Pexidartinib hydrochloride PLX-3397 hydrochloride|cas:2040295-03-0|西域试剂

Pexidartinib hydrochloride PLX-3397 hydrochloride,99.89%

产品编号：Bellancom-16749A| CAS NO：2040295-03-0| 分子式：C₂₀H₁₆Cl₂F₃N₅| 分子量：454.28

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货号	价格	库存与货期
Bellancom-16749A	￥600.00	杭州北京（现货）
Bellancom-16749A	￥800.00	杭州北京（现货）
Bellancom-16749A	￥2400.00	杭州北京（现货）

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Pexidartinib hydrochloride PLX-3397 hydrochloride

产品介绍

Pexidartinib hydrochloride (PLX-3397 hydrochloride) 是一种有效、具有口服活性的，选择性 ATP-竞争性的集落刺激因子 1 (CSF1R 或 M-CSFR) 和 c-Kit 抑制剂，IC₅₀ 值分别为 20 和 10 nM。Pexidartinib hydrochloride 对 c-Kit 和 CSF1R 的选择性是对其他相关激酶的 10-100 倍，例如 FLT3，KDR (VEGFR2)，LCK，FLT1 (VEGFR1) 和 NTRK3 (TRKC)，IC₅₀ 值分别为 160，350，860，880 和 890 nM。Pexidartinib hydrochloride 可以诱导细胞凋亡 (apoptosis) 具有抗肿瘤活性。

生物活性

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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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^[4].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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)^[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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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)^[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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 60 mg/mL (132.08 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2013 mL	11.0064 mL	22.0129 mL
5 mM	0.4403 mL	2.2013 mL	4.4026 mL
10 mM	0.2201 mL	1.1006 mL	2.2013 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.50 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.50 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.50 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
4.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution
5.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution