Description
Key facts
CAS number:1123837-84-2,
Purity:98%,
Form:SolidSee storage information,
Molecular weight:629.7 Da,
Molecular formula:C33H29F2N5O4S,
PubChem:25212148,
Nature:Synthetic,
Solubility:Soluble in DMSO (up to at least 25 mg/ml),
Biochemical name:Sitravatinib,
Biological description:Broad spectrum receptor tyrosine kinase inhibitor (e.g. Axl, c-Met, PDGFR, VEGFR, Ephrin receptor family, and FLT3). Better efficacy in mouse models than imatinib and crizotinib.,
Canonical smiles:COCCNCC1=CN=C(C=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F,
InChi:InChI=1S/C33H29F2N5O4S/c1-43-15-14-36-18-20-2-8-25(38-19-20)29-17-26-30(45-29)28(10-13-37-26)44-27-9-7-23(16-24(27)35)40-32(42)33(11-12-33)31(41)39-22-5-3-21(34)4-6-22/h2-10,13,16-17,19,36H,11-12,14-15,18H2,1H3,(H,39,41)(H,40,42),
InChiKey:WLAVZAAODLTUSW-UHFFFAOYSA-N,
IUPAC Name:1-N'-[3-fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]pyridin-2-yl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Properties and Storage Information:
Shipped at conditions-Ambient - Cannot 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.
TrkA Axl TrkB VEGF Receptor 2 c-Kit Met (c-Met) Flt3/CD135 and Ifnb1 are important proteins with distinct mechanical functions. TrkA also known as NTRK1 is a receptor tyrosine kinase with a mass of around 140 kDa expressed in nerve cells. Axl is another receptor tyrosine kinase found in various tissues including immune system cells. TrkB similar to TrkA plays roles in the nervous system while VEGF Receptor 2 also known as KDR or FLK1 is a critical player in vascular endothelial growth. c-Kit a stem cell factor receptor is influential in cell signal transduction. Met or c-Met acts as a receptor for hepatocyte growth factor mainly regulating cellular growth. Flt3 or CD135 is a part of early hematopoietic cell development. Ifnb1 also known simply as IFN-beta acts as a cytokine with functions in antiviral defense and immune regulation.
Biological function summary
These proteins engage in different areas of cellular processes. TrkA Axl and TrkB serve important roles in signal transduction for neuronal development and differentiation. VEGF Receptor 2 is involved in angiogenesis and endothelial cell proliferation while c-Kit participates in the development of melanocytes mast cells and germ cells. Met has a pivotal role in cell motility and invasive growth. Flt3/CD135 is essential for early development of blood cells and Ifnb1 is part of the immune response against viruses. These proteins may operate independently or be part of larger complexes facilitating broad cellular responses.
Pathways
These proteins integrate into key signaling routes. Both TrkA and TrkB are part of the neurotrophin signaling pathway interacting with nerve growth factors. Axl and Met contribute to the regulation of the MAPK and PI3K/AKT pathways which are important for cell survival and proliferation. VEGF Receptor 2 is central in the angiogenesis-related signal cascade. Within immune response pathways both Flt3/CD135 and Ifnb1 are significant impacting hematopoietic and antiviral pathways respectively. These proteins coordinate with others such as PI3K and AKT amplifying cell survival and growth signals.
These targets have significant implications. Mutations or dysregulation of TrkA Met and c-Kit are often linked to cancer including neuroblastoma and gastrointestinal stromal tumors. Abnormal activity of Axl and VEGF Receptor 2 contributes to cancer progression through promoting angiogenesis and metastasis. Flt3/CD135 mutations are primarily associated with acute myeloid leukemia affecting hematopoietic function. Ifnb1 plays a role in autoimmune diseases like multiple sclerosis by modulating immune responses. These proteins can influence disease pathways directly or through interactions with others like AKT and STAT3 driving pathological processes.
