	27.6 μM Compound: 3	Cytotoxicity against human BJ cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human BJ cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
HEF	IC₅₀	22.6 μM Compound: 3	Cytotoxicity against human HEF cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human HEF cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
HEL	IC₅₀	5.3 μM Compound: CC292	Antiproliferative activity against human HEL cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HEL cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
HeLa	IC₅₀	17.4 μM Compound: 3	Cytotoxicity against human HeLa cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
HepG2	IC₅₀	33.5 μM Compound: 3	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
HT-29	IC₅₀	18.9 μM Compound: 3	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
JeKo-1	IC₅₀	1.3 μM Compound: CC292	Antiproliferative activity against human JeKo1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human JeKo1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
JeKo-1	IC₅₀	1480 nM Compound: 8; Spe	Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human JeKo-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36399923]
Jurkat	IC₅₀	6.7 μM Compound: 3	Cytotoxicity against human Jurkat cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human Jurkat cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
K562	IC₅₀	12.6 μM Compound: 3	Cytotoxicity against human K562 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human K562 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
K562	IC₅₀	7400 nM Compound: 8; Spe	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36399923]
KARPAS-299	IC₅₀	20.3 μM Compound: 3	Cytotoxicity against human KARPAS299 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human KARPAS299 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
MCF-10A	IC₅₀	4.36 μM Compound: 3	Cytotoxicity against human MCF10A cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human MCF10A cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
MCF7	IC₅₀	29 μM Compound: 3	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
MDA-MB-231	IC₅₀	>40 μM Compound: 3	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
MOLT-4	IC₅₀	1463 nM Compound: 8; Spe	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36399923]
MV4-11	IC₅₀	245 nM Compound: 8; Spe	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK8 assay	[PMID: 36399923]
NAMALVA	IC₅₀	3.42 μM Compound: Spebrutinib	Antiproliferative activity against human NAMALWA cells after 72 hrs by CCK-8 assay Antiproliferative activity against human NAMALWA cells after 72 hrs by CCK-8 assay	[PMID: 29146136]
NCI-H1299	IC₅₀	38.5 μM Compound: 3	Cytotoxicity against human H1299 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human H1299 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
NCI-H3122	IC₅₀	32.5 μM Compound: 3	Cytotoxicity against human NCI-H3122 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human NCI-H3122 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
OCI-Ly10	IC₅₀	>10 μM Compound: CC292	Antiproliferative activity against human OCI-LY10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human OCI-LY10 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
PC-3	IC₅₀	22.2 μM Compound: 3	Cytotoxicity against human PC3 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability at 0.1 to 40 uM incubated for 48 hrs by MTS assay	[PMID: 31395509]
Raji	IC₅₀	17.6 μM Compound: CC292	Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
Raji	IC₅₀	21.6 μM Compound: 3	Antiproliferative activity against human Raji cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human Raji cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay	[PMID: 31395509]
Raji	IC₅₀	25.3 μM Compound: 4; AVL-292	Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay	[PMID: 27994736]
Raji	IC₅₀	25.3 μM Compound: Spebrutinib	Antiproliferative activity against human Raji cells measured after 48 hrs by CCK-8 assay Antiproliferative activity against human Raji cells measured after 48 hrs by CCK-8 assay	[PMID: 27956037]
Raji	IC₅₀	25.3 μM Compound: Spebrutinib	Antiproliferative activity against human Raji cells after 72 hrs by CCK-8 assay Antiproliferative activity against human Raji cells after 72 hrs by CCK-8 assay	[PMID: 29146136]
Raji	IC₅₀	29.4 μM Compound: 4	Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay Antiproliferative activity against human Raji cells after 48 hrs by CCK-8 assay	[PMID: 27912175]
Raji	IC₅₀	29.4 μM Compound: 4	Antiproliferative activity against human Raji cells over expressing BTK after 48 hrs by CCK-8 assay Antiproliferative activity against human Raji cells over expressing BTK after 48 hrs by CCK-8 assay	[PMID: 28432946]
Ramos	IC₅₀	14.2 μM Compound: Spebrutinib	Antiproliferative activity against human Ramos cells after 72 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells after 72 hrs by CCK-8 assay	[PMID: 29146136]
Ramos	IC₅₀	15.1 μM Compound: 4; AVL-292	Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay	[PMID: 27994736]
Ramos	IC₅₀	15.1 μM Compound: Spebrutinib	Antiproliferative activity against human Ramos cells measured after 48 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells measured after 48 hrs by CCK-8 assay	[PMID: 27956037]
Ramos	IC₅₀	18.8 μM Compound: 4	Antiproliferative activity against human Ramos cells over expressing BTK after 48 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells over expressing BTK after 48 hrs by CCK-8 assay	[PMID: 28432946]
Ramos	IC₅₀	20.9 μM Compound: 4	Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells after 48 hrs by CCK-8 assay	[PMID: 27912175]
Ramos	IC₅₀	3.9 μM Compound: CC292	Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 31843459]
Ramos	IC₅₀	5.44 μM Compound: 3	Antiproliferative activity against human Ramos cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay Antiproliferative activity against human Ramos cells assessed as reduction in cell growth incubated for 48 hrs by MTS assay	[PMID: 31395509]
Sf9	IC₅₀	0.6 nM Compound: 4; AVL-292	Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected sf9 cells using poly(4:1 Glu,Tyr) as substrate by ADP-Glo kinase assay Inhibition of recombinant human N-terminal His-tagged BTK expressed in baculovirus infected sf9 cells using poly(4:1 Glu,Tyr) as substrate by ADP-Glo kinase assay	[PMID: 27994736]
Sf9	IC₅₀	0.72 nM Compound: Spebrutinib	Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells measured after 60 mins by ADP-Glo kinase assay Inhibition of human recombinant full-length N-terminal His-tagged BTK expressed in baculovirus infected Sf9 insect cells measured after 60 mins by ADP-Glo kinase assay	[PMID: 27956037]
Sf9	IC₅₀	2.12 nM Compound: 3	Inhibition of human recombinant full length BTK expressed in baculovirus in Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 1 hr by ADP-Glo assay Inhibition of human recombinant full length BTK expressed in baculovirus in Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate incubated for 1 hr by ADP-Glo assay	[PMID: 31395509]
Sf9	IC₅₀	66.5 nM Compound: Spebrutinib	Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay Inhibition of recombinant human N-terminal GST-tagged JAK3 (781 to end residues) expressed in baculovirus infected Sf9 cells using poly (Glu,Tyr) 4:1 as substrate incubated for 60 mins in presence of ATP by ADP-Glo kinase assay	[PMID: 31866272]

