Abcam, ab141364, R428 (BGB324), AXL inhibitor

Size: 5mg / 25mg
MW 506.6 Da, Purity >98%. Potent and selective inhibitor of AXL kinase (IC 50 = 14 nM). Overcomes chemotherapy resistance to various agents in multiple cancer models. Suppresses myeloid cell activation and function. AXL inhibition combined with PD-1 blockade shows potent synergistic anti-tumor effects. Greater than 100-fold selective for AXL versus ABL. Selective (50-100-fold) versus Mer and Tyro3 in cell-based assays. Highly selective for AXL versus InsR, EGFR, HER2, and PDGFRbeta in cell-free assays.
Key facts
CAS number:1037624-75-1,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:506.6 Da,
Molecular formula:C30H34N8,
PubChem:46215462,
Nature:Synthetic,
Solubility:Soluble in DMSO to 25 mM,
Biochemical name:Bemcentinib,
Biological description:Potent and selective inhibitor of AXL kinase (IC50 = 14 nM). Overcomes chemotherapy resistance to various agents in multiple cancer models. Suppresses myeloid cell activation and function. AXL inhibition combined with PD-1 blockade shows potent synergistic anti-tumor effects. Greater than 100-fold selective for AXL versus ABL. Selective (50-100-fold) versus Mer and Tyro3 in cell-based assays. Highly selective for AXL versus InsR, EGFR, HER2, and PDGFRbeta in cell-free assays.,
Canonical smiles:C1CCN(C1)C2CCC3=C(CC2)C=C(C=C3)NC4=NN(C(=N4)N)C5=NN=C6C(=C5)CCCC7=CC=CC=C76,
Isomeric smiles:C1CCN(C1)[C@H]2CCC3=C(CC2)C=C(C=C3)NC4=NN(C(=N4)N)C5=NN=C6C(=C5)CCCC7=CC=CC=C76,
InChi:InChI=1S/C30H34N8/c31-29-33-30(32-24-13-10-20-11-14-25(15-12-22(20)18-24)37-16-3-4-17-37)36-38(29)27-19-23-8-5-7-21-6-1-2-9-26(21)28(23)35-34-27/h1-2,6,9-10,13,18-19,25H,3-5,7-8,11-12,14-17H2,(H3,31,32,33,36)/t25-/m0/s1,
InChiKey:KXMZDGSRSGHMMK-VWLOTQADSA-N,
IUPAC Name:1-(3,4-diazatricyclo[9.4.0.02,7]pentadeca-1(15),2,4,6,11,13-hexaen-5-yl)-3-N-[(7S)-7-pyrrolidin-1-yl-6,7,8,9-tetrahydro-5H-benzo[7]annulen-3-yl]-1,2,4-triazole-3,5-diamine

Product details:
Solutions in DMSO may be stored at -20°C for up to 3 months.

Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C, Storage information-Store under desiccating conditions

Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
Src Axl ALK VEGF Receptor 2 EGFR Aurora B Aurora A MERTK PDGFR alpha CD167a/DDR1 Met (c-Met) Flt3/CD135 and TYRO3 are significant proteins in cell signaling. Many of these proteins are kinases enzymes that transfer phosphate groups to specific substrates modulating their activity and function. For example Axl also known as a receptor tyrosine kinase weighs around 98 kDa and commonly expresses in tissues like the bone marrow and lungs. Other proteins such as EGFR and VEGF Receptor 2 express in various tissues and have alternate names like ErbB1 and KDR respectively.
Biological function summary
These proteins play roles in cell proliferation differentiation survival and migration. Many function as part of larger complexes such as the receptor tyrosine kinase complexes involved in cellular signaling cascades. For instance Axl operates with its ligands like Gas6 to control cellular processes. Meanwhile Aurora kinases including Aurora A and B play pivotal roles during mitosis ensuring accurate chromosome segregation.
Pathways
These proteins participate in critical signaling pathways like the MAPK and PI3K/AKT pathways. Src for instance influences cell cycle regulation and survival by interacting with proteins such as Ras and PI3K. EGFR and VEGF Receptor 2 engage with downstream signaling mediators to regulate angiogenesis and metabolism. They link with other receptor kinases and pathways to coordinate responses to external signals and maintain cellular homeostasis.
These proteins have significant implications in cancer and immune disorders. Dysregulation in EGFR or Met (c-Met) often associates with various cancers including lung and colorectal cancer by promoting uncontrolled cell growth. Axl connects with cancer metastasis and resistance mechanisms. Moreover inhibitors like Axl kinase inhibitors and BGB-324 are explored to inhibit aberrant signaling showcasing their potential as therapeutic targets. Axl's interaction with MERTK and TYRO3 influences immune responses implicating it in autoimmune conditions.