Pexidartinib (PLX3397)

製品コードS7818 バッチS781811

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	83 mg/mL (198.65 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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 inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively. ^[1]
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]

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 inhibits the CSF1-dependent proliferation with IC50 of 0.44 μM, 0.22 μMand 0.1 μM, respectively. ^[1]

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]

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 PLX3397.
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

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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：

The aging mouse CNS is protected by an autophagy-dependent microglia population promoted by IL-34 [ Nat Commun, 2024, 15(1):383]	PubMed: 38195627
Host-functionalization of macrin nanoparticles to enable drug loading and control tumor-associated macrophage phenotype [ Front Immunol, 2024, 15:1331480]	PubMed: 38545103
Microglia-endothelial cross-talk regulates diabetes-induced retinal vascular dysfunction through remodeling inflammatory microenvironment [ iScience, 2024, 27(3):109145]	PubMed: 38414848
Colony stimulating factor-1 (CSF-1) signalling is predictive of response to immune checkpoint inhibitors in advanced non-small cell lung cancer [ Lung Cancer, 2024, 188:107447]	PubMed: 38176297
Engineering an inhibitor-resistant human CSF1R variant for microglia replacement [ J Exp Med, 2023, 220(3)e20220857]	PubMed: 36584406
Polyoxazoline-Based Nanovaccine Synergizes with Tumor-Associated Macrophage Targeting and Anti-PD-1 Immunotherapy against Solid Tumors [ Adv Sci (Weinh), 2023, 10(25):e2300299]	PubMed: 37434063
The type-I interferon response potentiates seeded tau aggregation and exacerbates tau pathology [ Alzheimers Dement, 2023, 10.1002/alz.13493]	PubMed: 37849026
Repopulated retinal microglia promote Müller glia reprogramming and preserve visual function in retinal degenerative mice [ Theranostics, 2023, 13(5):1698-1715]	PubMed: 37056562
Meningeal macrophages inhibit chemokine signaling in pre-tumor cells to suppress mouse medulloblastoma initiation [ Dev Cell, 2023, 10.1038/s41418-023-01234-w]	PubMed: 37774709
ZIC2 induces pro-tumor macrophage polarization in nasopharyngeal carcinoma by activating the JUNB/MCSF axis [ Cell Death Dis, 2023, 14(7):455]	PubMed: 37479694

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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。

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