W-7 hydrochloride - CAS:61714-27-0

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W-7 hydrochloride

目录号 : KM7465 CAS No. : 61714-27-0 纯度 : 98%

Data Sheet 产品使用指南

W-7 hydrochloride 是一种选择性的钙调蛋白 (calmodulin) 拮抗剂。W-7 hydrochloride 抑制 Ca²⁺-钙调蛋白依赖性磷酸二酯酶 (phosphodiesterase) 和肌球蛋白轻链激酶 (myosin light chain kinase)，IC₅₀ 值分别为 28 μM 和 51 μM。W-7 hydrochloride 可诱导细胞凋亡 (apoptosis)，并具有抗癌活性。

规格	价格	是否有货
25mg		In-stock
50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

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生物活性

W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC₅₀ values of 28 μM and 51 µM, respectively. W-7 hydrochloride induces apoptosis and has antitumor activity.

体外研究

W-7 is distributed mainly in the cytoplasm, and inhibits proliferation of Chinese hamster ovary K1 (CHO-K1) cells. W-7 selectively blocks the phase of the cell cycle (G1/S boundary phase) in a manner. 25 μM W-7 arrests the growth of the cells at the G1/S boundary phase of the cell cycle.
W-7 (100 μM) exhibits a similar extent of antagonism between the contractile responses to carbachol and KCl. The increase in myosin light chain (P-LC) phosphate content in response to 1-min stimulation with 10 μM carbachol is inhibited by W-7. W-7 antagonizes the smooth muscle contraction through the inhibition of the initial increase in the P-LC phosphorylation.
Treatment with W-7 results in the dose-dependent inhibition of cell proliferation in various human multiple myeloma cell lines. W-7 induces G1 phase cell cycle arrest by downregulating cyclins and upregulating p21cip1. W-7 induces apoptosis via caspase activation; this occurred partly through the elevation of intracellular calcium levels and mitochondrial membrane potential depolarization and through inhibition of the STAT3 phosphorylation and subsequent downregulation of Mcl-1 protein.
W-7 competitively inhibits Ca/calmodulin-dependent phosphodiesterase with a K_i value of 300 μM.

体内研究

W-7 (3 mg/kg; intraperitoneal injection; on 5 consecutive days per week; female BALB/c nu mice) treatment significantly reduces tumor growth in a murine MM model.

Animal Model:	Female BALB/c nu mice (6-week-old) injected with RPMI 8226 cells
Dosage:	3 mg/kg
Administration:	Intraperitoneal injection; on 5 consecutive days per week
Result:	Significantly reduced tumor growth in a murine MM model.

分子式

C₁₆H₂₂Cl₂N₂O₂S

分子量

377.33

CAS号

61714-27-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 250 mg/mL (662.55 mM; Need ultrasonic)

H₂O : 1.43 mg/mL (3.79 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6502 mL	13.2510 mL	26.5020 mL
5 mM	0.5300 mL	2.6502 mL	5.3004 mL
10 mM	0.2650 mL	1.3251 mL	2.6502 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: ≥ 2.08 mg/mL (5.51 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.51 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.51 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.51 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.51 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.51 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。