MW 440.5 Da, Purity >99%. Highly potent, irreversible Bruton tyrosine kinase (BTK) inhibitor (IC50 = 0.5nM). Inhibits autophosphorylation of BTK IC50 = 11 nM), and phophorylation of PLCγ (IC50 = 29 nM) and ERK (IC50 = 13 nM). Potently inhbits BLK, BMS, FGR, EGFR and ITK kinases. Blocks B-cell antigen receptor (BCR) activation. Cytotoxic to chronic lymphocytic leukemia (CLL) cells.
AA407514, AGMX 1, AI838772, AT, ATK, AW493413, Agammaglobulinaemia tyrosine kinase, Avian erythroblastic leukemia viral (v erb b) oncogene homolog, B lymphocyte kinase, B lymphoid tyrosine kinase, B-cell progenitor kinase, BBDS, BEK, BEK fibroblast growth factor receptor, BFR1, BLK nonreceptor tyrosine kinase, BLK_HUMAN, BMX non receptor tyrosine kinase, BMX_HUMAN, BONE MARROW KINASE, X-LINKED, BPK, BTK_HUMAN, Bone marrow tyrosine kinase gene in chromosome X protein, Bruton agammaglobulinemia tyrosine kinase, Bruton tyrosine kinase, Bruton闂佺偨鍎查悰 Tyrosine Kinase, C ret, CD 135, CD135 antigen, CD332, CD332 antigen, CDHF 12, CDHR16, CEK3, CFD1, Cadherin family member 12, Cadherin related family member 16, Cell growth inhibiting protein 40, Cell proliferation inducing protein 61, Cellular Yes 1 protein, Craniofacial dysostosis 1, Cytoplasmic tyrosine-protein kinase BMX, DKFZP586N0721, DKFZp686J10186, EC 2.7.10.2, ECT1, EGFR_HUMAN, ELKS Fusion gene, ERBB, ERBB1, ETK, Epidermal growth factor receptor, Epidermal growth factor receptor (avian erythroblastic leukemia viral (v erb b) oncogene homolog), Epidermal growth factor receptor (erythroblastic leukemia viral (v erb b) oncogene homolog avian), Epithelial and endothelial tyrosine kinase, Errp, FGF receptor, FGFR2_HUMAN, FL cytokine receptor, FLJ11090, FLJ26625, FLT3_HUMAN, Fetal liver kinase 2, Fibroblast growth factor receptor 2, Flk 2, Fms related tyrosine kinase 3, Fms-like tyrosine kinase 3, Growth factor receptor tyrosine kinase type III, HER1, HSCR 1, HSPC193, HST17436, Hck 2, HsT441, IMD 1, JTK 8, JV15-2, JWS, Jackson Weiss syndrome, K-sam, KGFR, Keratinocyte growth factor receptor, Keratinocyte growth factor receptor 2, LDS1C, LDS3, LYN proto oncogene, Src family tyrosine kinase, LYN_HUMAN, Lck/Yes related novel protein tyrosine kinase, Ly-72, MAD (mothers against decapentaplegic Drosophila) homolog 3, MAD homolog 3, MAD, mothers against decapentaplegic homolog 3, MADH 3, MEN2A, MEN2B, MGC 10442, MGC104252, MGC112732, MGC126261, MGC126262, MGC60396, MODY 11, MTC 1, Mad homolog JV15 2, Mad protein homolog, Mothers against DPP homolog 3, Mothers against decapentaplegic homolog 3, Multiple endocrine neoplasia and medullary thyroid carcinoma 1, NISBD2, NKT38, NTK 38, ONCOGENE LYN, OTTHUMP0000004234, OTTHUMP00000063593, Oncogen ERBB, Oncogene RET, PIG61, PSCTK 1, PSCTK 2, PSCTK 3, PTC, Protein tyrosine kinase BMX, Proto oncogene tyrosine protein kinase YES, Proto-oncogene c-ErbB-1, Proto-oncogene c-Ret, Proto-oncogene c-Yes, Proto-oncogene tyrosine-protein kinase receptor ret, RET ELE1, RET transforming sequence, RET51, RET9, RET_HUMAN, RP24-311F12.2, Receptor type tyrosine protein kinase FLT3, Receptor tyrosine-protein kinase ErbB-1, Ret Proto oncogene, SA7, SCAN1, SMA and MAD related protein 3, SMAD, SMAD family member 3, SMAD, mothers against DPP homolog 3, SMAD3_HUMAN, STK-1, Species antigen 7, Stem cell tyrosine kinase 1, TK14, TK25, TYDP, TYDP1_HUMAN, Tyr-DNA phosphodiesterase 1, Tyrosine kinase B lymphocyte specific, Tyrosine protein kinase, Tyrosine-protein kinase BLK, Tyrosine-protein kinase BTK, Tyrosine-protein kinase Lyn, Tyrosine-protein kinase Yes, Tyrosine-protein kinase receptor FLT3, Tyrosyl-DNA phosphodiesterase 1, Urogastrone, V yes 1 Yamaguchi sarcoma viral related oncogene homolog, Viral oncogene yes 1 homolog 1, Wa5, XLA, YES proto oncogene 1, Src family tyrosine kinase, YES1 proto oncogene, Src family tyrosine kinase, YES_HUMAN, Yamaguchi sarcoma oncogene, Yamaguchi sarcoma viral (v yes 1) related oncogene homolog, Yes 1, bacteria-expressed kinase, c Yes, dominant-negative kinase-deficient Brutons tyrosine kinase, erb-b2 receptor tyrosine kinase 1, hMAD-3, hSMAD3, hydroxyaryl-protein kinase, mENA, p53Lyn, p55-BLK, p56Lyn, p61-Yes, protein tyrosine kinase, receptor like 14, soluble FGFR4 variant 4, truncated Bruton agammaglobulinemia tyrosine kinase, tyrosine-protein kinase BTK isoform (lacking exon 14, tyrosine-protein kinase receptor ret, v yes 1 Yamaguchi sarcoma viral oncogene homolog 1, v-erb-b Avian erythroblastic leukemia viral oncogen homolog, wa2
MW 440.5 Da, Purity >99%. Highly potent, irreversible Bruton tyrosine kinase (BTK) inhibitor (IC50 = 0.5nM). Inhibits autophosphorylation of BTK IC50 = 11 nM), and phophorylation of PLCγ (IC50 = 29 nM) and ERK (IC50 = 13 nM). Potently inhbits BLK, BMS, FGR, EGFR and ITK kinases. Blocks B-cell antigen receptor (BCR) activation. Cytotoxic to chronic lymphocytic leukemia (CLL) cells.
Soluble in DMSO to 50mM.
Highly potent, irreversible Bruton tyrosine kinase (BTK) inhibitor (IC50 = 0.5nM). Inhibits autophosphorylation of BTK IC50 = 11 nM), and phophorylation of PLCγ (IC50 = 29 nM) and ERK (IC50 = 13 nM). Potently inhbits BLK, BMS, FGR, EGFR and ITK kinases. Blocks B-cell antigen receptor (BCR) activation. Cytotoxic to chronic lymphocytic leukemia (CLL) cells.
Solutions in DMSO may be stored at -20°C for up to 3 months.
Lyn BLK Ret EGFR TDP1 FGFR2 Smad3 Yes1 BTK and Flt3/CD135 represent a diverse group of proteins involved in various signaling pathways. Lyn a Src family tyrosine kinase is expressed in hematopoietic cells and plays roles in signal transduction. BLK and Yes1 are also tyrosine kinases belonging to the Src family with expression largely in B cells and epithelial cells respectively. Ret a receptor tyrosine kinase is significant in nervous system development. EGFR a receptor tyrosine kinase known as ErbB1 or HER1 is widely expressed in epithelial tissues and weighs approximately 134 kDa. TDP1 a DNA repair enzyme is expressed in cell nuclei. FGFR2 a receptor tyrosine kinase is present in mesenchymal and epithelial tissues. Smad3 a signaling mediator functions downstream in transforming growth factor-beta signaling. BTK a non-receptor tyrosine kinase functions in B cell development while Flt3/CD135 another receptor tyrosine kinase is expressed in hematopoietic progenitor cells. BMX a tyrosine kinase shows expression in various tissues including endothelial and epithelial cells.
These proteins perform diverse and significant roles. Lyn BLK Yes1 and BTK participate in immune cell signaling pathways modulating cell activation and differentiation. Ret functions in cell growth and neuronal development often forming complexes with co-receptors like GFRα. EGFR is important for cell growth differentiation and survival often partnering with ligands like EGF. TDP1 acts in DNA repair mechanisms while FGFR2 influences cell proliferation and differentiation. Smad3 mediates TGF-beta-induced transcriptional responses and Flt3/CD135 regulates hematopoietic progenitor cell survival and proliferation. BMX contributes to cellular processes like growth and survival through signaling modulation.
These proteins integrate into critical signaling networks. Lyn and BTK engage in the B cell receptor pathway interfacing with proteins such as Syk and PLCγ2. EGFR plays a role in the MAPK/ERK pathway interacting with GRB2 and SOS to relay signals. FGFR2 also participates in the MAPK/ERK pathway influencing cell division and differentiation. Ret links to the PI3K/AKT pathway interacting with Shc and phosphoinositide 3-kinase modulating cell growth and survival. Smad3 as part of the TGF-beta pathway collaborates with Smad4 to control gene expression.
These proteins associate with various conditions. Lyn and BTK have links to chronic lymphocytic leukemia (CLL) where aberrant signaling leads to uncontrolled B cell proliferation. EGFR mutations are common in non-small cell lung cancer influencing tumor growth and resistance to therapy. Ret mutations associate with multiple endocrine neoplasia type 2 (MEN2) driving abnormal cancerous growths in endocrine tissues. FGFR2 mutations relate to skeletal disorders like Apert syndrome while Smad3 mutations connect to vascular diseases like aneurysms. Flt3 mutations are commonly found in acute myeloid leukemia (AML) influencing uncontrolled cell proliferation. BMX involvement appears in prostate cancer affecting tumor progression and resistance. These connections highlight the importance of targeted therapies such as BTK inhibitors like ibrutinib which inhibit BTK's role in disease pathways.
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