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1029044-16-3 Usage


Pexidartinib is a small-molecule, oral, potent multi-targeted receptor tyrosine kinase (RTK) inhibitor of CSF-1R, Kit, and Flt3 and it can cross the blood-brain barrier. In M-NFS-60, Bac 1.2F5 and M-07e cells, PLX3397 (Pexidartinib) inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μM and 0.1 μM, respectively. It has been reported that PLX3397 strongly attenuates systemic and local accumulation of macrophages driven by B16F10 melanoma and does not affect Gr-1+ bone marrow-derived suppressor cells. Besides, PLX3397 weakly inhibited the growth of SK-N-SH cells with an IC50 of 10 μM and had little effect on the growth of MDA-MB-231 human tumor cell xenografts. In MMTV-PyMT mice, pexidartinib (40 mg/kg, p.o.) significantly inhibits both steady-state and PTX-induced tumor infiltration by CD45 + CD11b + Ly6C ? Ly6G ? F4/80 +. Pexidartinib/PTX therapy also results in a significant reduction in CD31+ vessel density within mammary tumors, paralleling induction of apoptosis and necrosis.


Different sources of media describe the Description of 1029044-16-3 differently. You can refer to the following data:
1. Pexidartinib (TURALIO?) is a novel, orally available small molecule tyrosine kinase inhibitor (TKI) with potent and selective activity against the colony-stimulating factor 1 (CSF1) receptor. Pexidartinib also inhibits KIT proto-oncogene receptor tyrosine kinase (KIT) and FMS-like tyrosine kinase 3 harboring an internal tandem duplication mutation (FLT3-ITD). Pexidartinib has been developed by Daiichi Sankyo for the treatment of tenosynovial giant cell tumor (TGCT; also known as giant cell tumor of the tendon sheath or pigmented villonodular synovitis.
2. 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 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.

Synthetic Routes

The synthetic routes of pexidartinib were developed by Daiichi Sankyo Company6. A novel efficient synthetic route for pexidartinib was designed via Tsuji–Trost/Heck tandem reaction in combination with palladium and silver catalysis, which avoids the need for ultra-low temperature and greatly reduces the amount of corrosive trifluoroacetic acid. The cheap and easily available materials and reagents and easy operations for workup and purification make this route more practical.

Anti-tumor Activity

Administration of PLX3397 reduced CIBP, induced substantial intratumoral fibrosis, and was also highly efficacious in reducing tumor cell growth, formation of new tumor colonies in bone, and pathological tumor-induced bone remodeling. PLX3397 is superior to imatinib in the treatment of malignant peripheral nerve sheath tumor (MPNST), and the combination of PLX3397 with a TORC1 inhibitor could provide a new therapeutic approach for the treatment of this disease.


Pexidartinib is RTK inhibitor. It can be used in pharmacological activity, therapeutic use, and biological study of inhibition of colony stimulating factor-1 receptor improves antitumor efficacy of BRAF inhibition.

in vitro

plx3397 strongly dampened the systemic and local accumulation of macrophages driven by b16f10 melanomas, without affecting gr-1+ myeloid derived suppressor cells [1].

in vivo

wild-type c57 mice were orthotopically injected with gl261 cells and fed with plx3397 compound. after 2 wks, tumors in the control group showed extensive microglia infiltration. in animals fed plx3397, however, there was a substantial reduction in the number of iba1- positive cells at the tumor [2].


