WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H130490
CAS#: TBD
Description: EGFRL858R/T790M inhibitor 28f is a selective EGFR L858R/T790M inhibitor, exhibiting strong inhibitory activity against EGFR L858R/T790M (IC50 = 3.5 nM) and greater than 368-fold selectivity over EGFR WT (IC50 = 1290 nM), a 6.7-fold improvement over osimertinib, effectively inhibiting downstream signaling pathways and inducing apoptosis in mutant cells.
Hodoodo Cat#: H130490
Name: EGFRL858R/T790M inhibitor 28f
CAS#: TBD
Chemical Formula: C28H28FN7O
Exact Mass: 497.23
Molecular Weight: 497.578
Elemental Analysis: C, 67.59; H, 5.67; F, 3.82; N, 19.71; O, 3.22
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Synonym: EGFRL858R/ T790M inhibitor 28f, EGFRL858R / T790M inhibitor 28f, EGFRL858R/T790M-28f, EGFRL858R/T790M 28f
IUPAC/Chemical Name: N-(3-((6-Fluoro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)quinazolin-4-yl)amino)phenyl)acrylamide
InChi Key: KDWNVZXLHSMELQ-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H28FN7O/c1-3-26(37)30-21-5-4-6-22(18-21)31-27-24-17-19(29)7-12-25(24)33-28(34-27)32-20-8-10-23(11-9-20)36-15-13-35(2)14-16-36/h3-12,17-18H,1,13-16H2,2H3,(H,30,37)(H2,31,32,33,34)
SMILES Code: C=CC(NC1=CC=CC(NC2=C3C=C(F)C=CC3=NC(NC4=CC=C(N5CCN(C)CC5)C=C4)=N2)=C1)=O
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 497.58 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1. Pei J, Wang G, Wang A, Wu C, Pan X, Shuai W, Bu F, Zhu Y, Wang Y, Ouyang L, Li W. Design, Synthesis, and Antitumor Activity of Potent and Selective EGFR L858R/T790M Inhibitors and Identification of a Combination Therapy to Overcome Acquired Resistance in Models of Non-small-cell Lung Cancer. J Med Chem. 2023 Apr 27;66(8):5719-5752. doi: 10.1021/acs.jmedchem.3c00027. Epub 2023 Apr 12. PMID: 37042119.