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CAS號	152121-47-6	產地	進口
級別	其他

注：本產品僅用于科研，不可用于臨床

Adezmapimod抑制劑

Adezmapimod (SB 203580) 是一種選擇性的，ATP 競爭性的 p38 MAPK 抑制劑，對 SAPK2a/p38 和 SAPK2b/p38β2 的 IC₅₀ 分別為 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，是一種自噬 (autophagy) 和線粒體自噬 (mitophagy) 激活劑。

Adezmapimod抑制劑 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

IC₅₀ & Target^[1]

p38

50 nM (IC₅₀)

p38β2

500 nM (IC₅₀)

體外研究
(In Vitro)

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^[1].
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^[1].

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

Cell Proliferation Assay^[1]

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.

體內研究
(In Vivo)

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^[1].

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

Animal Model:	Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors^[1]
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).

分子量

377.43

性狀

Solid

Formula

C₂₁H₁₆FN₃OS

CAS 號

152121-47-6

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

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

溶解性數(shù)據(jù)

In Vitro:

DMSO : 20 mg/mL (52.99 mM; ultrasonic and warming and heat to 60°C)

配制儲備液

濃度溶劑體積質量	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

請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內使用，-20°C 儲存時，請在 1 個月內使用。

In Vivo:

請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨浮Ｒ韵氯芙夥桨付颊埾劝凑?nbsp;In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 0.5% CMC-Na/saline water
Solubility: 16.67 mg/mL (44.17 mM); Suspended solution; Need ultrasonic
2.

請依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic
4.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic
5.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic