Adezmapimod - CAS:152121-47-6

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Adezmapimod (Synonyms:SB 203580; RWJ 64809)

目录号 : KM2439 CAS No. : 152121-47-6 纯度 : 98%

Data Sheet SDS 产品使用指南

Adezmapimod (SB 203580) 是一种选择性的，ATP 竞争性的 p38 MAPK 抑制剂，对 SAPK2a/p38 和 SAPK2b/p38β2 的 IC₅₀ 分别为 50 nM 和 500 nM。Adezmapimod 抑制 LCK，GSK3β 和 PKBα，IC₅₀ 比 SAPK2a/p38 高 100-500 倍。Adezmapimod 不抑制 JNK 活性，是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 激活剂。

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生物活性

Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC₅₀s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC₅₀s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator.

体外研究

Adezmapimod (SB 203580) (preincubated with 0-30 μM for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2) prevents the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC₅₀ of 3-5 μM.
SB203580 blocks PKB phosphorylation (IC₅₀ 3-5 μM). SB203580 inhibitsthe phosphorylation of Ser473 in a dose-dependent manner in both CT6 and activated human T cells and IL-2-responsive BA/F3 F7 B cells.

Cell Proliferation Assay

Cell Line:	CT6, BA/F3 cell line F7, and PBMC/T cells
Concentration:	0-30 μM
Incubation Time:	Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2
Result:	Prevented the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC₅₀ of 3-5 μM.

Western Blot Analysis

Cell Line:	CT6 cells, activated human T cells, and BA/F3 F7 cells
Concentration:	0-30 μM
Incubation Time:	Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min
Result:	Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.

体内研究

Adezmapimod (SB 203580) (5 mg/kg/day; intra peritoneal injected daily for 16 consecutive days, in female atymic Nu/Nu mice) treatment, p38WT tumors show a significantly smaller tumor burden when compared with p38TM tumors that were treated in parallel.

Animal Model:	Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors
Dosage:	5 mg/kg/day
Administration:	Intra peritoneal injected daily for 16 consecutive days
Result:	After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10).

分子式

C₂₁H₁₆FN₃Os

分子量

377.43

CAS号

152121-47-6

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 : 20 mg/mL (52.99 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	2.6495 mL	13.2475 mL	26.4950 mL
5 mM	0.5299 mL	2.6495 mL	5.2990 mL
10 mM	0.2649 mL	1.3247 mL	2.6495 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： 0.5% CMC-Na/saline water

Solubility: 16.67 mg/mL (44.17 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 50% PEG300 → 50% saline

Solubility: 10 mg/mL (26.49 mM); Suspended solution; Need ultrasonic
3.

请依序添加每种溶剂： 5% DMSO → 40% PEG300 → 5% Tween-80 → 50% saline

Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution
4.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45%saline

Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic

此方案可获得 2 mg/mL (5.30 mM) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.0 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。

5.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic

此⽅案可获得 2 mg/mL (5.30 mM) 的澄清溶液。

以 1 mL ⼯作液为例，取 100 μL 20.0 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。
6.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic

此方案可获得 2 mg/mL (5.30 mM) 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 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ⽟⽶油中，混合均匀。
7.

请依序添加每种溶剂：2% DMSO → 40% PEG300 → 5% Tween-80 → 53% saline

Solubility: ≥ 1 mg/mL (2.65 mM); Clear solution
8.

请依序添加每种溶剂： 2% DMSO → 98% (20% SBE-β-CD in saline)

Solubility: ≥ 1 mg/mL (2.65 mM); Clear solution