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[CAS NO. 2040295-03-0] Pexidartinibhydrochloride

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Catalog:	HY-16749A
Brand:	MCE
CAS:	2040295-03-0

Overview

MDL	-
Molecular Weight	454.28
Molecular Formula	C20H16Cl2F3N5
SMILES	FC(C1=CC=C(CNC2=NC=C(CC3=CNC4=NC=C(Cl)C=C43)C=C2)C=N1)(F)F.Cl

For research use only. We do not sell to patients.

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 hydrochloride (PLX-3397 hydrochloride) 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 hydrochloride exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib hydrochloride induces cell apoptosis and has anti-cancer 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 hydrochloride (PLX-3397 hydrochloride) 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 hydrochloride (0.25, 1 mg/kg, i.p., twice daily for 8 days) inhibits the proliferation of microglia and BrdU-positive cells in neonatal mice ^[2] .
Pexidartinib hydrochloride (1 mg/kg, twice daily for 8 day) shows no obvious effect on the cleaved caspase-3-positive cells in mice ^[2] .
Pexidartinib hydrochloride (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
NCT02401815	Cogent Biosciences, Inc.\|Plexxikon	Gastrointestinal Stromal Tumors	March 6, 2015	Phase 1\|Phase 2
NCT02975700	Daiichi Sankyo Co., Ltd.\|Daiichi Sankyo, Inc.	Melanoma	January 2017	Not Applicable
NCT02584647	Gulam Manji\|Daiichi Sankyo, Inc.\|Columbia University	Sarcoma\|Malignant Peripheral Nerve Sheath Tumors	November 4, 2015	Phase 1\|Phase 2
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
NCT01090570	Plexxikon	Rheumatoid Arthritis	May 2010	Phase 1
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
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
NCT01217229	Daiichi Sankyo, Inc.\|Plexxikon	Hodgkin Lymphoma	March 3, 2011	Phase 2
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
NCT02777710	Centre Leon Berard\|AstraZeneca\|Plexxikon	Colorectal Cancer\|Pancreatic Cancer\|Metastatic Cancer\|Advanced Cancer	June 2016	Phase 1
NCT01499043	Daiichi Sankyo, Inc.\|Plexxikon	Prostate Cancer	May 25, 2012	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
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
NCT03158103	Memorial Sloan Kettering Cancer Center\|Array BioPharma\|Plexxikon	Gastrointestinal Stromal Tumor (GIST)	April 15, 2017	Phase 1
NCT04488822	Daiichi Sankyo Co., Ltd.\|Daiichi Sankyo, Inc.	Tenosynovial Giant Cell Tumor	September 2, 2020	Phase 3
NCT02734433	Daiichi Sankyo Co., Ltd.\|Daiichi Sankyo, Inc.	Advanced Solid Tumors	June 2016	Phase 1
NCT02071940	The Christie NHS Foundation Trust\|Cancer Research UK\|Christie Charitable Funds	Malignant Melanoma	October 2015	Phase 2
NCT01349049	Daiichi Sankyo, Inc.\|Plexxikon	Acute Myeloid Leukemia	November 21, 2011	Phase 1\|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
NCT01004861	Daiichi Sankyo, Inc.\|Plexxikon	Solid Tumor	October 1, 2009	Phase 1
NCT01790503	Daiichi Sankyo, Inc.\|Plexxikon	Patients With Newly Diagnosed Glioblastoma	July 18, 2013	Phase 1\|Phase 2
NCT01525602	Daiichi Sankyo, Inc.\|Plexxikon	Solid Tumors	May 2012	Phase 1
NCT01349036	Daiichi Sankyo, Inc.\|Plexxikon	Recurrent Glioblastoma	December 3, 2011	Phase 2
NCT04223635	Daiichi Sankyo, Inc.	Moderate Hepatic Impairment	January 7, 2020	Early Phase 1
NCT03138759	Daiichi Sankyo, Inc.	Pharmacokinetics in Healthy Volunteers	February 27, 2017	Phase 1
NCT04526704	Daiichi Sankyo, Inc.	Tenosynovial Giant Cell Tumor	October 20, 2020	Phase 4

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 60 mg/mL ( 132.08 mM ; Need ultrasonic)

H ₂ O : < 0.1 mg/mL (ultrasonic) (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2013 mL	11.0064 mL	22.0129 mL
5 mM	0.4403 mL	2.2013 mL	4.4026 mL
10 mM	0.2201 mL	1.1006 mL	2.2013 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution
4.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution
5.

Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

* All of the co-solvents are available by MCE.

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.

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