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Chemical Structure : GMB-475
CAS No.: 2490599-18-1
Catalog No.: PC-20007Not For Human Use, Lab Use Only.
GMB-475 (GMB475) is an allosteric BCR-ABL1 PROTAC with DC50 of 340 nM, degrades the BCR-ABL1 through the ubiquitin-proteasome pathway.
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|---|---|---|---|
| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
| 50 mg | $528 | In stock | |
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GMB-475 (GMB475) is an allosteric BCR-ABL1 PROTAC with DC50 of 340 nM, degrades the BCR-ABL1 through the ubiquitin-proteasome pathway.
GMB-475 induced the degradation of BCR-ABL1 and c-ABL1 in the context of both K562 and Ba/F3 cells with concomitant inhibition of downstream signaling via the STAT5 pathway, in a dose- and time-dependent fashion.
GMB-475 was capable of inhibiting cell proliferation with IC50 of 1 uM.
GMB-475-mediated degradation enhances efficacy of ATP-competitive TKIs and retains potency against imatinib resistant point mutations (T351I, IC50=1.98 uM; G250E, IC50=0.37 uM).
GMB-475 reduced viability and increased apoptosis in primary CML CD34+ cells, with no effect on healthy CD34+ cells at identical concentrations.
GMB-475 degraded BCR-ABL1 and reduced cell viability in primary CML stem cells.
| M.Wt | 861.94 | |
| Formula | C43H46F3N7O7S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(2S,4R)-1-((S)-3,3-dimethyl-2-(2-(2-(4-(6-((4-(trifluoromethoxy)phenyl)amino)pyrimidin-4-yl)phenoxy)ethoxy)acetamido)butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide |
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1. Burslem GM, et al. Cancer Res. 2019 Sep 15;79(18):4744-4753.
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