AZD5104 free base · Synonyms: AZD-5104

AZ-5104 is an active, demethylated metabolite of AZD 9291.

For research use only. Not for human or veterinary use.

Target EGFR

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

AZD5104 structure

CAS No.: 1421373-98-9

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
500 mg	USD 497.00	BP-02312-500mg	In stock	Get quote
1 g	USD 820.00	BP-02312-1g	In stock	Get quote
2 g	USD 1,315.00	BP-02312-2g	In stock	Get quote
3 g	USD 1,580.00	BP-02312-3g	In stock	Get quote
5 g	USD 2,100.00	BP-02312-5g	In stock	Get quote
10 g	USD 3,370.00	BP-02312-10g	In stock	Get quote

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Description

AZ-5104 is an active, demethylated metabolite of AZD 9291. AZ-5104 is an EGFR inhibitor with IC50s of 1, 6, 1, 25 and 7 nM for EGFR L858R/T790M, EGFR L858R, EGFR L861Q, EGFR and ErbB4, respectively.

Biological activity

In Vitro AZ-5104 inhibits EGFR phosphorylation with IC50s of 2, 1, 2, 53, and 33 nM in H1975 (EGFRL858R/T790M), PC-9VanR (EGFRExon 19 deletion/T790M), PC-9 (EGFRExon 19 deletion), H2073 (WT), and LOVO (WT), respectively. AZ5104 exhibits a reduced selectivity margin against wild-type EGFR when compared to AZD9291. AZ5104 display minimal off-target activity against other non-HER family kinases, but has the potential to target both HER2 and HER4 kinase activity. In Vivo The metabolite, AZ5104 (5 mg/kg/day), is effective in shrinking tumors in both C/L858R and C/L+T mice.

Identifiers

SMILES: COC1=C(NC2=NC(=CC=N2)C2=CNC3=CC=CC=C23)C=C(NC(=O)C=C)C(=C1)N(C)CCN(C)C
InChIKey: IQNVEOMHJHBNHC-UHFFFAOYSA-N

Specifications

MW (average): 485.5807
Formula: C₂₇H₃₁N₇O₂
CAS No.: 1421373-98-9
Physical state: Solid
Color: white to off-white
Shipping: 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: Powder 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Finlay MR, et al. Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor. J Med Chem. 2014 Oct 23;57(20):8249-67.

Same target

Search EGFR

Same research area

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