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[CAS NO. 1029044-16-3] Pexidartinib
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-16749 |
| Brand: | MCE |
| CAS: | 1029044-16-3 |
Overview
| MDL | MFCD28900745 |
|---|---|
| Molecular Weight | 417.81 |
| Molecular Formula | C20H15ClF3N5 |
| SMILES | FC(C1=CC=C(CNC2=NC=C(CC3=CNC4=NC=C(Cl)C=C43)C=C2)C=N1)(F)F |
42 Publications Citing Use of MCE
- [1]Nature. 2022 Mar;603(7899):138-144.
- [2]Cancer Cell. 2021 Sep 1;S1535-6108(21)00445-1.
- [3]Nat Biomed Eng. 2018 Aug;2(8):578-588.
- [4]Circ Res. 2021 Sep 17;129(7):e121-e140.
- [5]Neuron. 2021 Aug 18;109(16):2573-2589.e9.
- [6]J Exp Med. 2023 Mar 6;220(3):e20220857.
- [7]Theranostics. 2020 Jan 1;10(1):74-90.
- [8]Cancer Lett. 2022 Jun 16;215795.
- [9]Glia. 2022 Jun 30.
- [10]Glia. 2021 Feb 15.
- [11]Glia. 2021 Apr;69(4):943-953.
- [12]J Neuroinflammation. 2022 Jan 21;19(1):20.
- [13]J Neuroinflammation. 2020 Jan 23;17(1):31.
- [14]J Neurosci. 2020 May 6;40(19):3862-3879.
- [15]Cell Oncol. 2021 Feb;44(1):193-204.
- [16]Transl Psychiatry. 2020 Jan 27;10(1):32.
- [17]Front Immunol. 2022 May 13;13:866073.
- [18]Biochem Pharmacol. 2022 Feb 9;198:114952.
- [19]Biomedicines. 2022, 10(7), 1653.
- [20]Biomedicines. 2021, 9(10), 1387.
- [21]J Neurosci Res. 2021 Feb 20.
- [22]Neuropharmacology. 2020 Aug 1;172:108132.
- [23]Neuropharmacology. 2019 Apr 4;151:33-44.
- [24]Am J Physiol Cell Physiol. 2020 Sep 1;319(3):C605-C610.
- [25]Cells. 2021, 10(8), 1862
- [26]Cells. 2021, 10(4), 874.
- [27]Prog Neuropsychopharmacol Biol Psychiatry. 2020 Jul 13;101:109931.
- [28]Biomolecules. 2022 May 4;12(5):666.
- [29]Sci Rep. 2021 Aug 6;11(1):15989.
- [30]Chem Biol Interact. 2022: 110255.
- [31]Mol Pharmacol. April 5, 2022.
- [32]Life Sci. 2020 Oct 1;258:118099.
- [33]Molecules. 2022, 27(1), 297.
- [34]J Neurooncol. 2021 May 8.
- [35]Neural Regen Res. 2023.
- [36]Anti-Cancer Drug. 2022 Dec.
- [37]J Ocul Pharmacol Ther. 2020 Jun;36(5):311-319.
- [38]Research Square Preprint. 2022 Jul.
- [39]Research Square Print. 2022 Jun.
- [40]Research Square Preprint. 2021 Sep.
- [41]Karolinska Institutet. Dept of Clinical Neuroscience. 2021 Feb.
- [42]Methods Mol Biol. 2018;1711:351-398.
Summary
Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC 50 s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity [1] .
IC50 & Target
IC50: 10 nM (c-Kit), 20 nM (cFMS), 160 nM (FLT3), 350 nM (KDR), 860 nM (LCK), 880 nM (FLT1), 890 nM (NTRK3) [1]
In Vitro
Pexidartinib (PLX-3397) is a potent, selective and ATP-competitive CSF1R (cFMS) and c-Kit inhibitor, shows 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases, such as FLT3, KDR (VEGFR2), LCK, FLT1 (VEGFR1) and NTRK3 (TRKC), with IC 50 s of 160, 350, 860, 880, and 890 nM, respectively [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Pexidartinib (PLX3397; 0.25, 1 mg/kg, twice daily for 8 days) inhibits the proliferation of microglia and BrdU-positive cells in neonatal mice
[2]
.
