Skip to main content

MW 568.7 Da, Purity >98%. Potent and selective inihbitor of the tyrosine kinases Lck and Src with IC50 values of 2 nM for Lck and 6 nM for Src.

Be the first to review this product! Submit a review

Publications

Key facts

CAS number
837422-57-8
Purity
> 98%
Form
Powder
Molecular weight
568.7 Da
Molecular formula
C32H36N6O4
PubChem identifier
11844351
Nature
Synthetic

Alternative names

Recommended products

MW 568.7 Da, Purity >98%. Potent and selective inihbitor of the tyrosine kinases Lck and Src with IC50 values of 2 nM for Lck and 6 nM for Src.

Key facts

Purity
> 98%
PubChem identifier
11844351
Solubility

Soluble in DMSO: 20 mg/ml.

Biochemical name
2,6-Dimethylphenyl (2,4-dimethoxyphenyl)(2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)carbamate
Biological description

Potent and selective inihbitor of the tyrosine kinases Lck and Src with IC50 values of 2 nM for Lck and 6 nM for Src.

Canonical SMILES
CC1=C(C(=CC=C1)C)OC(=O)N(C2=C(C=C(C=C2)OC)OC)C3=NC(=NC=C3)NC4=CC=C(C=C4)N5CCN(CC5)C
InChI
InChI=1S/C32H36N6O4/c1-22-7-6-8-23(2)30(22)42-32(39)38(27-14-13-26(40-4)21-28(27)41-5)29-15-16-33-31(35-29)34-24-9-11-25(12-10-24)37-19-17-36(3)18-20-37/h6-16,21H,17-20H2,1-5H3,(H,33,34,35)
InChIKey
NBTNHSGBRGTFJS-UHFFFAOYSA-N
IUPAC name
(2,6-dimethylphenyl) N-(2,4-dimethoxyphenyl)-N-[2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]carbamate

Storage

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C

Supplementary info

This supplementary information is collated from multiple sources and compiled automatically.
Activity summary

The targets p38 Src VEGF Receptor 2 and Lck play significant roles in various cellular processes. p38 also known as MAPK14 is part of the mitogen-activated protein kinase (MAPK) family and it has a mass of about 41 kDa. It is widely expressed in many tissues like the heart skeletal muscle and liver. Src a non-receptor tyrosine kinase weighs approximately 60 kDa and resides in the cytoplasm and membranes of cells. VEGF Receptor 2 also known as KDR or FLK-1 is integral to cell signaling and shows a molecular weight of 150 kDa. It is found in endothelial cells facilitating vascular growth. Lck a lymphocyte-specific tyrosine kinase with a mass of roughly 56 kDa localizes mainly in T-cells and is important for T-cell receptor signaling.

Biological function summary

These proteins perform essential functions in cellular signaling. p38 for instance regulates inflammatory responses by activating downstream effectors in stress-stimulated pathways. Src plays a significant role in the regulation of cell division and survival by interacting with various signal transducers. VEGF Receptor 2 is fundamental to angiogenesis a process vital for new blood vessel formation. It participates in a complex with VEGF to transmit signals for endothelial cell proliferation. Lck functions in the immune system by initiating the signaling cascade necessary for T-cell activation and development.

Pathways

These proteins impact significant cellular communication networks. p38 is an important player in the MAPK pathway involved in responses to stress stimuli. It interacts with other MAPKs like JNK in controlling cytokine production. Src integrates into the Src-family kinase pathway modulating cell growth and movement by activating downstream proteins such as FAK. VEGF Receptor 2 is pivotal in the VEGF signaling pathway partnering with PI3K and AKT to promote endothelial cell responses. Lck fits into the T-cell receptor pathway where it associates with proteins like ZAP-70 to relay activation signals.

Associated diseases and disorders

These targets link to several pathological conditions. p38 plays an essential role in inflammatory diseases like arthritis where it mediates inflammatory cytokine production. Src is implicated in cancer carrying mutations or overexpressions in various malignancies often accompanied by proteins such as FAK that drive tumor progression. VEGF Receptor 2 contributes to angiogenesis-related disorders including cancer where its pathway's overactivation supports tumor vasculature development. Lck links with immune disorders like autoimmune diseases as improper signaling here leads to abnormal T-cell responses. In these contexts therapeutic targeting of these proteins can provide compelling strategies to mitigate disease progression.

Product promise

We are dedicated to supporting your work with high quality reagents and we are here for you every step of the way should you need us.

In the unlikely event of one of our products not working as expected, you are covered by our product promise.

Full details and terms and conditions can be found here:
Terms & Conditions.

0 product images

    Downloads

    Product protocols

    For this product, it's our understanding that no specific protocols are required. You can:

    Please note: All products are 'FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC OR THERAPEUTIC PROCEDURES'.

    For licensing inquiries, please contact partnerships@abcam.com