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You are here:Home-Inhibitors & Agonists-Tyrosine Kinase-BTK

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Bruton's tyrosine kinase (Btk or BTK) is a kinase that plays a crucial role in B-cell development. BTK plays a crucial role in B cell maturation as well as mast cell activation through the high-affinity IgE receptor. BTK has emerged as a promising drug target for multiple diseases, particularly haematopoietic malignancies and autoimmune diseases related to B lymphocytes. Considerable progress has been made in the development of irreversible inhibitors, most of which target the SH3 pocket and the cysteine 481 residue of BTK.

Ibrutinib, a first-in-class BTK inhibitor, has demonstrated high response rates in both relapsed/refractory and treatment naïve chronic lymphocytic leukemia (CLL). However, scientists identified a structurally novel mutation (BTKT316A) in the SH2 domain, but not kinase domain, of Bruton tyrosine kinase which was associated with disease relapse.

Acalabrutinib (ACP-196) demonstrated higher biochemical and cellular selectivity than ibrutinib and spebrutinib. Acalabrutinib is a BTK inhibitor with key pharmacologic differentiators versus ibrutinib and spebrutinib and is currently being evaluated in clinical trials. More BTK inhibitors (GDC-0834, CGI-560, CGI-1746, HM-71224, CC-292, and ONO-4059, CNX-774, LFM-A13) are under inverstigation in the treatment of B-cell malignancies and autoimmune disorders.

 

References:

1. Winer ES, et al. Expert Opin Investig Drugs. 2012 Mar;21(3):355-61.

2. Kharfan-Dabaja MA, et al. Leukemia. 2014 Mar;28(3):507-17.

3. Aw A, et al. Drugs Aging. 2017 Jul;34(7):509-527.

4. Sharma S, et al. Oncotarget. 2016 Oct 18;7(42):68833-68841.

5. Barf T, et al. J Pharmacol Exp Ther. 2017 Nov;363(2):240-252.

Cat. No. Product Name CAS No. Information
GY02740

(±)-Zanubrutinib

1633350-06-7

The active enantiomer of Zanubrutinib (BGB3111), a potent, selective and orally available Btk inhibitor; shows much more restricted off-target activities against a panel of kinases, including ITK, compared with Ibrutinib; demonstrates nanomolar BTK inhibition activity, inhibits BCR aggregation-triggered BTK autophosphorylation, blocks downstream PLC-γ2 signaling, and potently inhibits cell proliferation in several MCL and DLBCL cell lines; demonstrates better anti-tumor activity than ibrutinib in TMD-8 subcutaneous xenograft model.

GY02686

Ibrutinib-biotin

1599432-18-4

A chemical probe that consists of Ibrutinib linked to biotin via a long chain linker, has IC50 of 0.755-1.02 nM for Btk kinase; extracted from patent WO2014059368A1 Compound 1-5.

GY02613

QL-47

1469988-75-7

A potent, selective, and irreversible BTK inhibitor with IC50 of 7 nM; inhibits BTK kinase activity with an IC50 of 7 nM, inhibits autophosphorylation of BTK on Tyr223 in cells with an EC50 of 475 nM, and inhibits phosphorylation of a downstream effector PLCγ2 (Tyr759) with an EC50 of 318 nM; induces a G1 cell cycle arrest that is associated with pronounced degradation of BTK protein in Ramos cells; inhibits the proliferation of B-cell lymphoma cancer cell lines at submicromolar concentrations.

GY02574

ONO-4059 hydrochloride

1439901-97-9

A potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively; weak activity against wt EGFR (IC50=184 nM); inhibits signaling pathways and cellular growth in both EGFRm(+) and EGFRm(+)/T790M(+) mutant cell lines in vitro; exhibits tumor regression in EGFR-mutant tumor xenograft and transgenic models; orally active.

GY02565

Fenebrutinib

1434048-34-6

An orally bioavailable, selective, non-covalent and reversible BTK inhibitor with IC50 of 2-9 nM; has demonstrated efficacy in pre-clinical autoimmune disease models and is being developed for the treatment of rheumatoid arthritis and lupus, with future development for other autoimmune indications.

GY02520

Evobrutinib

1415823-73-2

A potent, highly selective BTK inhibitor for the treatment of various autoimmune disorders.

GY02431

AVL-292 besylate

1360053-81-1

AVL-292 besylate (Spebrutinib, CC-292) is a highly selective, covalent Btk inhibitor with IC50 of <1 nM; also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC50s of 723 nM, 1.729 uM, 2.43 uM, 4.4 uM, and 7.15 uM, rspectively; shows anti-inflammatory activity in the collagen-induced arthritis model of autoimmune disease; also prevents NRG- and EGF-dependent growth factor-driven resistance to lapatinib in HER2(+) breast cancer cells.

GY02413

Tirabrutinib

1351636-18-4

A potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively; weak activity against wt EGFR (IC50=184 nM); inhibits signaling pathways and cellular growth in both EGFRm(+) and EGFRm(+)/T790M(+) mutant cell lines in vitro; exhibits tumor regression in EGFR-mutant tumor xenograft and transgenic models; orally active.

GY10114

BTK inhibitor 4b

1646608-10-7

BTK inhibitor 4b is a potent, highly selective inhibitors of BTK with IC50 of 4.2 and 0.9 nM against activated and unactivated BTK, respectively; demonstrates significant efficacy in models in vivo and good ADME and safety profiles.

GY01887

LFM-A13

244240-24-2

A highly specific inhibitor of BTK with Ki of 1.4 uM, IC50 of 17.2 uM; shows no activity against EGFR, IRK, JAK1, JAK3, or HCK; enhances the sensitivity to ceramide- or vincristine-induced apoptosis in BTK+ B-lineage leukemic cells; prolongs the median survival time of VPL-treated mice; also inhibits Plk3 with IC50 of 61 uM, prevented bipolar mitotic spindle assembly in human breast cancer cells and glioblastoma cells, delays tumor progression in MMTV/neu transgenic mouse model of HER2 positive breast cancer.

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