Pexidartinib (1 mg/kg, twice daily for 8 day) shows no obvious effect on the cleaved caspase-3-positive cells in mice
[2]
.
Pexidartinib (50 mg/kg; p.o.; every second day for 3 weeks) reduces tissue macrophage levels without affecting glucose homeostasis in mice
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Neonatal mice [2] |
| Dosage: | 0.25, 1 mg/kg |
| Administration: | I.P. twice daily for 8 days |
| Result: | Decreased the number of microglia and BrdU-positive proliferative cells, but did not change the cleaved caspase-3-positive cells. |
| Animal Model: | 10-week old litter mate C57BL/6 mice (chow and high-fat diet fed mice) [4] |
| Dosage: | 50 mg/kg |
| Administration: | P.o.; every second day for 3 weeks |
| Result: | Substantially reduced macrophage numbers in adipose tissue of both chow and high-fat diet fed mice without affecting total myeloid cell levels. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03158103 | Memorial Sloan Kettering Cancer Center|Array BioPharma|Plexxikon |
Gastrointestinal Stromal Tumor (GIST)
|
April 15, 2017 | Phase 1 |
| NCT01790503 | Daiichi Sankyo, Inc.|Plexxikon |
Patients With Newly Diagnosed Glioblastoma
|
July 18, 2013 | Phase 1|Phase 2 |
| NCT04526704 | Daiichi Sankyo, Inc. |
Tenosynovial Giant Cell Tumor
|
October 20, 2020 | Phase 4 |
| NCT01217229 | Daiichi Sankyo, Inc.|Plexxikon |
Hodgkin Lymphoma
|
March 3, 2011 | Phase 2 |
| NCT01826448 | Daiichi Sankyo, Inc.|Plexxikon |
V600-mutated BRAF Unresectable Melanoma|V600-mutated BRAF Metastatic Melanoma|Stage III or Stage IV Metastatic Melanoma That Has Not Been Previously Treated With a Selective BRAF Inhibitor
|
November 5, 2013 | Phase 1 |
| NCT02472275 | Barbara Ann Karmanos Cancer Institute|National Cancer Institute (NCI) |
Stage I Prostate Adenocarcinoma|Stage II Prostate Adenocarcinoma|Stage III Prostate Adenocarcinoma
|
June 2015 | Phase 1 |
| NCT01499043 | Daiichi Sankyo, Inc.|Plexxikon |
Prostate Cancer
|
May 25, 2012 | Phase 2 |
| NCT03138759 | Daiichi Sankyo, Inc. |
Pharmacokinetics in Healthy Volunteers
|
February 27, 2017 | Phase 1 |
| NCT01349049 | Daiichi Sankyo, Inc.|Plexxikon |
Acute Myeloid Leukemia
|
November 21, 2011 | Phase 1|Phase 2 |
| NCT01349036 | Daiichi Sankyo, Inc.|Plexxikon |
Recurrent Glioblastoma
|
December 3, 2011 | Phase 2 |
| NCT02401815 | Cogent Biosciences, Inc.|Plexxikon |
Gastrointestinal Stromal Tumors
|
March 6, 2015 | Phase 1|Phase 2 |
| NCT01596751 | Hope Rugo, MD|Susan G. Komen Breast Cancer Foundation|Plexxikon|University of California, San Francisco |
Metastatic Breast Cancer
|
July 12, 2012 | Phase 1|Phase 2 |
| NCT01090570 | Plexxikon |
Rheumatoid Arthritis
|
May 2010 | Phase 1 |
| NCT02071940 | The Christie NHS Foundation Trust|Cancer Research UK|Christie Charitable Funds |
Malignant Melanoma
|
October 2015 | Phase 2 |
| NCT01042379 | QuantumLeap Healthcare Collaborative |
