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505021 BMX-IN-1 - CAS 1431525-23-3 - Calbiochem

BMX-IN-1 - CAS 1431525-23-3 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-(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

Primary Target: BMX
505021
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Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

CAS #Empirical Formula
1431525-23-3C₂₉H₂₄N₄O₄S

Products

KatalógusszámCsomagolás Menny./csomag
5.05021.0001 Üvegpalack 10 mg
Description
OverviewA 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, while being less potent against TEC family kinases TEC, JAK3, BLK with the same conserved cysteine (IC50 = 175, 377, and 653 nM, respectively). Only PI 3-Kγ/PIK3CG, SBK1, PIP5K2C (by ≥94% at 1 µM), and TXK (by 75% at 1 µM) are significantly inhibited by BMX-IN-1 in a selectivity profiling against 437 other kinase constructs. 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 µM) or a panel of 5 prostate cancer cell lines (GI50 ≥2.46 µM).
Catalogue Number505021
Brand Family Calbiochem®
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
References
ReferencesLiu, F., et al. 2013. ACS Chem. Biol. 8, 1423.
Product Information
CAS number1431525-23-3
FormOff-white solid
Hill FormulaC₂₉H₂₄N₄O₄S
Chemical formulaC₂₉H₂₄N₄O₄S
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
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
Global Trade Item Number
Katalógusszám GTIN
5.05021.0001 04055977263312

Documentation

BMX-IN-1 - CAS 1431525-23-3 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Hivatkozások áttekintése
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.

Revision03-September-2020 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 number1431525-23-3
Chemical formulaC₂₉H₂₄N₄O₄S
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (12.5 mg/ml). Use only fresh DMSO for reconstitution.
Storage Protect from light
-20°C
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.