[CAS NO. 1029044-16-3] Pexidartinib

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PRODUCTS SPECIFICATIONS [1029044-16-3]

Catalog

HY-16749

Brand

MCE

CAS

1029044-16-3

DESCRIPTION [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

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

42 Publications Citing Use of MCE

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

In Vitro:

DMSO : 100 mg/mL ( 239.34 mM ; Need ultrasonic)

Preparing
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

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

In Vivo:

1.

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

Solubility: 5 mg/mL (11.97 mM); Suspended solution; Need ultrasonic
2.

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

Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution
3.

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

Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution
4.

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

Solubility: ≥ 2.08 mg/mL (4.98 mM); Clear solution

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

References

Synonyms

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

N-[5-[(5-Chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-6-(trifluoromethyl)-3-pyridinemethanamine

Pexidartinib

PLX 3397

Turalio