Anticancer Azd-9291 (Mesylate) Osimertinib for Lung Cancer CAS 1421373-65-0

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Model NO.: Pharmacopoeial grade
CAS: 1421373-65-0
Trademark: Biocar
Transport Package: Aluminum Foil Bag or as Required
Specification: SGS/ CTI/ ITS
Origin: Hubei, China
HS Code: 8676530000
Model NO.: Pharmacopoeial grade
CAS: 1421373-65-0
Trademark: Biocar
Transport Package: Aluminum Foil Bag or as Required
Specification: SGS/ CTI/ ITS
Origin: Hubei, China
HS Code: 8676530000
Product Description
Product Name    AZD-9291 / Osimertinib 
 
CAS    1421373-65-0
 
MF    C28H33N7O2
 
MW    499.61
 
Purity    99%
 
Appearance    White Powder
 
Grade    Pharma Grade
 

Application

AZD9291 administered once daily orally at 5 mg/kg caused profound regression of tumours across EGFRm+ (PC9; 178% inhibition) and EGFRm+/T790M (H1975; 119% inhibition) tumour models in vivo,
after 14 days dosing. Furthermore 5 mg/kg AZD9291 was sufficient to cause significant shrinkage of EGFRm+ and EGFRm+/T790M transgenic mouse lung tumours. Tumour  inhibition was associated with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK. Chronic long-term treatment of PC9 and H1975 xenograft tumours with AZD9291 led to a complete and sustained macroscopic response, with no visible tumours after 40 days dosing, and being maintained beyond 100 days. Furthermore, pre-clinical data also indicates that AZD9291 could target tumours that have acquired resistance to the more recently identified HER2-amplification mechanism, thus potentially extending its benefit in TKI resistant patients.


Main Function

AZD 9291 is an irreversible inhibitor of epidermal  receptor (EGFR) sensitizing and T790M
resistance mutations (IC50s = 15-17 nM) while sparing the wild-type form of the receptor (IC50 = 480 nM). It binds the related 1R and hERG receptors with significantly reduced potency (IC50s = 2.9 and 16.2 μM, respectively). AZD 9291 has been shown to inhibit tumor  in a xenograft mouse model at oral doses of 5-10 mg/kg and has been tested clinically in patients with advanced EGFR mutant non-small-cell lung cancer.


Usage

Cell lines.Human lung cancer cells with EGFR-mutations or wild type EGFR stable expression Product Description
Product Name    AZD-9291 / Osimertinib 
 
CAS    1421373-65-0
 
MF    C28H33N7O2
 
MW    499.61
 
Purity    99%
 
Appearance    White Powder
 
Grade    Pharma Grade
 

Application

AZD9291 administered once daily orally at 5 mg/kg caused profound regression of tumours across EGFRm+ (PC9; 178% inhibition) and EGFRm+/T790M (H1975; 119% inhibition) tumour models in vivo,
after 14 days dosing. Furthermore 5 mg/kg AZD9291 was sufficient to cause significant shrinkage of EGFRm+ and EGFRm+/T790M transgenic mouse lung tumours. Tumour  inhibition was associated with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK. Chronic long-term treatment of PC9 and H1975 xenograft tumours with AZD9291 led to a complete and sustained macroscopic response, with no visible tumours after 40 days dosing, and being maintained beyond 100 days. Furthermore, pre-clinical data also indicates that AZD9291 could target tumours that have acquired resistance to the more recently identified HER2-amplification mechanism, thus potentially extending its benefit in TKI resistant patients.


Main Function

AZD 9291 is an irreversible inhibitor of epidermal  receptor (EGFR) sensitizing and T790M
resistance mutations (IC50s = 15-17 nM) while sparing the wild-type form of the receptor (IC50 = 480 nM). It binds the related 1R and hERG receptors with significantly reduced potency (IC50s = 2.9 and 16.2 μM, respectively). AZD 9291 has been shown to inhibit tumor  in a xenograft mouse model at oral doses of 5-10 mg/kg and has been tested clinically in patients with advanced EGFR mutant non-small-cell lung cancer.


Usage

Cell lines.Human lung cancer cells with EGFR-mutations or wild type EGFR stable expression