| Identification | Back 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 Properties | Back 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 |
| Hazard Information | Back 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).1 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.1 NVP-TAE226 has been shown to inhibit glioma and ovarian tumor growth in in vivo tumor models.2 | [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. |
|
| Company Name: |
Energy Chemical
|
| Telephone: |
400-0056266 |
| Website: |
www.energy-chemical.com |
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
|