MW 485.9 Da, Purity >98%. Potent, irreversible Her2/ErbB 2 and EGFR kinase inhibitor (IC50 values are 0.5, 0.4, 10 and 14 nM for EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 respectively). Shows antitumor effects in vivo. Orally active.
850140-72-6
> 98%
Powder
485.9 Da
C24H25ClFN5O3
10184653
Synthetic
1810038L18Rik, 4ICD, AA48924, ABL, ABL proto oncogene 1 non receptor tyrosine kinase, ABL1_HUMAN, ALS19, Abelson murine leukemia viral oncogene homolog 1, Abelson tyrosine protein kinase 1, Auxilin 2, Avian erythroblastic leukemia viral (v erb b) oncogene homolog, Avian erythroblastic leukemia viral oncogene homolog 4, Avian erythroblastic leukemia viral v erb b2 oncogene homolog 4, B lymphocyte kinase, B lymphoid tyrosine kinase, BLK nonreceptor tyrosine kinase, BLK_HUMAN, BSK, BSK/IYK, Bcr/c abl oncogene protein, Beta cell Src homology tyrosine kinase, C erb B2/neu protein, C85044, CD 135, CD135 antigen, CD340, CD340 antigen, CKI-epsilon, CKIe, CSAID Binding Protein 1, CSAID-binding protein, CSBP, CSBP 1, CSBP 2, CSNK 1E, CSPB1, Casein kinase 1 epsilon, Casein kinase I, Casein kinase I epsilon, Casein kinase I isoform epsilon, Cell growth inhibiting protein 40, Cell proliferation inducing protein 61, CerbB2, Csaids binding protein, Cyclin-G-associated kinase, Cytokine suppressive anti-inflammatory drug-binding protein, DNAJ26, DNAJC26, DYR1A_HUMAN, DYRK, DYRK 1, DYRK2_HUMAN, DYRKA, Doubletime, Drosophila, homolog of, Dual specificity YAK 1 related kinase, Dual specificity YAK1-related kinase, Dual specificity mitogen-activated protein kinase kinase 5, Dual specificity tyrosine (Y) phosphorylation regulated kinase 1A, Dual specificity tyrosine (Y) phosphorylation regulated kinase 2, Dual specificity tyrosine phosphorylation regulated kinase, Dual specificity tyrosine phosphorylation regulated kinase 1, Dual specificity tyrosine-phosphorylation-regulated kinase 1A, Dual specificity tyrosine-phosphorylation-regulated kinase 2, E4ICD, EC 2.7.10.1, EC 2.7.10.2, EC 2.7.11.1, EC 2.7.12.1, EC 2.7.12.2, EGFR_HUMAN, EHK-2, EPH homology kinase 2, EPHA6_HUMAN, ERBB, ERBB1, ERBB2_HUMAN, ERBB3 protein, ERBB3_HUMAN, ERBB4 intracellular domain, ERBB4_HUMAN, EXIP, Eph Receptor A6, Ephrin type-A receptor 6, 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), Erb b2 receptor tyrosine kinase 2, Erb b2 receptor tyrosine kinase 3, ErbB-2 proto-oncogene, Errp, FL cytokine receptor, FLJ16629, FLJ21217, FLJ21365, FLJ40395, FLT3_HUMAN, FRK_HUMAN, FYN-related kinase, Fetal liver kinase 2, Flk 2, Fms related tyrosine kinase 3, Fms-like tyrosine kinase 3, Frk fyn related kinase, G protein coupled receptor kinase 7, GAK protein, GAK_HUMAN, GASK, GPRK7, GSD9C, GTK, GTK, mouse, homolog of, Gastrointestinal associated kinase, Gastrointestinal associated tyrosine kinase, Glial growth factor receptor, Growth factor receptor tyrosine kinase type III, HCK IE, HER 2, HER 2/NEU, HER 3, HER 4, HER1, HIPK4_HUMAN, HP 86, Hek12, Herstatin, Homeodomain-interacting protein kinase 4, HsT17454, Human epidermal growth factor receptor 2, Human epidermal growth factor receptor 3, IMD22, IRAK, IRAK1-S, IRAK1_HUMAN, Il1rak, Interleukin-1 receptor-associated kinase 1, Intestine tyrosine kinase, JTK7, KC1E_HUMAN, LCCS2, LCK proto-oncogene, Src family tyrosine kinase, LCK_HUMAN, LSK, Lck p56, Leukocyte C-terminal Src kinase, Ly-72, Lymphocyte cell-specific protein-tyrosine kinase, Lymphocyte specific protein tyrosine kinase, MAP kinase 14, MAP kinase MXI2, MAP kinase interacting kinase 1, MAP kinase interacting serine threonine kinase, MAP kinase interacting serine threonine kinase 2, MAP kinase interacting serine threonine protein kinase 2, MAP kinase interacting serine/threonine kinase 1, MAP kinase kinase 5, MAP kinase kinase MEK5b, MAP kinase p38 alpha, MAP kinase signal-integrating kinase 1, MAP kinase signal-integrating kinase 2, MAP kinase-activated protein kinase 2, MAP kinase-interacting serine/threonine-protein kinase 1, MAP kinase-interacting serine/threonine-protein kinase 2, MAP2K5, MAPK 14, MAPK interacting kinase 2, MAPK signal integrating kinase 1, MAPK signal integrating kinase 2, MAPK-activated protein kinase 2, MAPK/ERK kinase 5, MAPK2_HUMAN, MAPKAP kinase 2, MAPKAPK-2, MAPKK 5, MAX-interacting protein 2, MDA BF 1, MGC 10398, MGC 10442, MGC138404, MGC88033, MGC99654, MITOGEN-ACTIVATED PROTEIN KINASE-INTERACTING SERINE/THREONINE KINASE 1, MK14_HUMAN, MKK5, MKNK1_HUMAN, MKNK2_HUMAN, MLN 19, MNB, MNB protein kinase, MNB protein kinase, Serine/threonine-specific, MNB/DYRK protein kinase, MNBH, MODY 11, MP2K5_HUMAN, MRD7, Membrane associated protein tyrosine kinase, Mer4, Metastatic lymph node gene 19 protein, Minibrain (Drosophila) homolog, Minibrain homolog, Minibrain, Drosophila, homolog of, Mitogen activated protein kinase activated protein kinase 2, Mitogen activated protein kinase interacting serine threonine kinase 2, Mitogen-activated protein kinase 14, Mitogen-activated protein kinase p38 alpha, Mnb protein kinase homolog hp86, Mxi 2, NEU, NEU proto oncogene, NGL, NISBD2, Neuro/glioblastoma derived oncogene homolog, Neuroblastoma/glioblastoma derived oncogene homolog, Nuclear tyrosine protein kinase RAK, OTTHUMP00000026014, OTTHUMP00000026015, OTTHUMP00000026020, OTTHUMP0000004234, OTTHUMP00000109090, OTTHUMP00000109091, OTTHUMP00000109094, OTTHUMP00000174799, OTTHUMP00000180621, Oncogen ERBB, Oncogene ERBB4, Oncogene lck, P150, P38, PHK gamma LT, PHK gamma T, PHK-gamma-M, PHKG1_HUMAN, PHKIN01, PIG61, PRKM14, PRKM15, PRKMK5, PSK C3, PTK5, PTK5 protein tyrosine kinase 5, Pelle, Pelle homolog, Pelle-like protein kinase, Phkg, Phosphorylase b kinase gamma catalytic chain, Phosphorylase b kinase gamma catalytic chain skeletal muscle/heart isoform, Phosphorylase b kinase gamma catalytic chain testis/liver isoform, Phosphorylase b kinase gamma catalytic chain, liver/testis isoform, Phosphorylase kinase catalytic subunit gamma 2, Phosphorylase kinase gamma subunit 2, Phosphorylase kinase subunit gamma 2, Phosphorylase kinase subunit gamma-1, Phosphorylase kinase, gamma 2 (testis), Phosphorylase kinase, gamma 2 (testis/liver), Phosphorylase kinase, muscle, gamma-1, Plpk, Protein YT16, Protein kinase minibrain homolog, Protein kinase, mitogen-activated, kinase 5, Protein-tyrosine kinase 5, Proto oncogene tyrosine protein kinase ABL1, Proto oncogene tyrosine protein kinase LCK, Proto-oncogene Lck, Proto-oncogene Neu, Proto-oncogene c-Abl, Proto-oncogene c-ErbB-1, Proto-oncogene c-ErbB-2, Proto-oncogene-like protein c-ErbB-3, Proto-oncogene-like