+86 137 2013 4139
+86 137 2013 4139
| CAS: | 2649400-34-8 | Cat No: | JKN03255 | Purity: | 98% |
Note: All products of the company are for scientific research only, and do not provide products and services for any individual
Product Description
| CAS | 2649400-34-8 | Cat No | JKN03255 | |
| Name | NX-5948 | |||
| Synonyms | NX-5948 | |||
| Smiles | CN1CCN(C1=O)[C@@H]2CCCN(C2)C3=CN=C(C(=N3)NC4=CC=C(C=C4)C5CCN(CC5)CC6CCN(CC6)C7=CN=C(C=C7)C(=O)N[C@H]8CCC(=O)NC8=O)C(=O)N | |||
| Chemical Name | 3-[4-[1-[[1-[6-[[(3S)-2,6-dioxopiperidin-3-yl]carbamoyl]pyridin-3-yl]piperidin-4-yl]methyl]piperidin-4-yl]anilino]-5-[(3R)-3-(3-methyl-2-oxoimidazolidin-1-yl)piperidin-1-yl]pyrazine-2-carboxamide | |||
| Formula | C42H54N12O5 | MWt | 807.0 | |
| Purity | 98% | Storage | Store at 4--8℃ | |
| Description | BTK Degrader NX-5948 is an orally bioavailable chimeric targeting molecule (CTM) and targeted degrader of Bruton's tyrosine kinase (BTK), with potential antineoplastic activity. NX-5948 is comprised of a cereblon (CRBN)-binding moiety conjugated, via a linker, to a BTK-binding moiety. Upon oral administration, BTK degrader NX-5948 targets and binds to BTK with its BTK-targeting moiety. Upon binding, the CRBN-binding moiety recruits CRBN, a component of the CRL4-CRBN E3 ubiquitin ligase complex. This catalyzes ubiquitination and proteasome-mediated degradation of BTK, and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B-cells that overexpress BTK. NX-5948 does not catalyze the degradation of CRBN neosubstrates and transcription factors Aiolos (IKZF3) and Ikaros (IKZF1), and does not possess immunomodulatory activity. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B-lymphocyte development, activation, signaling, proliferation and survival. CRBN, the substrate recognition component of the CRL4-CRBN E3 ubiquitin ligase complex, plays a key role in the ubiquitination of certain proteins. NX-5948 may overcome tumor resistance associated with BTK inhibitor-induced resistance mutations. In addition, NX-5948 is able to cross the blood-brain barrier (BBB) and thus potentially useful in the treatment of central nervous system (CNS) metastases. | |||
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