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Ibrutinib

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) BCL6 (1) Btk (20) CD20 (1) Eukaryotic Initiation Factor (eIF) (1) Fc Receptor (FcR) (1) Isotope-Labeled Compounds (3) Ligands for Target Protein for PROTAC (3) MNK (1) PI3K (1) PROTAC Linkers (2) PROTACs (2) Reference Standards (1) Src (1)
By Research Areas:	Cancer (26) Inflammation/Immunology (1)
Click Chemistry:	PROTAC Synthesis (2) Alkynes (2)

Inhibitors & Agonists

Inhibitory Antibodies

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10997

*Ibrutinib* Maximum Cited Publications 110 Publications Verification PCI-32765	Btk Ligands for Target Protein for PROTAC	Cancer
Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM .

HY-43521

Ibrutinib-MPEA	Btk	Cancer
Ibrutinib-MPEA (Compound 20) is ibrutinib derivative. Ibrutinib is a covalent and irreversible inhibitor of Bruton's tyrosine kinase (BTK) that has been used to treat haematological malignancies .

HY-10997A

Ibrutinib Racemate 1 Publications Verification PCI-32765 Racemate	Btk	Cancer
Ibrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with IC₅₀ value of 0.5 nM.

HY-78727

Ibrutinib deacryloylpiperidine IBT4A	Btk	Cancer
Ibrutinib deacryloylpiperidine (IBT4A) is an impurity of Ibrutinib . Ibrutinib is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM .

HY-10997R

Ibrutinib (Standard) PCI-32765 (Standard)	Reference Standards Btk Ligands for Target Protein for PROTAC	Cancer
Ibrutinib (Standard) is the analytical standard of Ibrutinib. This product is intended for research and analytical applications. Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM .

HY-100342

Ibrutinib-biotin 2 Publications Verification	Btk	Cancer
Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, extracted from patent WO2014059368A1 Compound 1-5, has an IC₅₀ of 0.755-1.02 nM for BTK.

HY-10997S

Ibrutinib-d5 PCI-32765-d₅	Btk	Cancer
Ibrutinib-d₅ is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor .

HY-100659

Dihydrodiol-Ibrutinib PCI-45227	Btk	Cancer
Dihydrodiol-Ibrutinib (PCI-45227) is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib .

HY-136113

Ibrutinib dimer	Btk	Cancer
Ibrutinib dimer is a Dimer of Ibrutinib. Ibrutinib dimer is an impurity of Ibrutinib . Ibrutinib is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM .

HY-10997AR

Ibrutinib Racemate (Standard)	Btk	Cancer
Ibrutinib (Racemate) (Standard) is the analytical standard of Ibrutinib (Racemate). This product is intended for research and analytical applications. Ibrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.

HY-130983

*N-piperidine Ibrutinib* hydrochloride**	Btk Ligands for Target Protein for PROTAC	Cancer
N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC₅₀s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively . N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC₅₀ of 7.9 nM .

HY-100659S

*Dihydrodiol-Ibrutinib-d5* PCI-45227-d₅	Btk Isotope-Labeled Compounds	Cancer
Dihydrodiol-Ibrutinib-d5 is the deuterium labeled Dihydrodiol-Ibrutinib (HY-100659). Dihydrodiol-Ibrutinib is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib .

HY-Z2289S1

*(S)-Ibrutinib-d4*	Isotope-Labeled Compounds	Others
(S)-Ibrutinib-d₄ is the deuterium labeled (S)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (Ibrutinib Impurity） (HY-Z2289).

HY-W749795

*N-Boc-Ibrutinib-d4*	Isotope-Labeled Compounds	Others
N-Boc-Ibrutinib-d₄ is the deuterium labeled (R)-tert-Butyl 3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate (HY-78859).

HY-148585

BTK-IN-22	Btk	Cancer
BTK-IN-22 is a BTK inhibitor (IC₅₀: 0.9 nM). BTK-IN-22 also inhibits BLX and BMX with IC₅₀s of 1.4 and 1.2 nM respectively. BTK-IN-22 shows improved kinase selectivity compared to Ibrutinib (HY-10997)

HY-148594

BTK-IN-23	Btk	Cancer
BTK-IN-23 is a BTK inhibitor (IC₅₀: 12.8 nM). BTK-IN-23 also inhibits BLX and BMX with IC₅₀s of 35.6 and 5.7 nM respectively. BTK-IN-23 shows improved kinase selectivity compared to Ibrutinib (HY-10997) .

HY-15805

KIN-8194	Src Btk	Cancer
KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC₅₀ values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice .

HY-13036A

IBT6A	Btk	Cancer
IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct . Ibrutinib is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM .

HY-13036B

IBT6A hydrochloride	Btk	Cancer
IBT6A hydrochloride is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct . Ibrutinib is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM .

HY-13036C

(Rac)-IBT6A hydrochloride	Btk	Cancer
(Rac)-IBT6A hydrochloride is a racemate of IBT6A hydrochloride. IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct . Ibrutinib is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM .

HY-13036

(Rac)-IBT6A	Btk	Cancer
(Rac)-IBT6A is a racemate of IBT6A. IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct . Ibrutinib is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM .

HY-150638

PI3Kδ/γ-IN-3	PI3K Apoptosis	Cancer
PI3Kδ/γ-IN-3 (Compound 58) is a potent and orally active PI3Kδ and PI3Kγ dual inhibitor with IC₅₀s of 1 nM and 16 nM, respectively. PI3Kδ/γ-IN-3 induces tumor cell apoptosis and can be used for B-cell malignancies research .

HY-163479

MNK1/2-IN-7	Eukaryotic Initiation Factor (eIF) MNK	Cancer
MNK1/2-IN-7 (compound 20j) is an orally available inhibitor of MNK1/2 with anticancer activity and hERG safety. MNK1/2-IN-7 also inhibits the phosphorylation of eIF4E, inhibiting the MNK/eIF4E signaling pathway and cancer cell proliferation. MNK1/2-IN-7 is synergistic with Ibrutinib (HY-109970) .

HY-130481

Propargyl-PEG4-acid	PROTAC Linkers	Cancer
Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib (HY-10997)-based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC₅₀ of 200 nM in THP-1 cells . Propargyl-PEG4-acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-130504

Propargyl-PEG1-acid 1 Publications Verification	PROTAC Linkers	Cancer
Propargyl-PEG1-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-CRBN PROTACs Ibrutinib(HY-10997)-based PROTAC 4 and PROTAC 5. PROTAC 5 causes the degradation of BTK and induces the degradation of CSK, LYN, and LAT2 at 10 μM . Propargyl-PEG1-acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-P991225

BI-1206	Fc Receptor (FcR) CD20	Inflammation/Immunology Cancer
BI-1206 is a recombinant and antagonistic human monoclonal antibody targeting FcγRIIB (CD32B). BI-1206 can block CD20 internalization induced by Rituximab (HY-P9913) itself or combined with others including Ibrutinib (HY-10997), Venetoclax (HY-15531), and CHOP. BI-1206 can enhance or recover the activity of Rituximab or other anti-CD20 monoclonal antibodies. BI-1206 has cytolytic activity against malignant B cells. BI-1206 can be studied for cancer research such as mantle cell lymphoma (MCL) .

HY-153220

NX-2127	PROTACs Btk	Cancer
NX-2127 (Compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk) . NX-2127 inhibits proliferation of BTK ^C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells . (Pink: BTK ligand 10 (HY-168302); Black: (R)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168348); Blue: Thalidomide 5-fluoride (HY-W087383)

HY-161989

DZ-837	PROTACs BCL6	Cancer
DZ-837 (compound 3d) is a PROTAC targeting BCL6 with a DC50 of approximately 600 nM. DZ-837 can induce cell cycle arrest and exert synergistic anticancer effects with Ibrutinib (HY-10997). DZ-837 is composed of PROTAC target protein ligand BCL6 ligand-2 (HY-161990) (red part), E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), and PROTAC Linker (HY-W245803) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is 2-(2,6-Dioxopiperidin-3-yl)-4-((2-(2-hydroxyethoxy)ethyl)amino)isoindoline-1,3-dione (HY-W924949) ^{[1] ^.}

Cat. No.	Product Name	Target	Research Area

HY-P991225

BI-1206	Fc Receptor (FcR) CD20	Inflammation/Immunology Cancer
BI-1206 is a recombinant and antagonistic human monoclonal antibody targeting FcγRIIB (CD32B). BI-1206 can block CD20 internalization induced by Rituximab (HY-P9913) itself or combined with others including Ibrutinib (HY-10997), Venetoclax (HY-15531), and CHOP. BI-1206 can enhance or recover the activity of Rituximab or other anti-CD20 monoclonal antibodies. BI-1206 has cytolytic activity against malignant B cells. BI-1206 can be studied for cancer research such as mantle cell lymphoma (MCL) .

Cat. No.	Product Name	Chemical Structure

HY-10997S

Ibrutinib-d5
Ibrutinib-d₅ is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor .

HY-100659S

*Dihydrodiol-Ibrutinib-d5*
Dihydrodiol-Ibrutinib-d5 is the deuterium labeled Dihydrodiol-Ibrutinib (HY-100659). Dihydrodiol-Ibrutinib is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitory activity towards BTK approximately 15 times lower than that of ibrutinib .

HY-Z2289S1

*(S)-Ibrutinib-d4*
(S)-Ibrutinib-d₄ is the deuterium labeled (S)-1-(3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (Ibrutinib Impurity） (HY-Z2289).

HY-W749795

*N-Boc-Ibrutinib-d4*
N-Boc-Ibrutinib-d₄ is the deuterium labeled (R)-tert-Butyl 3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidine-1-carboxylate (HY-78859).

Cat. No.	Product Name		Classification

HY-130481

Propargyl-PEG4-acid		Alkynes PROTAC Synthesis
Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib (HY-10997)-based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC₅₀ of 200 nM in THP-1 cells . Propargyl-PEG4-acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-130504

Propargyl-PEG1-acid 1 Publications Verification		PROTAC Synthesis Alkynes
Propargyl-PEG1-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-CRBN PROTACs Ibrutinib(HY-10997)-based PROTAC 4 and PROTAC 5. PROTAC 5 causes the degradation of BTK and induces the degradation of CSK, LYN, and LAT2 at 10 μM . Propargyl-PEG1-acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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