ChemicalBook > CAS DataBase List > 2-Pyrazinecarboxamide, 3-[[4-[1-[[(3S)-1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-3-pyrrolidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-(1-piperidinyl)-

2-Pyrazinecarboxamide, 3-[[4-[1-[[(3S)-1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-3-pyrrolidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-(1-piperidinyl)-

Product Name: 2-Pyrazinecarboxamide, 3-[[4-[1-[[(3S)-1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-3-pyrrolidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-(1-piperidinyl)-
CAS No.: 2416131-46-7
Chemical Name: 2-Pyrazinecarboxamide, 3-[[4-[1-[[(3S)-1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-3-pyrrolidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-(1-piperidinyl)-
Synonyms: NX2127|||NX 2127;3-[[4-[1-[[(3S)-1-[2-(2,6-Dioxo-3-piperidyl)-1,3-dioxo-5-isoindolinyl]-3-pyrrolidinyl]methyl]-4-piperidyl]phenyl]amino]-5-(1-piperidyl)pyrazine-2-carboxamide;3-((4-(1-(((3S)-1-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)pyrrolidin-3-yl)methyl)piperidin-4-yl)phenyl)amino)-5-(piperidin-1-yl)pyrazine-2-carboxamide;3-((4-(1-(((3R)-1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)pyrrolidin-3-yl)methyl)piperidin-4-yl)phenyl)amino)-5-(piperidin-1-yl)pyrazine-2-carboxamide;2-Pyrazinecarboxamide, 3-[[4-[1-[[(3S)-1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-3-pyrrolidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-(1-piperidinyl)-
CBNumber: CB913027822
Molecular Formula: C39H45N9O5
Formula Weight: 719.83
MOL File: 2416131-46-7.mol

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2-Pyrazinecarboxamide, 3-[[4-[1-[[(3S)-1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-3-pyrrolidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-(1-piperidinyl)- Property

Boiling point:: 949.0±65.0 °C(Predicted)
Density: 1.371±0.06 g/cm3(Predicted)
solubility: DMSO: Sparingly soluble: 1-10 mg/ml
pka: 10.83±0.40(Predicted)
form: Solid
color: Light yellow to yellow
InChIKey: XLWJWCMQMBVNSG-ACXKHFGCSA-N
SMILES: C1(C(N)=O)=NC=C(N2CCCCC2)N=C1NC1=CC=C(C2CCN(C[C@@H]3CCN(C4C=CC5=C(C=4)C(=O)N(C4CCC(=O)NC4=O)C5=O)C3)CC2)C=C1

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Hazard and Precautionary Statements (GHS)

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2-Pyrazinecarboxamide, 3-[[4-[1-[[(3S)-1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-3-pyrrolidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-(1-piperidinyl)- Chemical Properties,Usage,Production

Uses

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]. NX-2127 is composed of PROTAC target protein ligand (red part) BTK ligand 10 (HY-168302), E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383) and PROTAC Linker (black part) (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303). Among which, the conjugate of E3 ubiquitin ligase ligand + Linker compose of Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304).

in vivo

NX-2127 (1 mg/kg; po; once daily for 14 days) demonstrates potent degradation of BTK in cynomolgus monkeys in vivo^[1].
NX-2127 (po) leads to dose-proportional exposure in plasma and BTK degradation to <10% of baseline levels in circulating and splenic B cells^[1].
NX-2127 results in superior tumor growth inhibition (TGI) in both WT TMD8 and C481S mutant xenograft models in mouse^[1].

References

[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.
[3] DANIEL W. ROBBINS, FREDERICK COHEN* Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton’s Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B Cell Malignancies[J]. Journal of Medicinal Chemistry, 2024, 67 4: 2321-2336. DOI: 10.1021/acs.jmedchem.3c01007
[4] SKYE MONTOYA. Kinase-impaired BTK mutations are susceptible to clinical-stage BTK and IKZF1/3 degrader NX-2127[J]. Science, 2024, 383 6682. DOI: 10.1126/science.adi5798

2-Pyrazinecarboxamide, 3-[[4-[1-[[(3S)-1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-3-pyrrolidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-(1-piperidinyl)- Preparation Products And Raw materials

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2416131-46-7, 2-Pyrazinecarboxamide, 3-[[4-[1-[[(3S)-1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-3-pyrrolidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-(1-piperidinyl)-Related Search:

2-Pyrazinecarboxamide, 3-[[4-[1-[[(3S)-1-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-3-pyrrolidinyl]methyl]-4-piperidinyl]phenyl]amino]-5-(1-piperidinyl)-

3-((4-(1-(((3R)-1-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)pyrrolidin-3-yl)methyl)piperidin-4-yl)phenyl)amino)-5-(piperidin-1-yl)pyrazine-2-carboxamide

3-[[4-[1-[[(3S)-1-[2-(2,6-Dioxo-3-piperidyl)-1,3-dioxo-5-isoindolinyl]-3-pyrrolidinyl]methyl]-4-piperidyl]phenyl]amino]-5-(1-piperidyl)pyrazine-2-carboxamide

NX2127|||NX 2127

3-((4-(1-(((3S)-1-(2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)pyrrolidin-3-yl)methyl)piperidin-4-yl)phenyl)amino)-5-(piperidin-1-yl)pyrazine-2-carboxamide

2416131-46-7

C39H45N9O5