Osimertinib

SKU: orb1305406

Description

Osimertinib (AZD-9291) is an oral, irreversible third-generation EGFR inhibitor designed to target the T790M resistance mutation in non-small cell lung cancer (NSCLC). It is widely used in preclinical research, demonstrating potent antitumor activity in both in vitro cell assays and in vivo xenograft models of EGFR-mutant NSCLC.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	1421373-65-0
MW	499.61
Purity	>99.99% (May vary between batches)
Formula	C₂₈H₃₃N₇O₂
SMILES	CN1C=C(C=2C1=CC=CC2)C3=NC(NC4=C(OC)C=C(N(CCN(C)C)C)C(NC(C=C)=O)=C4)=NC=C3
Target	EGFR
Solubility	DMSO:120 mg/mL (240.19 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:9.2 mg/mL (18.41 mM);Ethanol:22 mg/mL (44.03 mM)

Bioactivity

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Target IC50	MNK2:48.6 nM\|EGFR (WT):493.8 nM\|MNK1:324 nM\|H1975 cells:1.78 μM\|PC9 cells:0.66 μM\|EGFR (exon 19 deletion):12.92 nM\|EGFR (L858R/T790M):11.44 nM
In Vivo	In mutant EGFR cell lines, AZD9291 effectively inhibits cell proliferation.
In Vitro	In the EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models, oral administration of AZD9291 (5 mg/kg) effectively inhibits AKT and ERK signaling pathways as well as EGFR phosphorylation in tumors, leading to tumor regression. Read more...
Cell Research	AZD-9291 is dissolved in DMSO and stored, and then diluted with appropriate medium before use. PC-9 cells are seeded into T75 flasks (5×105 cells/flask) in RPMI growth media and incubated at 37°C, 5% CO2. The following day the media is replaced with media supplemented with a concentration of EGFR inhibitor equal to the EC50 concentration predetermined in PC-9 cells. Media changes are carried out every 2-3 days and resistant clones allowed to grow to 80% confluency prior to the cells being trypsinised and reseeded at the original seeding density in media containing twice the concentration of EGFR inhibitor. Dose escalations are continued until a final concentration of 1.5 μM Gefitinib, 1.5 μM Afatinib, 1.5 μM WZ4002 or 160 nM AZD-9291 are achieved. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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PC-9, Osimertinib, Inhibitor, inhibit, Mereletinib, HER1, H1975, EGFR, EGFR (Exon 19 deletion), EGFR (L858R/T790M), Epidermal growth factor receptor, ErbB-1, AZD 9291, AZD9291, AZD-9291, Ba/F3 cells, cancer, tumor xenograft model

Quality Guarantee

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Compound Identifiers

PubChem CID

71496458 ↗

Key Properties

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No computed properties available.

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Osimertinib (orb1305406)

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MW:	345.4
Formula:	C₂₀H₁₉N₅O

CAS Number:	2889316-21-4
MW:	570.08
Formula:	C₃₂H₃₂ClN₅O₃

MW:	548.84
Formula:	C₂₄H₂₈BrClN₅OP

Purity:	99.65%
CAS Number:	2309762-40-9
MW:	522.04
Formula:	C₂₇H₃₂ClN₇O₂

Purity:	99.75%
CAS Number:	1421373-99-0
MW:	485.58
Formula:	C₂₇H₃₁N₇O₂

Osimertinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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