API Osimertinib CAS 1421373-66-1

Name

Osimertinib

CAS number

444731-52-6 (free base)

Description

Osimertinib is a third-generation, irreversible EGFR tyrosine kinase inhibitor (TKI) selective for both activating EGFR mutations (exon 19 deletion, L858R) and the T790M resistance mutation. In vitro, it inhibits EGFR phosphorylation in NSCLC cell lines harboring these mutations with IC₅₀ values of 0.5–2 nM, while sparing wild-type EGFR (IC₅₀ ~100 nM). It induces apoptosis and inhibits proliferation in T790M-positive cells at low nanomolar concentrations. In vivo, oral administration in xenograft mouse models bearing EGFR-mutant tumors (including T790M) leads to significant tumor regression at doses of 5–25 mg/kg/day, with near-complete inhibition of EGFR lation and downstream signaling (AKT, ERK) in tumors. Osimertinib shows superior brain penetration, reducing intracranial tumor growth in orthotopic models. Its potency against resistant EGFR mutations and favorable pharmacokinetics underlie its clinical efficacy in NSCLC patients with acquired T790M-mediated resistance.

Synonym

AZD9291; AZD 9291; AZD-9291; AZD-9291 freebase; Mereletinib; Osimertinib free base; trade name Tagrisso.

Related CAS #

1421373-65-0 (free base) 1421373-66-1 (mesylate)

Appearance

Solid powder

Quality Standard

USP, EP, BP, CP

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 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years).

Shelf Life

>2 years if stored properly

Sample package

Aluminium foil bag

Commercial package

Aluminium Tin, Fiber drum

Origin

China