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761437-28-9

761437-28-9 Structure

761437-28-9 Structure
IdentificationBack Directory
[Name]

TAE226 (NVP-TAE226)
[CAS]

761437-28-9
[Synonyms]

TAE226
CS-1694
NVP-TAE 226
TAE-226, >98%
TAE226 (NVP-TAE226)
TAE226 (NVP-TAE226), >98%
TAE226 (NVP-TAE226) USP/EP/BP
TAE226; TAE-226;TAE 226;NVPTAE226
2-((5-Chloro-2-((2-methoxy-4-morpholinophenyl)-amino)pyrimidin-4-yl)amino)-N-methylbenzamide
2-[[5-Chloro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]-N-methylbenzamide
Benzamide, 2-[[5-chloro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]-N-methyl-
NVP-TAE 226 2-[[5-Chloro-2-[[2-methoxy-4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]amino]-N-methylbenzamide
[Molecular Formula]

C23H25ClN6O3
[MDL Number]

MFCD12031516
[MOL File]

761437-28-9.mol
[Molecular Weight]

468.936
Chemical PropertiesBack Directory
[density ]

1.349
[storage temp. ]

Store at -20°C
[solubility ]

≥23.45 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
[form ]

solid
[pka]

14.57±0.46(Predicted)
[color ]

White to khaki
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
Hazard InformationBack Directory
[Description]

NVP-TAE226 is an inhibitor of focal adhesion kinase (FAK; IC50 = 5.5 nM) and the related proline-rich tyrosine kinase 2-β (PYK2β; IC50 = 5 nM). It can also inhibit the insulin-like growth factor 1 receptor (IC50 = 0.16 μM) as well as the activity of its downstream target genes such as MAPK and Akt. NVP-TAE226 has been shown to inhibit glioma and ovarian tumor growth in in vivo tumor models.
[Uses]

NVP-TAE 226 is FAK and IGF-IR inhibitor. It can be used in biological study and therapeutic use of TAE226, a bis-?anilino pyrimidine compound, inhibits the egfr-?mutant kinase including T790M mutant to show anti-?tumor effect on EGFR-?mutant non-?small cell lung cancer cells.
[Definition]

ChEBI: 2-[[5-chloro-2-[2-methoxy-4-(4-morpholinyl)anilino]-4-pyrimidinyl]amino]-N-methylbenzamide is a member of morpholines.
[in vivo]

Treatment with NVP-TAE 226 (TAE226) at 50 or 75 mg/kg extends the median survival of U87 xenograft animals by 6 and 7 days, respectively (P=0.084 and P=0.042, respectively, compared with vehicle-treated animals). However, NVP-TAE 226 treatment of LN229-engrafted animals significantly prolongs their median survival by 19 days (P<0.004 for both dosages, compared with vehicle-treated animals)[1].

[target]

PYK2
[storage]

Store at -20°C
[References]

[1]. liu, t.j., et al., inhibition of both focal adhesion kinase and insulin-like growth factor-i receptor kinase suppresses glioma proliferation in vitro and in vivo. mol cancer ther, 2007. 6(4): p. 1357-67.
[2]. plaza-menacho, i., et al., focal adhesion kinase (fak) binds ret kinase via its ferm domain, priming a direct and reciprocal ret-fak transactivation mechanism. j biol chem, 2011. 286(19): p. 17292-302.
Spectrum DetailBack Directory
[Spectrum Detail]

TAE226 (NVP-TAE226)(761437-28-9)1HNMR
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