NX-2127

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)

Product Specifications

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.