Breast Neoplasms|Breast Cancer|Breast Tumors|Angiosarcoma|TNBC - Triple-Negative Breast Cancer|HER2-positive Breast Cancer|HER2-negative Breast Cancer|Hormone Receptor Positive Tumor|Hormone Receptor Negative Tumor|Early-stage Breast Cancer|Locally Advanced Breast Cancer
|
March 1, 2010 | Phase 2 |
| NCT02371369 | Daiichi Sankyo, Inc. |
Pigmented Villonodular Synovitis|Giant Cell Tumors of the Tendon Sheath|Tenosynovial Giant Cell Tumor
|
May 11, 2015 | Phase 3 |
| NCT02452424 | Daiichi Sankyo, Inc.|Plexxikon|Merck Sharp & Dohme LLC |
Melanoma|Non-small Cell Lung Cancer|Squamous Cell Carcinoma of the Head and Neck|Gastrointestinal Stromal Tumor (GIST)|Ovarian Cancer
|
July 2, 2015 | Phase 1|Phase 2 |
| NCT04223635 | Daiichi Sankyo, Inc. |
Moderate Hepatic Impairment
|
January 7, 2020 | Early Phase 1 |
| NCT04703322 | Daiichi Sankyo Co., Ltd.|Daiichi Sankyo, Inc. |
Tenosynovial Giant Cell Tumor
|
March 15, 2021 | Phase 2 |
| NCT03291288 | Daiichi Sankyo, Inc. |
Drug Interaction Potential
|
February 26, 2018 | Phase 1 |
| NCT02584647 | Gulam Manji|Daiichi Sankyo, Inc.|Columbia University |
Sarcoma|Malignant Peripheral Nerve Sheath Tumors
|
November 4, 2015 | Phase 1|Phase 2 |
| NCT02734433 | Daiichi Sankyo Co., Ltd.|Daiichi Sankyo, Inc. |
Advanced Solid Tumors
|
June 2016 | Phase 1 |
| NCT02975700 | Daiichi Sankyo Co., Ltd.|Daiichi Sankyo, Inc. |
Melanoma
|
January 2017 | Not Applicable |
| NCT04488822 | Daiichi Sankyo Co., Ltd.|Daiichi Sankyo, Inc. |
Tenosynovial Giant Cell Tumor
|
September 2, 2020 | Phase 3 |
| NCT02777710 | Centre Leon Berard|AstraZeneca|Plexxikon |
Colorectal Cancer|Pancreatic Cancer|Metastatic Cancer|Advanced Cancer
|
June 2016 | Phase 1 |
| NCT01004861 | Daiichi Sankyo, Inc.|Plexxikon |
Solid Tumor
|
October 1, 2009 | Phase 1 |
| NCT01525602 | Daiichi Sankyo, Inc.|Plexxikon |
Solid Tumors
|
May 2012 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 239.34 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3934 mL | 11.9672 mL | 23.9343 mL |
| 5 mM | 0.4787 mL | 2.3934 mL | 4.7869 mL |
| 10 mM | 0.2393 mL | 1.1967 mL | 2.3934 mL |
References
- [1] DeNardo DG, et al. Leukocyte complexity predicts breast cancer survival and functionally regulates response to chemotherapy. Cancer Discov. 2011 Jun;1(1):54-67.
- [2] Kuse Y, et al. Microglia increases the proliferation of retinal precursor cells during postnatal development. Mol Vis. 2018 Jul 30;24:536-545. eCollection 2018.
- [3] Lee JH, et al. A phase I study of pexidartinib, a colony-stimulating factor 1 receptor inhibitor, in Asian patients with advanced solid tumors. Invest New Drugs. 2019 Mar 2.
- [4] Merry TL, et al. The CSF1 receptor inhibitor pexidartinib (PLX3397) reduces tissue macrophage levels without affecting glucose homeostasis in mice. Int J Obes (Lond). 2020;44(1):245-253.
Synonyms
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