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AB254454

Pexidartinib, CSF1R inhibitor

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MW 417.8 Da, Purity >98%. Potent MCSF Receptor (CSF1R) inhibitor (IC50 = 13 nM). Also inhibits Kit (IC50 = 16 nM) and Flt3 (IC50 = 160 nM). Highly selective (IC50 >1 μM) against a panel of over 200 kinases. Inhibits MCSF Receptor-dependent proliferation (0.1 - 0.44 μM) in cell models. Inhibits glioblastoma invasion in mouse xenograft models.

View Alternative Names

AAK1_HUMAN, AP2 associated kinase 1, AP2-associated protein kinase 1, Adaptor-associated kinase 1, C-FMS, CD 115, CD 135, CD115 antigen, CD135 antigen, CSF-1 receptor, CSF1R_HUMAN, CSFR, Colony stimulating factor 1 receptor, Colony stimulating factor I receptor, DKFZp686F03202, DKFZp686K16132, EC 2.7.10.1, FIM 2, FL cytokine receptor, FLJ23712, FLJ25931, FLJ31060, FLJ42882, FLJ45252, FLT3_HUMAN, FMS, FMS proto oncogene, Fetal liver kinase 2, Flk 2, Fms related tyrosine kinase 3, Fms-like tyrosine kinase 3, Growth factor receptor tyrosine kinase type III, HDLS, KIAA1048, KPCT_HUMAN, Ly-72, M-CSF Receptor, M-CSF-R, MGC126514, MGC138170, MGC141919, MGC164568, MGC164570, Macrophage colony stimulating factor I receptor, Macrophage colony-stimulating factor 1 receptor, McDonough feline sarcoma viral (v fms) oncogene homolog, OTTHUMP0000004234, OTTHUMP00000043364, OTTHUMP00000043365, Oncogen FMS, PKC 0, PRKCT, Prkcq, Protein kinase C theta, Protein kinase C theta type, Proto-oncogene c-Fms, Receptor type tyrosine protein kinase FLT3, STK-1, Stem cell tyrosine kinase 1, Tyrosine-protein kinase receptor FLT3, V-FMS McDonough feline sarcoma viral oncogen homolog, formerly, nPKC-theta

1 Images
Chemical Structure - Pexidartinib, CSF1R inhibitor (AB254454)
  • Chemical Structure

Supplier Data

Chemical Structure - Pexidartinib, CSF1R inhibitor (AB254454)

2D chemical structure image of ab254454, Pexidartinib, CSF1R inhibitor

Key facts

CAS number

1029044-16-3

Purity

>98%

Form

Solid

form

Molecular weight

417.8 Da

Molecular formula

C<sub>2</sub><sub>0</sub>H<sub>1</sub><sub>5</sub>ClF<sub>3</sub>N<sub>5</sub>

PubChem

25151352

Nature

Synthetic

Solubility

Soluble in DMSO to 10 mM

Biochemical name

Pexidartinib

Biological description

Potent MCSF Receptor (CSF1R) inhibitor (IC50 = 13 nM). Also inhibits Kit (IC50 = 16 nM) and Flt3 (IC50 = 160 nM). Highly selective (IC50 >1 μM) against a panel of over 200 kinases. Inhibits MCSF Receptor-dependent proliferation (0.1 - 0.44 μM) in cell models. Inhibits glioblastoma invasion in mouse xenograft models.

Canonical smiles

C1=CC(=NC=C1CC2=CNC3=C2C=C(C=N3)Cl)NCC4=CN=C(C=C4)C(F)(F)F

InChi

InChI=1S/C20H15ClF3N5/c21-15-6-16-14(10-28-19(16)29-11-15)5-12-2-4-18(26-7-12)27-9-13-1-3-17(25-8-13)20(22,23)24/h1-4,6-8,10-11H,5,9H2,(H,26,27)(H,28,29)

InChiKey

JGWRKYUXBBNENE-UHFFFAOYSA-N

IUPAC Name

5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-[[6-(trifluoromethyl)pyridin-3-yl]methyl]pyridin-2-amine

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Product details

Solutions in DMSO may be stored at -20°C for up to 2 months.
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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
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Supplementary information

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

Protein Kinase C theta (PKCθ/PRKCQ) CSF-1-R (colony stimulating factor 1 receptor) and Flt3/CD135 are involved in various cellular functions. PKCθ with a mass of approximately 82 kDa primarily expresses in T cells and is important for T-cell receptor signaling. CSF-1-R also referred to as macrophage colony-stimulating factor receptor (M-CSFR) has a mass of about 120 kDa and expresses in macrophages and osteoclast precursors. Flt3 alternatively known as CD135 weighs around 158 kDa and is predominantly found in hematopoietic progenitor cells. These proteins perform unique mechanical roles integral to cellular processes.
Biological function summary

PKCθ functions in T-cell activation and survival acting as part of a larger signaling complex during immune responses. CSF-1-R is responsible for macrophage proliferation differentiation and survival. It forms a receptor complex upon binding its ligand contributing to tissue homeostasis and inflammation response. Flt3 plays a pivotal role in hematopoiesis especially in the development and maintenance of multipotent progenitor cells. These activities highlight the essential roles each target plays in maintaining immune and hematopoietic systems.

Pathways

PKCθ participates in the NF-kB and AP-1 pathways important for T-cell activation and cytokine production. It signalizes alongside proteins like LAT and SLP-76. CSF-1-R involves in the PI3K-Akt and MAPK/ERK pathways important for cell growth and survival. It interacts with proteins such as Grb2 and Src to propagate its signaling. Flt3 functions in the JAK-STAT and PI3K pathways important for gene expression and cell cycle regulation and associates with STAT5 and Akt proteins. These interactions place these targets within critical cellular communication networks.

PKCθ links to autoimmune diseases like rheumatoid arthritis due to its role in T-cell signaling and activation. It directly influences the production of inflammatory cytokines contributing to disease pathology. CSF-1-R relates to cancer and inflammatory disorders as its dysregulation can lead to tumor growth and chronic inflammation. Pexidartinib acts as a CSF-1-R inhibitor offering therapeutic potential in conditions like tenosynovial giant cell tumors. Flt3 mutations associate with acute myeloid leukemia where its overactivation leads to uncontrolled cell growth. Flt3’s connection to STAT5 indicates its contribution to leukemogenesis.
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Product protocols

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