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505021 Sigma-AldrichBMX-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.

MSDS
参考
Data Sheet

同义词: 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

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
1431525-23-3	C₂₉H₂₄N₄O₄S

价格及供货情况

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Description
Overview	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, 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 Number	505021
Brand Family	Calbiochem®
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

References
References	Liu, F., et al. 2013. ACS Chem. Biol. 8, 1423.

Product Information
CAS number	1431525-23-3
Form	Off-white solid
Hill Formula	C₂₉H₂₄N₄O₄S
Chemical formula	C₂₉H₂₄N₄O₄S
Reversible	N
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	BMX
Secondary target	BTK
Purity	≥95% by HPLC

Physicochemical Information
Cell permeable	Y

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 Instructions	Following 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
产品目录编号	GTIN
5.05021.0001	04055977263312

Documentation

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

职位
物料安全数据表 (MSDS)

参考

参考信息概述
Liu, F., et al. 2013. ACS Chem. Biol. 8, 1423.

数据表

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.

Revision	03-September-2020 JSW
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
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).
Form	Off-white solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	1431525-23-3
Chemical formula	C₂₉H₂₄N₄O₄S
Structure formula
Purity	≥95% by HPLC
Solubility	DMSO (12.5 mg/ml). Use only fresh DMSO for reconstitution.
Storage	Protect from light -20°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 3 months at -70°C.
Toxicity	Standard Handling
References	Liu, F., et al. 2013. ACS Chem. Biol. 8, 1423.

种类

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

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