PLX647|cas:873786-09-5|西域试剂

PLX647,99.07%

产品编号：Bellancom-13838| CAS NO：873786-09-5| 分子式：C₂₁H₁₇F₃N₄| 分子量：382.38

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货号	价格	库存与货期
Bellancom-13838	￥600.00	杭州北京（现货）
Bellancom-13838	￥900.00	杭州北京（现货）
Bellancom-13838	￥2500.00	杭州北京（现货）
Bellancom-13838	￥4500.00	杭州北京（现货）

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PLX647

产品介绍

PLX647 是一种高度特异性的，具有口服活性的 FMS 和 KIT 双激酶抑制剂，IC₅₀ 分别为 28 和 16 nM。PLX647 (1 μM) 在 400 个激酶组中显示出对 FMS 和 KIT 有选择性，但 FLT3 和 KDR 除外 (IC₅₀=91 和 130 nM)。

生物活性

PLX647 is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC₅₀s of 28 and 16 nM, respectively. PLX647 shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and KDR (IC₅₀s=91 and 130 nM, respectively).

体外研究

In vitro, PLX647 potently inhibits proliferation of BCR-FMS cells, with an IC₅₀ of 92 nM. A corresponding Ba/F3 cell line expressing BCR-KIT is also quite sensitive to PLX647, with an IC₅₀ of 180 nM. PLX647 also inhibits endogenous FMS and KIT, as demonstrated by inhibition of the ligand-dependent cell lines M-NFS-60 (IC₅₀=380 nM) and M-07e (IC₅₀=230 nM), which express FMS and KIT, respectively.
PLX647 potently inhibits the growth of FLT3–ITD-expressing MV4-11 cells (IC₅₀=110 nM). PLX647 displayed minimal inhibition of the proliferation of Ba/F3 cells expressing BCR–KDR (IC₅₀=5 μM). PLX647 inhibits osteoclast differentiation with an IC₅₀ of 0.17 μM.

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

体内研究

PLX647 (40 mg/kg; p.o.; twice daily for 7 days) reduces macrophage accumulation in UUO kidney and blood monocytes.
PLX647 (40 mg/kg; p.o.; male Swiss Webster mice) reduces LPS-induced TNF-α and IL-6 release.
PLX647 (20-80 mg/kg; p.o.; daily or twice daily from 27-41 days) shows effects on collagen-induced arthritis.
PLX647 (30 mg/kg) results in significant inhibition of TRAP5b immunostaining and bone osteolysis. PLX647 (30 mg/kg BID) is able to prevent bone damage by the tumor cells.

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

Animal Model:	Male C57BL/6 mice (mouse unilateral ureter obstruction model)
Dosage:	40 mg/kg
Administration:	P.o.; twice daily for 7 days
Result:	Resulted in reduction in the levels of F4/80+ macrophages by 77%.

Animal Model:	7-9 wk old Male DBA/1J mice (Mouse collagen-induced arthritis model)
Dosage:	20 mg/kg, 80 mg/kg
Administration:	P.o.; daily (20 mg/kg) from 27-41 days, twice daily (80 mg/kg) from 27-41 days
Result:	20 mg/kg PLX647 had no initial effect on the development of severe arthritis. However, starting on day 33, no further development of disease severity was recorded, and a 30% inhibition of the macroscopic signs of arthritis was evident in clinical score on day 41. Mice treated with 80 mg/kg BID PLX647 initially shows delayed development of severe arthritic signs. Starting on day 33, the signs of arthritis began to decrease in this treatment group, reaching a maximum reversal of 76% on day 41.

体内研究

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

Animal Model:	Male C57BL/6 mice (mouse unilateral ureter obstruction model)
Dosage:	40 mg/kg
Administration:	P.o.; twice daily for 7 days
Result:	Resulted in reduction in the levels of F4/80+ macrophages by 77%.

Animal Model:	7-9 wk old Male DBA/1J mice (Mouse collagen-induced arthritis model)
Dosage:	20 mg/kg, 80 mg/kg
Administration:	P.o.; daily (20 mg/kg) from 27-41 days, twice daily (80 mg/kg) from 27-41 days
Result:	20 mg/kg PLX647 had no initial effect on the development of severe arthritis. However, starting on day 33, no further development of disease severity was recorded, and a 30% inhibition of the macroscopic signs of arthritis was evident in clinical score on day 41. Mice treated with 80 mg/kg BID PLX647 initially shows delayed development of severe arthritic signs. Starting on day 33, the signs of arthritis began to decrease in this treatment group, reaching a maximum reversal of 76% on day 41.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (65.38 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6152 mL	13.0760 mL	26.1520 mL
5 mM	0.5230 mL	2.6152 mL	5.2304 mL
10 mM	0.2615 mL	1.3076 mL	2.6152 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。-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 (6.54 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.54 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% corn oil
Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.54 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。