Pexidartinib (PLX3397)

製品コードS7818 バッチS781815

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₀H₁₅ClF₃N₅

分子量

417.81

CAS No.

1029044-16-3

Solubility (25°C)*

体外

DMSO

84 mg/mL (201.04 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	10.000mg/ml (23.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.650mg/ml (1.56mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Pexidartinib (PLX3397) is an oral, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3.
in vitro	In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib (PLX3397) inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively.
in vivo	In MMTV-PyMT mice, Pexidartinib (PLX3397) (40 mg/kg, p.o.) significantly inhibits both steady-state and PTX-induced tumor infiltration by CD45+CD11b+Ly6C−Ly6G−F4/80+. This compound/PTX therapy also results in a significant reduction in CD31+ vessel density within mammary tumors, paralleling induction of apoptosis and necrosis. In C57 mice bearing GL261 tumors, this compound (p.o.) inhibits glioblastoma invasion. In cmo mice, this chemical significantly attenuates autoinflammatory disease by decreasing the erosive bone lesions in tails and paws and the levels of circulating MIP-1α. In mice bearing B16F10 melanomas, this compound (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma.

製品説明

Pexidartinib (PLX3397) is an oral, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Pexidartinib (PLX3397) induces apoptosis and necrosis with antitumor activity. Phase 3.

in vitro

In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib (PLX3397) inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively.

in vivo

In MMTV-PyMT mice, Pexidartinib (PLX3397) (40 mg/kg, p.o.) significantly inhibits both steady-state and PTX-induced tumor infiltration by CD45+CD11b+Ly6C−Ly6G−F4/80+. This compound/PTX therapy also results in a significant reduction in CD31+ vessel density within mammary tumors, paralleling induction of apoptosis and necrosis.

In C57 mice bearing GL261 tumors, this compound (p.o.) inhibits glioblastoma invasion.

In cmo mice, this chemical significantly attenuates autoinflammatory disease by decreasing the erosive bone lesions in tails and paws and the levels of circulating MIP-1α.

In mice bearing B16F10 melanomas, this compound (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma.

プロトコル(参考用のみ)

キナーゼアッセイ	Kinase assay
キナーゼアッセイ	PLX3397 is identified as a potent CSF-1R and c-KIT kinase inhibitor by using a Scaffold- and X-ray structure-based discovery approach. The IC50 data are from SelectScreen™ profiling service.
細胞アッセイ	細胞株	Myelinating cultures
	濃度	1 uM
	反応時間
	実験の流れ	Myelinating cultures were treated with hemin or vehicle control in the absence or presence of this compound.
動物実験	動物モデル	MMTV-PyMT mice
	投薬量	40 mg/kg/day
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/22039576/
https://pubmed.ncbi.nlm.nih.gov/22294205/
https://pubmed.ncbi.nlm.nih.gov/22923495/

https://pubmed.ncbi.nlm.nih.gov/25110953/
https://pubmed.ncbi.nlm.nih.gov/35569511/

+ 展开

カスタマーフィードバック

: Data from [Data independently produced by , , Nat Commun, 2017, 8:14293]

: Data from [Data independently produced by , , Clin Cancer Res, 2017, 23(20):6021-6030]

: Data from [Data independently produced by , , Brain Behav Immun, 2018, 68:248-260]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Small intestinal γδ T17 cells promote SAE through STING/C1q-induced microglial synaptic pruning in male mice [ Nat Commun, 2025, 16(1):6779]	PubMed: 40702081
Targeting C1q prevents microglia-mediated synaptic removal in neuropathic pain [ Nat Commun, 2025, 16(1):4590]	PubMed: 40382320
Microglia replacement by peripheral delivery of CSF1R inhibitor-resistant hematopoietic cells [ Mol Ther, 2025, S1525-0016(25)00871-8]	PubMed: 41232525
Stress induces behavioral disorders by promoting microglial phagocytosis via decreasing neuronal Dkk3 [ Mol Psychiatry, 2025, 30(12):5731-5748]	PubMed: 41136744
Exosome-mediated microglia-astrocyte interactions drive neuroinflammation in Parkinson's disease with Peli1 as a potential therapeutic target [ Pharmacol Res, 2025, 219:107908]	PubMed: 40816423
Deciphering the preeclampsia-specific immune microenvironment and the role of pro-inflammatory macrophages at the maternal-fetal interface [ Elife, 2025, 13RP100002]	PubMed: 40152904
Macrophage polarization, inflammatory monocytes, and impaired MDSCs are associated with murine and human immune aplastic anemia [ J Leukoc Biol, 2025, 117(6)qiaf073]	PubMed: 40411822
Depletion of HSP60 in Microglia Leads to Synaptic Dysfunction and Depression-Like Behaviors Through Enhanced Synaptic Pruning in Male Mice [ CNS Neurosci Ther, 2025, 31(4):e70394]	PubMed: 40237297
C3/C3aR Bridges Spinal Astrocyte-Microglia Crosstalk and Accelerates Neuroinflammation in Morphine-Tolerant Rats [ CNS Neurosci Ther, 2025, 31(1):e70216]	PubMed: 39801259
Mechanistic study of pexidartinib-induced toxicity in human hepatic cells [ Chem Biol Interact, 2025, 419:111641]	PubMed: 40617559

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。