NX-2127

CAT: 0804-HY-153220-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-153220-01Size:5 mg
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Description
NX-2127 (Compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk) . NX-2127 inhibits proliferation of BTKC481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997) . NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells[1][2]. (Pink: BTK ligand 10 (HY-168302) ; Black: (R) -4- (1- (Pyrrolidin-3-ylmethyl) piperidin-4-yl) aniline (HY-168348) ; Blue: Thalidomide 5-fluoride (HY-W087383)
CAS Number
[2416131-46-7]
UNSPSC
12352005
Target
Btk; PROTACs
Type
Reference compound
Related Pathways
PROTAC; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/nx-2127.html
Purity
99.72
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C1C2=CC(N3C[C@H](CN4CCC(C5=CC=C(C=C5)NC6=C(N=CC(N7CCCCC7)=N6)C(N)=O)CC4)CC3)=CC=C2C(N1C8C(NC(CC8)=O)=O)=O
Molecular Formula
C39H45N9O5
Molecular Weight
719.83
References & Citations
[1]Robbins D W, et al. Nx-2127, a degrader of BTK and IMiD neosubstrates, for the treatment of B-cell malignancies. Blood, 2020, 136: 34. |[2]Mato A, et al. A first-in-human phase 1 trial of NX-2127, a first-in-class oral BTK degrader with IMiD-like activity, in patients with relapsed and refractory B-cell malignancies. 2022.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, protect from light)
Scientific Category
Reference compound1
Clinical Information
Phase 1

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