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AZ5104

Cat. No. M4977
AZ5104 Structure
Size Price Availability Quantity
10mM*1mL USD 80  USD80 In stock
10mg USD 100  USD100 In stock
50mg USD 300  USD300 In stock
100mg USD 500  USD500 In stock
200mg USD 750  USD750 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In both C/L858R and C/L+T mice, AZ5104 (5 mg/kg/d, p.o.) induces significant and sustained tumor regression.AZ-5104 is an active, demethylated metabolite of AZD-9291. AZ-5104 displays similar overall activity profile with AZD-9291, but is more potent against mutant EGFR forms, while hitting the wild-type EGFR form at a lower concentration thus demonstrating a smaller selectivity margin compared with the parent.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 485.58
Formula C27H31N7O2
CAS Number 1421373-98-9
Purity >98%
Solubility 10 mM in DMSO
Storage at -20°C
References

[1] Cross DA,et.al. Cancer Discov AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.

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