Osimertinib(AZD9291 Tagrisso)

Molecular Weight (MW)	499.61
Formula	C28H33N7O2
CAS No.	1421373-65-0
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 99 mg/mL (198.12 mM)
Water: <1 mg/mL
Ethanol: 43 mg/mL (86.01 mM)
Solubility (In vivo)	1% DMSO+30% PEG 300+dd H2O: 30mg/mL
Synonyms	AZD-9291; AZD9291; AZD 9291; Osimertinib free base; Mereletinib; Trade name: Tagrisso Chemical Name: N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide InChi Key: DUYJMQONPNNFPI-UHFFFAOYSA-N InChi Code: 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) SMILES Code: C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O

Molecular Weight (MW)

499.61

Formula

C28H33N7O2

CAS No.

1421373-65-0

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 99 mg/mL (198.12 mM)

Water: <1 mg/mL

Ethanol: 43 mg/mL (86.01 mM)

Solubility (In vivo)

1% DMSO+30% PEG 300+dd H2O: 30mg/mL

Synonyms

AZD-9291; AZD9291; AZD 9291; Osimertinib free base; Mereletinib; Trade name: Tagrisso

Chemical Name: N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide

InChi Key: DUYJMQONPNNFPI-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O

In Vitro	In vitro activity: AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro. Kinase Assay: Osimertinib (formerly known as AZD-9291 and mereletinib) is an oral available, irreversible, and mutant-selective, 3rd generation EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. It inhibits both activating and resistant EGFR mutations while sparing the normal form of EGFR that is present in normal skin and gut cells, thereby reducing the side effects encountered with currently available medicines. Cell Assay: AZD9291 potently inhibits EGFR phosphorylation in EGFRm+ (e.g. PC9; < 25 nM) and EGFR m+/T790M (e.g. H1975; < 25 nM) cell lines in vitro, whilst demonstrating much less activity against wild-type EGFR lines (e.g. LoVo;> 500 nM). Consistently, AZD9291 showed significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro.
In Vivo	AZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK in vivo.
Animal model	EGFRm+ and EGFRm+/T790M transgenic mice
Formulation & Dosage	5 mg/kg; p.o
References	Transl Lung Cancer Res. 2014 Dec;3(6):370-2; J Med Chem. 2014 Oct 23;57(20):8249-67.

In Vitro

In vitro activity: AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro.

Kinase Assay: Osimertinib (formerly known as AZD-9291 and mereletinib) is an oral available, irreversible, and mutant-selective, 3rd generation EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. It inhibits both activating and resistant EGFR mutations while sparing the normal form of EGFR that is present in normal skin and gut cells, thereby reducing the side effects encountered with currently available medicines.

Cell Assay: AZD9291 potently inhibits EGFR phosphorylation in EGFRm+ (e.g. PC9; < 25 nM) and EGFR m+/T790M (e.g. H1975; < 25 nM) cell lines in vitro, whilst demonstrating much less activity against wild-type EGFR lines (e.g. LoVo;> 500 nM). Consistently, AZD9291 showed significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro.

In Vivo

AZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK in vivo.

Animal model

EGFRm+ and EGFRm+/T790M transgenic mice

Formulation & Dosage

5 mg/kg; p.o

References

Transl Lung Cancer Res. 2014 Dec;3(6):370-2; J Med Chem. 2014 Oct 23;57(20):8249-67.

CAS NO:	1421373-65-0
规格:	≥98%

包装	价格(元)
100mg	电议
500mg	电议
1g	电议
2g	电议
5g	电议