protein c-ErbB-4, Putative map kinase interacting kinase, RAK, RK, Receptor protein tyrosine kinase erbB 4 precursor, Receptor type tyrosine protein kinase FLT3, Receptor tyrosine protein kinase erbB 4, Receptor tyrosine-protein kinase ErbB-1, Receptor tyrosine-protein kinase erbB-2, Receptor tyrosine-protein kinase erbB-3, SA7, SAPK2A, SAPKK5, SKK5, STK-1, Serine/threonine kinase MNB, Serine/threonine protein kinase PHKG2, Serine/threonine-protein kinase PHKG1, Species antigen 7, Stem cell tyrosine kinase 1, Stress-activated protein kinase 2a, T cell-specific protein-tyrosine kinase, T lymphocyte specific protein tyrosine kinase p56lck, TKR1, Tyrosine kinase B lymphocyte specific, Tyrosine kinase-type cell surface receptor HER2, Tyrosine kinase-type cell surface receptor HER3, Tyrosine kinase-type cell surface receptor HER4, Tyrosine protein kinase, Tyrosine-protein kinase ABL1, Tyrosine-protein kinase BLK, Tyrosine-protein kinase FRK, Tyrosine-protein kinase Lck, Tyrosine-protein kinase receptor FLT3, Urogastrone, V erb b2 avian erythroblastic leukemia viral oncogene homolog 2, V erb b2 avian erythroblastic leukemia viral oncogene homolog 2 (neuro/glioblastoma derived oncogene homolog), V erb b2 avian erythroblastic leukemia viral oncogene homolog 3, V erb b2 avian erythroblastic leukemia viral oncoprotein 2, V erb b2 erythroblastic leukemia viral oncogene homolog 2, neuro/glioblastoma derived oncogene homolog, V erb b2 erythroblastic leukemia viral oncogene homolog 2, neuro/glioblastoma derived oncogene homolog (avian), V-ERB-B2 avian erythroblastic leukemia viral oncogene homolog 4, VERBB2, Verb b2 erythroblastic leukemia viral oncogene homolog 2, neuro/glioblastoma derived-oncogene homolog, Verba avian erythroblastic leukemia viral oncogene homolog like 4, Wa5, YT 16, bcr/abl, c ABL, c abl oncogene 1 non receptor tyrosine kinase, c abl oncogene 1 receptor tyrosine kinase, c erbB 3, ephrin receptor EphA6, epsilon isoform, erb-b2 receptor tyrosine kinase 1, erbB3 S, hMNB, human epidermal growth factor receptor 4, kinase CK1 epsilon, mENA, mPLK, mitogen-activated protein kinase kinase 5, p180 ErbB3, p180erbB4, p185erbB2, p38 ALPHA, p38 MAP kinase, p38 MAPK, p38 mitogen activated protein kinase, p38alpha Exip, p45 sErbB3, p55-BLK, p56(LSTRA) protein tyrosine kinase, p56-LCK, p85 sErbB3, phosphorylase b kinase gamma catalytic chain, skeletal muscle isoform, phosphorylase kinase gamma, phosphorylase kinase, gamma 1 (muscle), pp58 lck, proto-oncogene-like protein c ErbB 3, s80HER4, skeletal muscle/heart isoform, v abl, v abl Abelson murine leukemia viral oncogene homolog 1, v erb a avian erythroblastic leukemia viral oncogene homolog like 4, v erb a erythroblastic leukemia viral oncogene homolog 4, v erb b2 erythroblastic leukemia viral oncogene homolog 3, v erb b2 erythroblastic leukemia viral oncogene homolog 3 (avian), v-erb-a erythroblastic leukemia viral oncogene homolog 4 (avian), v-erb-b Avian erythroblastic leukemia viral oncogen homolog, wa2
MW 485.9 Da, Purity >98%. Potent, irreversible Her2/ErbB 2 and EGFR kinase inhibitor (IC50 values are 0.5, 0.4, 10 and 14 nM for EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 respectively). Shows antitumor effects in vivo. Orally active.
