Product Information
Applications
Biological Information
Primary TargetBMX
Secondary targetBTK
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 3 months at -70°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

BMX-IN-1 - CAS 1431525-23-4 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Liu, F., et al. 2013. ACS Chem. Biol. 8, 1423.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision09-December-2013 JSW
SynonymsN-(2-Methyl-5-(9-(4-(methylsulfonamido)phenyl)-2-oxobenzo[h][1,6]naphthyridin-1(2H)-yl)phenyl)acrylamide, BMX/BTK Inhibitor, Bruton's Tyrosine Kinase Inhibitor IV, BLK Inhibitor I, BMX Inhibitor I, JAK3 Inhibitor XIII, PI 3-K Inhibitor XX, PIP5K2C Inhibitor I, SBK1 Inhibitor I, TEC Inhibitor I, TXK Inhibitor I
DescriptionA 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).
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1431525-23-4
Chemical formulaC₂₉H₂₄N₄O₄S
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (12.5 mg/ml). Use only fresh DMSO for reconstitution.
Storage -20°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 3 months at -70°C.
Toxicity Standard Handling
ReferencesLiu, F., et al. 2013. ACS Chem. Biol. 8, 1423.

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Categories

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Other Kinase Inhibitors