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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
7 Results for "
T474I
" in MedChemExpress (MCE) Product Catalog:
Products (7)
7 Results for "T474I" in MCE Product Catalog:
12
Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research .
NRX-0492 is an orally active BTK PROTAC degrader, with a binding IC50 of 1.2 nM for both wild-type BTK and BTK T474I, and 2.7 nM for BTK C481S, and exhibits cellular DC50 values of 0.1 nM and 0.2 nM against wild-type BTK and BTK C481S, respectively. NRX-0492 catalyzes the ubiquitination and proteasomal degradation of wild-type and drug-resistant mutant BTK by recruiting the CRBN E3 ubiquitin ligase complex. NRX-0492 inhibits the BCR signaling pathway and its downstream NF-κB/MYC transcriptional program, achieves rapid and sustained degradation in primary CLL cells, and exhibits extremely low cytotoxicity. NRX-0492 degrades BTK, inhibits tumor cell proliferation and activation, and significantly suppresses tumor growth in xenograft models. NRX-0492 can be used in research related to chronic lymphocytic leukemia and diffuse large B-cell lymphoma .
Cat. No.: HY-174850
CAS No.: 2941611-57-8
CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27 nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia .
Cat. No.: HY-124153
CAS No.: 1433820-83-7
Target:
Research Areas:
GNE-431 is a potent, selective and noncovalent “pan-BTK” inhibitor against C481R, T474I and T474Ms mutants. GNE-431 shows potency against wild-type BTK (IC50= 3.2 nM) and potency against C481S mutant (IC50= 2.5 nM). GNE-431 is proming for rasearch of haematological disorders and autoimmune diseases .
Cat. No.: HY-19834R
CAS No.: 1434048-34-6
Synonyms: GDC-0853 (Standard)
Target:
Research Areas:
Fenebrutinib (Standard) is the analytical standard of Fenebrutinib (HY-19834). This product is intended for research and analytical applications. Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine Kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research .
Cat. No.: HY-P704029
Purity: ≥ 85%, as determined by reducing SDS-PAGE.
Synonyms: BTK; Tyrosine-Protein Kinase BTK Isoform (Lacking Exon 13 To 17); Prev. AGMX1; Tyrosine-Protein Kinase BTK Isoform (Lacking Exon 14); Prev. IMD1; Tyrosine-Protein Kinase BTK Isoform 52; ATK; Tyrosine-Protein Kinase BTK Isoform 51; PSCTK1; Tyrosine-Protein
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-P705751
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: BTK; Tyrosine-Protein Kinase BTK Isoform (Lacking Exon 13 To 17); Prev. AGMX1; Tyrosine-Protein Kinase BTK Isoform (Lacking Exon 14); Prev. IMD1; Tyrosine-Protein Kinase BTK Isoform 52; ATK; Tyrosine-Protein Kinase BTK Isoform 51; PSCTK1; Tyrosine-Protein
Species:
Human
Source:
sf9 insect cells
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
