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General description
A cell-permeable tricyclic quinoline-acrylamide compound that potently inhibits BMX and BTK kinase activity (IC50 = 8 and 10.4 nM, respectively) by covalently targeting ATP-binding site cysteine (Ser496 and S481 of respective human sequence), while being less potent against 3 other TEC family kinases with the same conserved cysteine (IC50 = 175, 377, and 653 nM against TEC, JAK3, and BLK, respectively) and completely ineffective toward BMX C496S even at concentrations as high as 10 µM. Only PI 3-Kγ/PIK3CG, SBK1, and PIP5K2C are significantly inhibited by BMX-IN-1 (by ≥94% at 1 µM) in a selectivity profiling against 437 other kinase constructs, including TEC family members EGFR/T790M, ITK (IC50 = 4.28 and 5.25 µM, respectively), TXK, ErbB2/Her2, ErbB4/Her4, JAK1, and JAK2 (75%, 10%, 22%, 13%, and 14% inhibition at 1 µM, respectively). Potently inhibits the proliferation of TEL-BMX transformed Ba/F3 Ba/F3 (GI50 = 25 nM), while being much less effective against TEL-BLK, TEL-JAK1, TEL-JAK2, TEL-JAK3, or TEL-TYK2E957D transformed Ba/F3 (GI50 = 3.64, 4.92, 5.83, 7.98, and 6.09 µM, respectively) or prostate cancer cells using a panel of 5 established lines (GI50 ≥2.46 µM).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
BMX
Reversible: no
Secondary Target
BTK
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 3 months at -70°C.
Use only fresh DMSO for reconstitution.
Other Notes
Liu, F., et al. 2013. ACS Chem. Biol.8, 1423.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥95% (HPLC) |
| Quality Segment | 100 |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | off-white |
| solubility | DMSO: 12.5 mg/mL |
| storage temp. | −20°C |
| SMILES string | [S](=O)(=O)(Nc1ccc(cc1)c2cc3c4[n]([c](ccc4cnc3cc2)=O)c5cc(c(cc5)C)NC(=O)C=C)C |
| InChI | 1S/C29H24N4O4S/c1-4-27(34)31-26-16-23(12-5-18(26)2)33-28(35)14-9-21-17-30-25-13-8-20(15-24(25)29(21)33)19-6-10-22(11-7-19)32-38(3,36)37/h4-17,32H,1H2,2-3H3,(H,31,34) |
| InChI key | SFMJNHNUOVADRW-UHFFFAOYSA-N |
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询价
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¥ 2013.69
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¥ 1451.54
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¥ 5725.45
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¥ 3812.28
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¥ 1653.62
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¥ 15214.65
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¥ 10277.12
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¥ 2842.54
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