| Bioactivity | Tilfrinib (compound 4f) is a potent and selective Brk/PTK6 inhibitor with an IC50 value of 3.15 nM for Brk. Tilfrinib shows good anti-proliferative activity and has potential of anti-tumour[1][2]. | |||||||||
| Target | IC50: 3.15 nM (Brk), PTK6. | |||||||||
| Invitro | Tilfrinib (20 µM; 36 h) shows inhibition of PTK6, and decreases the ETV4 WT-induced expression of CXCL1 or CXCL8 in UM-UC-3 cells and expression of VEGFA or MMP9 in TANs[1].Tilfrinib (compound 4f) shows good anti-proliferative activity against MCF7, HS-578/T and BT-549 cells with GI50 values of 0.99, 1.02 and 1.58 µM[2]. Western Blot Analysis[1] Cell Line: | |||||||||
| Name | Tilfrinib | |||||||||
| CAS | 1600515-49-8 | |||||||||
| Formula | C17H13N3O | |||||||||
| Molar Mass | 275.30 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Zhang Q, Liu S, et al. ETV4 mediated tumor-associated neutrophil recruitment promotes lymphangiogenesis and lymphatic metastasis of bladder cancer[J]. 2022. [2]. Mahmoud KA, et al. Discovery of 4-anilino α-carbolines as novel Brk inhibitors. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1948-51. |
Tilfrinib
CAS: 1600515-49-8 F: C17H13N3O W: 275.30
Tilfrinib (compound 4f) is a potent and selective Brk/PTK6 inhibitor with an IC50 value of 3.15 nM for Brk. Tilfrinib sh
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