Pexidartinib (PLX3397)

製品コード：S7818 純度：99.94%

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.

CAS No. 1029044-16-3

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 41500	国内在庫なし(納期7~10日)
10mg	JPY 29500	国内在庫なし(納期7~10日)
50mg	JPY 71500	国内在庫あり
200mg	JPY 145500	国内在庫あり
1g	JPY 295500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（104）

製品安全説明書

現在のバッチを見る：純度： 99.94%

99.94

Pexidartinib (PLX3397)と併用されることが多い化合物

Tween 80

Pexidartinib is dissolved in Tween 80 with additional solvents to provide a solution for C57BL/6 mice oral administration of the medication in drinking water.

Ni RJ, et al. Zool Res. 2023;44(3):543-555.

PEG300

Pexidartinib is dissolved in polyethylene glycol 300 (PEG300) with additional solvents to provide a solution for Swiss mice to study the role of microglia in drug abuse.

da Silva MCM, et al. Sci Rep. 2021 Aug 6;11(1):15989.

Rapamycin (Sirolimus)

PLX3397 and Rapamycin combination significantly inhibits tumor growth in malignant peripheral nerve sheath tumor (MPNST) xenografts.

Manji GA, et al. Clin Cancer Res. 2021;27(20):5519-5527.

Imatinib

PLX3397 and Imatinib inhibit malignant peripheral nerve sheath tumor (MPNST) cell proliferation in vitro.

Manji GA, et al. Clin Cancer Res. 2021;27(20):5519-5527.

Dovitinib (TKI-258)

Pexidartinib and Dovitinib combination enhances anti-glioma efficacy in the PDGF-B-driven glioma (PDG) model.

Yan D, et al. Oncogene. 2017;36(43):6049-6058.

Pexidartinib (PLX3397)関連製品

関連製品	Sotuletinib (BLZ945) GW2580 PLX5622 Edicotinib(JNJ-40346527) CSF1R-IN-1 Sulfatinib	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Cell Cycle compound library Angiogenesis Related compound Library	もっと見る

シグナル伝達経路

CSF-1Rシグナル伝達経路

CSF-1R阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
4T1 cells	Cell viability assay	0.01-100 ng/mL	24 h	Treatment with Pexidartinib (0.01-100 ng/mL) for 24 hours did not significantly affect murine 4T1 carcinoma cell number in vitro as measured by crystal violet stain.	30936739
Caco-2 cells	Cytotoxicity assay		48 h	IC50 = 5.43 μM	ChEMBL
Caco-2 cells	Cell Viability Assay		48 h	CC50 = 41.53 μM	ChEMBL
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

Kit ^[1] (Cell-free assay)	CSF-1R ^[1] (Cell-free assay)	Flt3 ^[1] (Cell-free assay)
10 nM	20 nM	160 nM

In Vitro
In vitro	In M-NFS-60, Bac1.2F5 and M-07e cells, Pexidartinib inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively. ^[1]
Kinase Assay	Kinase assay
Kinase Assay	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.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	p-c-Jun / c-Jun / p-ERK / ERK / p-MEK / MEK / p-CSF1R / CSF1R p-c-KIT (Y703) / p-FMS (Y546) / p-AKT (S473) / pS6 (S235-236) / p-ERK		28932635

In Vivo
In Vivo	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. ^[1] In C57 mice bearing GL261 tumors, Pexidartinib (p.o.) inhibits glioblastoma invasion. ^[2] In cmo mice, PLX3397 significantly attenuates autoinflammatory disease by decreasing the erosive bone lesions in tails and paws and the levels of circulating MIP-1α. ^[3] In mice bearing B16F10 melanomas, Pexidartinib (45 mg/kg, p.o.) enhances CD8-mediated immunotherapy of melanoma. ^[4]
動物実験	動物モデル	MMTV-PyMT mice
	投与量	40 mg/kg/day
	投与経路	p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT04703322	Recruiting	Tenosynovial Giant Cell Tumor	Daiichi Sankyo Co. Ltd.\|Daiichi Sankyo Inc.	March 15 2021	Phase 2
NCT04635111	Recruiting	Hepatotoxicity\|Tenosynovial Giant Cell Tumor	Daiichi Sankyo Inc.	January 7 2021	--
NCT04488822	Active not recruiting	Tenosynovial Giant Cell Tumor	Daiichi Sankyo Co. Ltd.\|Daiichi Sankyo Inc.	September 25 2020	Phase 3
NCT04223635	Completed	Moderate Hepatic Impairment	Daiichi Sankyo Inc.	January 7 2020	Early Phase 1
NCT03291288	Completed	Drug Interaction Potential	Daiichi Sankyo Inc.	February 26 2018	Phase 1

参考
[1] DeNardo DG, et al. Cancer Discov. 2011, 1(1), 54-67. [2] Coniglio SJ, et al. Mol Med. 2012, 18, 519-527. [3] Chitu V, et al. Blood. 2012, 120(15), 3126-3135. [4] Sluijter M, et al. PLoS One. 2014, 9(8), e104230. [5] Baldacchino K, et al. Exp Neurol. 2022 Aug;354:114113. + 展開

参考

+ 展開

化学情報

分子量	417.81	化学式	C₂₀H₁₅ClF₃N₅
CAS No.	1029044-16-3	SDF	Download Pexidartinib (PLX3397) SDFをダウンロードする
Smiles	C1=CC(=NC=C1CC2=CNC3=C2C=C(C=N3)Cl)NCC4=CN=C(C=C4)C(F)(F)F
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 84 mg/mL ( (201.04 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	10%DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O	7.2mg/ml	Taking the 1 mL working solution as an example, add 100 μL of 72 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 clarify; then continue to add 450 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5%DMSO 1 Corn oil	10.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 200 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	10.0mg/ml	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	0.65mg/ml	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.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

よくある質問（FAQ）

質問1:
I am going to use PLX3397 for mice experiment. but I am not sure how to dissolve it, could you tell me the detail?

回答
S7818 Pexidartinib (PLX3397) can dissolve in 5% DMSO+45% PEG 300+5% Tween 80+ddH2O at 10mg/ml.

C1=C0/X	C1:	LOG(C1):
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C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
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C8=C7/X	C8:	LOG(C8):