850140-72-6
> 98%
Powder
485.9 Da
C24H25ClFN5O3
10184653
Synthetic
Soluble in ethanol to 25 mM. Soluble in DMSO to 100 mM.
Afatinib
Potent, irreversible Her2/ErbB 2 and EGFR kinase inhibitor (IC50 values are 0.5, 0.4, 10 and 14 nM for EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 respectively). Shows antitumor effects in vivo. Orally active.
CN(C)CC=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OC4CCOC4
CN(C)C/C=C/C(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)O[C@H]4CCOC4
InChI=1S/C24H25ClFN5O3/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29)/b4-3+/t16-/m0/s1
ULXXDDBFHOBEHA-CWDCEQMOSA-N
(E)-N-[4-(3-chloro-4-fluoroanilino)-7-[(3S)-oxolan-3-yl]oxyquinazolin-6-yl]-4-(dimethylamino)but-2-enamide
Ambient - Can Ship with Ice
-20°C
-20°C
Store under desiccating conditions, The product can be stored for up to 12 months
This supplementary information is collated from multiple sources and compiled automatically.
IRAK-1 p38 BLK FRK MK2 ErbB3/HER3 ErbB2/HER2 EGFR Lck ErbB4/HER4 ABL1 CK1 epsilon Eph receptor A6 DYRK1A Flt3/CD135 MEK5 GAK PHKG2 MNK1 DYRK2 PHKG1 MNK2 and HIPK4 are proteins with diverse roles in cellular processes. These proteins often referred by alternate names such as EGFR (HER1) and ErbB2 (HER2) vary in molecular weight and structure. For instance afatinib is a molecule targeting EGFR with precise mass properties. Expression of these proteins is observed in various tissues and cell types reflecting their significance in cellular function.
Many of these proteins like EGFR and HER2 function as part of larger receptor complexes involved in signal transduction. They play important roles in cell proliferation differentiation and survival. For example HER2 is an important member of the ErbB family receptor complex contributing to signal amplification. Proteins like MK2 interact with p38 to mediate cellular responses to external stress factors. Expression patterns of these proteins affect cellular behavior significantly.
These proteins partake in important signaling pathways such as the MAPK/ERK and PI3K/AKT pathways. EGFR and HER2 signal through these pathways influencing cell growth and survival. Their interactions with other proteins like PI3K allow for cross-talk between signaling pathways. These pathways are essential for cellular response to growth factors and stress signals thereby modulating cell fate decisions.
Aberrant function or expression of these proteins often relates to cancer and inflammatory diseases. Overexpression of EGFR and HER2 is commonly associated with breast and lung cancer as they drive uncontrolled cell proliferation. ABL1 is linked to chronic myeloid leukemia through its fusion with the BCR protein. Therapeutic agents like afatinib and its analogs target these proteins to manage and treat such diseases by inhibiting their activity and altering disease progression.
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2D chemical structure image of ab142018, Afatinib (BIBW 2992), Her2/ErbB 2 and EGFR kinase inhibitor
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