Pexidartinib

Colony stimulating factor 1 (CSF1) is a cytokine that is involved in the recruitment and activation of tissue macrophages. It exerts these effects by binding to its corresponding receptor tyrosine kinase, the cFMS/CSF1 receptor (CSF1R). Pexidartinib is a brain-penetrant inhibitor of CSF1R, as well as c-Kit and FLT3 (IC50s = 20, 10, and 160 nM in vitro, respectively). It has been used in combination with paclitaxel (Cay-10461) to block macrophage recruitment in mammary tumor-bearing mice, thus slowing primary tumor development and metastasis. Pexidartinib has also been used to block microglial stimulation of glioblastoma invasion in both cell culture and a mouse model of glioblastoma multiforme.Formal Name: N-[5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-6-(trifluoromethyl)-3-pyridinemethanamine. CAS Number: 1029044-16-3. Synonyms: PLX3397. Molecular Formula: C20H15ClF3N5. Formula Weight: 417.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml, DMSO: 20 mg/ml. lambdamax: 235, 303 nm. SMILES: ClC1=CC2=C(N=C1)NC=C2CC3=CN=C(NCC4=CN=C(C(F)(F)F)C=C4)C=C3. InChi Code: 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). InChi Key: JGWRKYUXBBNENE-UHFFFAOYSA-N.