In Vitro

Spebrutinib (CC-292) is a covalent, highly selective, orally active inhibitor of Btk with IC₅₀ value of 0.5 nM. Spebrutinib also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC₅₀s of 723 nM, 1.729 μM, 2.43 μM, 4.4 μM, and 7.15 μM, rspectively. Extensive analysis has revealed that the EC₅₀ of Btk occupancy from a Spebrutinib dose-response in Ramos cells (EC₅₀=6 nM) correlated directly with the cellular EC₅₀ of Btk kinase inhibition with Spebrutinib (EC₅₀=8 nM). Furthermore, the concentration at which Spebrutinib inhibits 90% of Btk activity in Ramos cells is 35 nM while the concentration of Spebrutinib required for 90% occupancy of Btk is 39 nM^[1].

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

Chemical Information

CAS. Nr. 1202757-89-8
Appearance Solid
Molecular Weight 423.44
Formel C₂₂H₂₂FN₅O₃
Color White to khaki
SMILES

COCCOC1=CC=C(NC2=NC=C(F)C(NC3=CC=CC(NC(C=C)=O)=C3)=N2)C=C1
Synonyms

AVL-292; CC-292
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (17)

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Journal Impact Factor

Blood

HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib. [Abstract]

2016 Jun 23;127(25):3237-52. PMID: 27143257
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Br J Pharmacol

A non-covalent inhibitor XMU-MP-3 overrides ibrutinib-resistant BtkC481S mutation in B-cell malignancies. [Abstract]

2019 Dec;176(23):4491-4509. PMID: 31364164
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Stem Cell Reports

Ibrutinib Displays Atrial-Specific Toxicity in Human Stem Cell-Derived Cardiomyocytes. [Abstract]

2019 May 14;12(5):996-1006. PMID: 31031187
Molecules

A Rapid and Sensitive Liquid Chromatography-Tandem Mass Spectrometry Bioanalytical Method for the Quantification of Encorafenib and Binimetinib as a First-Line Treatment for Advanced (Unresectable or Metastatic) Melanoma-Application to a Pharmacokinetic Study. [Abstract]

2022 Dec 22;28(1):79. PMID: 36615272
Sci Rep

Cysteine-reactive mitigators of small vessel disease-related NOTCH3 mutants. [Abstract]

2026 Mar 20;16(1):14300. PMID: 41862552
iScience

Inhibition of proteolytic and ATPase activities of the proteasome by the BTK inhibitor CGI-1746. [Abstract]

