貨號	規(guī)格	價格	上海	北京	武漢	南京
S89653-5mg	99.3%	￥350.00 S89653-5mg ￥350.00 現(xiàn)貨	5 5	-	-	-
S89653-10mg	99.3%	￥530.00 S89653-10mg ￥530.00 現(xiàn)貨	5 5	-	-	-
S89653-25mg	99.3%	￥1000.00 S89653-25mg ￥1000.00 現(xiàn)貨	5 5	-	-	-
S89653-100mg	99.3%	￥2800.00 S89653-100mg ￥2800.00 現(xiàn)貨	3 3	-	-	-

產(chǎn)品介紹

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 IC50s 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

產(chǎn)品描述：

靶點：

IC50: 10 nM (c-Kit), 20 nM (cFMS), 160 nM (FLT3), 350 nM (KDR), 860 nM (LCK), 880 nM (FLT1), 890 nM (NTRK3)

體外研究：

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 IC50s of 160, 350, 860, 880, and 890 nM, respectively

體內(nèi)研究：

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. Pexidartinib hydrochloride (1 mg/kg, twice daily for 8 day) shows no obvious effect on the cleaved caspase-3-positive cells in mice. Pexidartinib hydrochloride (50?mg/kg; p.o.; every second day for 3 weeks) reduces tissue macrophage levels without affecting glucose homeostasis in mice. Animal Model: Neonatal mice 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) 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.

參考文獻(xiàn)：

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.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.201 ml	11.006 ml	22.013 ml
5 mM	0.44 ml	2.201 ml	4.403 ml
10 mM	0.22 ml	1.101 ml	2.201 ml
50 mM	0.044 ml	0.22 ml	0.44 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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Pexidartinib HCl

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