| Identification | Back Directory | [Name]
KX2-391 | [CAS]
897016-82-9 | [Synonyms]
KX 01
CS-234
Tirbanibulin
KX2-391 (KX01)
KX2-391 USP/EP/BP
Tirbanibulin, KX2-391
KX2-391;KX2 391;KX2391
N-benzyl-2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)acetamide
N-benzyl-2-[5-[4-(2-morpholin-4-ylethoxy)phenyl]pyridin-2-yl]acetamide
5-[4-[2-(4-Morpholinyl)ethoxy]phenyl]-N-(phenylmethyl)-2-pyridineacetamide
2-Pyridineacetamide, 5-[4-[2-(4-morpholinyl)ethoxy]phenyl]-N-(phenylmethyl)- | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C26H29N3O3 | [MDL Number]
MFCD18633218 | [MOL File]
897016-82-9.mol | [Molecular Weight]
431.53 |
| Chemical Properties | Back Directory | [Boiling point ]
680.9±55.0 °C(Predicted) | [density ]
1.169 | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥121 mg/mL in DMSO; ≥2.44 mg/mL in EtOH with gentle warming and ultrasonic | [form ]
Powder | [pka]
14.73±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
A synthetic, orally bioavailable small molecule and non-ATP competitive Src tyrosine kinase inhibitor with an IC50 of average 72 nM. | [Biological Activity]
kx2-391 is a highly selective inhibitor of src kinase with ic50 value of 20nm [1].kx2-391 is a non-atp competitive inhibitor of src. it is the first inhibitor that targets src kinase within the substrate binding site. kx2-391 inhibits src catalyzed trans-phosphorylation of fak, shc, paxillin as well as src kinase autophosphorylation. kx2-391 has no effects on pdgfr, egfr, jak1, jak2 and lck demonstrating it as a selective inhibitor. it is also found to be an inhibitor of tubulin polymerization through binding to the unique confirmation on heterodimeric tubulin. in cellular assays, kx2-391 shows growth inhibition in nih3t3/c-src527f cells and syf/c-src527f cells with gi50 values of 23nm and 39nm, respectively [1, 2].since src acts as a regulator in cell proliferation survival, motility and invasiveness, kx2-391 is potent against a variety of solid tumors and many leukemia tumors. it is shown to inhibit primary tumor growth and to suppress metastasis [2]. | [target]
Src (HuH7) | [storage]
Store at -20°C | [References]
[1] fallah-tafti a, foroumadi a, tiwari r, et al. thiazolyl n-benzyl-substituted acetamide derivatives: synthesis, src kinase inhibitory and anticancer activities. european journal of medicinal chemistry, 2011, 46(10): 4853-4858.
[2] naing a, cohen r, dy g k, et al. a phase i trial of kx2-391, a novel non-atp competitive substrate-pocket-directed src inhibitor, in patients with advanced malignancies. investigational new drugs, 2013, 31(4): 967-973. |
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