1)?DeNardo?et al.?(2011)?Leukocyte Complexity Predicts Breast Cancer Survival and Functionally Regulates Response to Chemotherapy;?Cancer Discov.?1?54 2)?Mok?et al.?(2014)?Inhibition of CSF-1 receptor improves the antitumor efficacy of adoptive cell transfer immunotherapy;?Cancer Res.74?15 3)Sluijter?et al.?(2014)?Inhibition of CSF-1R supports T-cell mediated melanoma therapy;?PLoS One?9?e104230 4)?Peranzoni?et al.?(2018)?Macrophages impede CD8 T cells from reaching tumor cells and limit the efficacy of anti-PD-1 treatment;?Proc. Natl. Acad. Sci. USA?115?E4041 5)?Shi?et al.?(2019)?Modulating the Tumor Microenvironment via Oncolytic Viruses and CSF-1R Inhibition Synergistically Enhances Anti-PD-1 Immunotherapy;?Mol. Ther.?27?244 6) Dammeijer?et al.?(2017)?Depletion pf Tumor-Associated Macrophages with a CSF-1R Kinase Inhibitor Enhances Antitumor Immunity and Survival Induced by DC Immunotherapy;?Cancer Immunol. Res.?5?535

Check Digit Verification of cas no

The CAS Registry Mumber 1029044-16-3 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,2,9,0,4 and 4 respectively; the second part has 2 digits, 1 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1029044-16:
113 % 10 = 3
So 1029044-16-3 is a valid CAS Registry Number.



According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 19, 2017

Revision Date: Aug 19, 2017


1.1 GHS Product identifier

Product name PLX-3397

1.2 Other means of identification

Product number -
Other names Pexidartinib(PLX3397)

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:1029044-16-3 SDS

1029044-16-3Downstream Products

1029044-16-3Relevant articles and documents

Exploratory Process Development of Pexidartinib through the Tandem Tsuji-Trost Reaction and Heck Coupling

Chen, Dongsheng,Li, Jianqi,Liu, Yu,Zhang, Yi

, p. 2564 - 2571 (2019)

A novel synthetic route to CSF1R inhibitor pexidartinib was designed and demonstrated. Crucial to the successful synthesis is a tandem Tsuji-Trost reaction and Heck coupling in combination with palladium and silver catalysis. The final product was obtained via five steps in 49percent yield with purity as high as 99.2percent. The cheap and available materials and reagents and easy operations for workup and purification make this route more practical.

Synthetic method for continuously producing pexidartinib


Paragraph 0040-0044; 0047-0052; 0055-0060; 0063, (2020/06/20)

The invention relates to the field of chemical synthesis, and particularly discloses a synthetic method for continuously producing pexidartinib. According to the method, 5-chloro-7-azaindole and 2-chloro-5-chloromethylpyridine are adopted as initial raw materials; an alkylation intermediate is obtained with a high yield through an alkylation reaction of the 5-chloro-7-azaindole, the intermediate does not need purification and directly and continuously participates a next-step reaction, and an amino substitution reaction on the intermediate and 3-aminomethyl-6-(trifluoromethyl) pyridine is performed to obtain a target product pexidartinib. The invention provides the synthetic route for two-step continuous production of the pexidartinib for the first time, the method is particularly suitablefor commercial mass production, and can be used for preparing the pexidartinib with low cost, high yield, high purity and high environmental protection property.

Simple preparation method of (by machine translation)


, (2019/09/14)

The invention relates to a simple preparation method, in particular to a simple preparation method of. The method utilizes N - (2 -trifluoromethyl-pyridin -5 -yl) methyl -2 - amino -5 - alkoxymethylpyridine or N - (2 - trifluoromethyl-pyridin -5 -yl) methyl -2 - amino -5 - cyanmethylpyridine (II) and acetonitrile in the presence of a base to give N - (2 -trifluoromethyl-pyridin -5 -yl) methyl -2 - amino -5 -cyanacetylmethylpyridine (III), compound III and nitromethane to prepare compound IV. The compound V, which is obtained by the addition, of 2 3 - dichloropropenal addition and base, is then subjected to hydrogenation reduction - cyclization in the presence of a catalyst to prepare the piroxicin. The method is cheap and easily available, short, simple and convenient to operate, low in waste water amount, high, green and environment-friendly, and facilitates industrial production. (by machine translation)

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