2024 Sep 24;27(11):110961. PMID: 39759071
ACS Pharmacol Transl Sci

Comprehensive Characterization of Bruton's Tyrosine Kinase Inhibitor Specificity, Potency, and Biological Effects: Insights into Covalent and Noncovalent Mechanistic Signatures. [Abstract]

2025 Mar 12;8(4):917-931. PMID: 40242575
R Soc Open Sci

A highly sensitive LC-MS/MS method to determine novel Bruton's tyrosine kinase inhibitor spebrutinib: application to metabolic stability evaluation. [Abstract]

2019 Jun 5;6(6):190434. PMID: 31312501
Leuk Res

Naquotinib exerts antitumor activity in activated B-cell-like diffuse large B-cell lymphoma. [Abstract]

2020 Jan:88:106286. PMID: 31865062
bioRxiv

COOKIE-Pro: Covalent Inhibitor Binding Kinetics Profiling on the Proteome Scale. [Abstract]

2025 Jun 22:2025.06.19.660637. PMID: 40666940
bioRxiv

2024 September 08.
Heliyon

Reactive intermediates formation and bioactivation pathways of spebrutinib revealed by LC-MS/MS: In vitro and in silico metabolic study. [Abstract]

2023 Jun 9;9(6):e17058. PMID: 37484253
Methods Mol Biol

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898
Oncotarget

Analysis of the mutational landscape of classic Hodgkin lymphoma identifies disease heterogeneity and potential therapeutic targets. [Abstract]

2017 Nov 30;8(67):111386-111395. PMID: 29340061
Patent

US20170333436A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 45 mg/mL (106.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.3616 mL

11.8080 mL

23.6161 mL

5 mM

0.4723 mL

2.3616 mL

4.7232 mL

10 mM

0.2362 mL

1.1808 mL

2.3616 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, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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: ≥ 2.5 mg/mL (5.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.90 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 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.
%
+
+
%
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

Protokoll

Cell Assay^[1]

Cells are incubated in serum-free RPMI media for 1-1.5 hours. Isolated human B cells are incubated with Spebrutinib at a final concentration of 0.001, 0.01, 0.1 and 1 μM. Ramos cells are incubated with 0.1 nM-3 μM Spebrutinib. Cells are then incubated in the presence of compound for 1 hour at 37°C. Following incubation, cells are centrifuged and resuspended in 100 μL of serum-free RPMI and BCR is stimulated with addition of 5 μg/mL α-human IgM. Samples are centrifuged, washed in phosphate-buffered saline (PBS), and lysed in 100 μL of Cell Extraction Buffer plus 1:10 (v/v) PhosSTOP Phosphatase Inhibitor and 1:10 (v/v) Complete Protease Inhibitor. Antibodies used for immunoblot analysis include P-PLCγ2, PLCγ2 (3871; CST), Syk (2712; CST), P-Syk (2710; CST), Btk, P-Btk, and Tubulin. Membranes are scanned on a Li-Cor Odyssey scanner using infrared fluorescence detection^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Evans EK, et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J Pharmacol Exp Ther. 2013 Aug;346(2):219-28. [Content Brief]

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, 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	2.3616 mL	11.8080 mL	23.6161 mL	59.0402 mL
	5 mM	0.4723 mL	2.3616 mL	4.7232 mL	11.8080 mL
	10 mM	0.2362 mL	1.1808 mL	2.3616 mL	5.9040 mL
	15 mM	0.1574 mL	0.7872 mL	1.5744 mL	3.9360 mL
	20 mM	0.1181 mL	0.5904 mL	1.1808 mL	2.9520 mL
	25 mM	0.0945 mL	0.4723 mL	0.9446 mL	2.3616 mL
	30 mM	0.0787 mL	0.3936 mL	0.7872 mL	1.9680 mL
	40 mM	0.0590 mL	0.2952 mL	0.5904 mL	1.4760 mL
	50 mM	0.0472 mL	0.2362 mL	0.4723 mL	1.1808 mL
	60 mM	0.0394 mL	0.1968 mL	0.3936 mL	0.9840 mL
	80 mM	0.0295 mL	0.1476 mL	0.2952 mL	0.7380 mL
	100 mM	0.0236 mL	0.1181 mL	0.2362 mL	0.5904 mL

Keywords

Spebrutinib

17 Cited Publications

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Spebrutinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Orally Active Compound Library

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Anti-Blood Cancer Compound Library

Cysteine Targeted Covalent Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

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High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Spebrutinib

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

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Complete Stock Solution Preparation Table

Spebrutinib

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Orally Active Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Cysteine Targeted Covalent Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Spebrutinib

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Spebrutinib Related Classifications

HY-18012 Related Classifications