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Chemical Structure : NX-2127
CAS No.: 2416131-46-7
Catalog No.: PC-20560Not For Human Use, Lab Use Only.
NX-2127 (NX2127) is a hetero-bifunctional, orally active PROTAC that induces the degradation of BTK and IKZF3 ubiquitination and proteasomal degradation in cells through recruitment of cereblon (CRBN).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $258 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $598 | In stock | |
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| 100 mg | Get quote |
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NX-2127 (NX2127) is a hetero-bifunctional, orally active PROTAC that induces the degradation of BTK and IKZF3 ubiquitination and proteasomal degradation in cells through recruitment of cereblon (CRBN).
NX-2127 degrades BTK in multiple B cell lymphoma lines with DC50 values in the range of 1-13 nM.
NX-2127 displays efficient cellular degradation yet binds to WT and mutant BTK with affinities that render covalent and noncovalent BTK inhibitors ineffective.
NX-2127 drives cellular ternary complex formation between BTK and CRBN by inducing positive cooperativity in both WT and acquired resistance mutant settings.
NX-2127 induces potent degradation of C481S, T474I, V416L, and L528W-mutant BTK and suppresses activation marker expression on cells harboring these mutations.
NX-2127 demonstrates oral bioavailability across pre-clinical species and shows robust tumor growth inhibition in WT and mutant mouse models of lymphoma upon once daily PO dosing.
| M.Wt | 719.85 | |
| Formula | C39H45N9O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
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)- |
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1. Jeffrey T. Mihalic, et al. Cancer Res (2023) 83 (7_Supplement): 3423.
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