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AZD-9291

CAT: 0013-GTR19163263-02Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19163263-02Size:5 mg
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Description
A potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively; weak activity against wt EGFR (IC50=184 nM) ; inhibits signaling pathways and cellular growth in both EGFRm (+) and EGFRm (+) /T790M (+) mutant cell lines in vitro; exhibits tumor regression in EGFR-mutant tumor xenograft and transgenic models; orally active.Lung Cancer Approved (In Vitro) :Osimertinib (AZD9291) (0-10 μM; 72 hours) dramatically inhibits cell proliferation with IC50s of 41, 26, 41, and 31 nM, respectively.Osimertinib (0-10 μM; 72 hours) inhibits cell proliferation (Ba/F3 cells harboring a T790M mutation, exon 19del+T790M, or L858R+T790M) with IC50s of 6, 7, and 74 nM, respectively.Osimertinib (0-10 μM; 72 hours) inhibits Ba/F3 cells harboring EGFR exon 20 insertion mutations (IC50 ranging from 16 to 701 nM for A763_Y764insFQEA (FQEA), Y764_V765insHH (HH), A767_V769dupASV (ASV), and D770_N771insNPG (NPG) cells) .Osimertinib shows high levels of phenotype potency in both sensitizing-mutant (mean IC50 of 8 nM in PC-9) and T790M (mean IC50s of 11 and 40 nM in H1975 and PC-9VanR respectively) EGFR cell lines. Osimertinib has much less activity towards wild-type EGFR (mean IC50s of 650 and 461 nM in Calu3 and H2073 respectively) .Osimertinib (0.1 μM; 48 hours) induces apoptosis in Ba/F3 cells (apoptosis rates of 40.9% and 90% in EGFR exon 19del+T790M, EGFR L858R+T790M respectively) (In Vivo) :Osimertinib (0.1-25 mg/kg; p.o.; daily for 14 days) induces significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.
CAS Number
1421373-65-0
Product Name Alternative
Osimertinib | Mereletinib | AZD9291 | AZD 9291
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 30 mg/mL
Smiles
COC1=C (NC2=NC=CC (=N2) C2=CN (C) C3=CC=CC=C23) C=C (NC (=O) C=C) C (=C1) N (C) CCN (C) C
Molecular Formula
C28H33N7O2
Molecular Weight
499.6073
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
2-Propenamide, N-[2-[[2- (dimethylamino) ethyl]methylamino]-4-methoxy-5-[[4- (1-methyl-1H-indol-3-yl) -2-pyrimidinyl]amino]phenyl]-

Chemical Information

Osimertinib

Osimertinib is a member of the class of aminopyrimidines that is 4-(1-methylindol-3-yl)pyrimidin-2-amine in which one of the amino hydrogens is replaced by a 2-methoxy-4-[2-(dimethylamino)ethyl](methyl)amino-5-acrylamidophenyl group. Used (as the mesylate salt) for treatment of EGFR T790M mutation positive non-small cell lung cancer. It has a role as an antineoplastic agent and an epidermal growth factor receptor antagonist. It is a secondary carboxamide, a member of acrylamides, a member of indoles, a monomethoxybenzene, an aminopyrimidine, a substituted aniline, a secondary amino compound, a tertiary amino compound and a biaryl. It is a conjugate base of an osimertinib(1+).

CAS Number1421373-65-0
PubChem CID71496458
IUPAC NameN-[2-[2-(dimethylamino)ethyl-methylamino]-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide
Molecular FormulaC28H33N7O2
Molecular Weight499.6
XLogP3.7
Topological Polar Surface Area87.6
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count7
Rotatable Bond Count10
Heavy Atom Count37
Formal Charge0
Complexity752
SMILES
CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC
InChI
InChI=1S/C28H33N7O2/c1-7-27(36)30-22-16-23(26(37-6)17-25(22)34(4)15-14-33(2)3)32-28-29-13-12-21(31-28)20-18-35(5)24-11-9-8-10-19(20)24/h7-13,16-18H,1,14-15H2,2-6H3,(H,30,36)(H,29,31,32)
InChIKey
DUYJMQONPNNFPI-UHFFFAOYSA-N
Chemical Structure
2D Structure
2D structure of Osimertinib
CAS: 1421373-65-0
CID: 71496458
Formula: C28H33N7O2
MW: 499.6
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight499.6
XLogP33.7
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count7
Rotatable Bond Count10
Exact Mass499.26957332
Monoisotopic Mass499.26957332
Topological Polar Surface Area87.6 Ų
Heavy Atom Count37
Formal Charge0
Complexity752
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

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