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Chemical Structure : BLU-945
CAS No.: 2660250-10-0
Catalog No.: PC-72903Not For Human Use, Lab Use Only.
BLU-945 (ZL-2313, BLU945, BLU 945) is a potent, mutant-selective inhibitor of EGFR T790M/C797S and EGFR+/T790M mutations (IC50<1 nM).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $228 | In stock | |
| 10 mg | $358 | In stock | |
| 25 mg | $558 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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BLU-945 (ZL-2313, BLU945, BLU 945) is a potent, mutant-selective inhibitor of EGFR T790M/C797S and EGFR+/T790M mutations (IC50<1 nM).
BLU-945 inhibits EGFRex19del/T790M/C797S, EGFRL858R/T790M/C797S, EGFRex19del/T790M, and EGFRL858R/T790M mutants with sub-nanomolar IC50 values in an enzyme assay, with >1000-fold selectivity over EGFR WT.
BLU-945 achieves potent EGFR pathway inhibition in NCI-H1975 EGFRL858R/T790M, Ba/F3 EGFRL858R/T790M/C797S, and Ba/F3 EGFRex19del/T790M/C797S cell lines and a large window relative to EGFRWT inhibition.
Oral administration of BLU-945 to tumor-bearing mice demonstrated potent EGFR pathway inhibition and anti-tumor activity at well-tolerated doses in the subcutaneous NCI-H1975 CDX model, and osimertinib-resistant CDX and PDX models.
| M.Wt | 556.701 | |
| Formula | C28H37FN6O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-(2-((3S,4R)-3-fluoro-4-methoxypiperidin-1-yl)pyrimidin-4-yl)-5-isopropyl-8-((2R,3S)-2-methyl-3-((methylsulfonyl)methyl)azetidin-1-yl)isoquinolin-3-amine |
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1. Sun Min Lim, et al. Cancer Res (2021) 81 (13_Supplement): 1467.
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