1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR

EAI045 (Synonyms: EAI 045; EAI-045)

Cat. No.: HY-100213 Purity: 99.33%
Data Sheet SDS Handling Instructions

EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants.

For research use only. We do not sell to patients.
EAI045 Chemical Structure

EAI045 Chemical Structure

CAS No. : 1942114-09-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $77 In-stock
5 mg $70 In-stock
10 mg $90 In-stock
50 mg $260 In-stock
100 mg $450 In-stock
200 mg $750 In-stock
500 mg $1300 In-stock
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Description

EAI045 is an allosteric inhibitor that targets selected drug-resistant EGFR mutants. target: EGFR [1] In vitro: EAI045 potently inhibit EGFR Y1173 phosphorylation in H1975 cells. ( EC50: 2 nM ). [1] EAI045 represents a novel selective inhibitor that can overcome T790M and C797S resistance mutations. [2] In vivo: EAI045 in combination with cetuximab is effective in mouse models of lung cancer driven by EGFR(L858R/T790M) and by EGFR(L858R/T790M/C797S), a mutant that is resistant to all currently available EGFR TKIs. EAI045 revealed a maximal plasma concentration of 0.57 μM, a half-life of 2.15 h, and oral bioavailability of 26% after dosing at 20 mg/kg.[1] EAI045 markedly reduced tumor growth in a mouse model of L858R/T790M. [2]

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.6082 mL 13.0412 mL 26.0824 mL
5 mM 0.5216 mL 2.6082 mL 5.2165 mL
10 mM 0.2608 mL 1.3041 mL 2.6082 mL
References
M.Wt

383.4

Formula

C₁₉H₁₄FN₃O₃S

CAS No.

1942114-09-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 28 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.33%

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EAI045
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