CEP-37440|cas:1391712-60-9|西域试剂

CEP-37440,99.58%

产品编号：Bellancom-15841| CAS NO：1391712-60-9| 分子式：C₃₀H₃₈ClN₇O₃| 分子量：580.12

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-15841	￥900.00	杭州北京（现货）
Bellancom-15841	￥1600.00	杭州北京（现货）
Bellancom-15841	￥6300.00	杭州北京（现货）
Bellancom-15841	￥10230.00	杭州北京（现货）

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CEP-37440

产品介绍

CEP-37440 是一种口服有效的双重 FAK/ALK 抑制剂，抑制 FAK 和 ALK 的 IC₅₀ 值分别为 2.3 nM和 3.5 nM。CEP-37440 通过阻断 FAK1 (Tyr 397) 的自磷酸化激酶活性降低细胞增殖。

生物活性

CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC₅₀ values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397).

体外研究

CEP-37440 (0-3000 nM; 0-192 h) decreases the proliferation of inflammatory breast cancer (IBC) cells in a dose-dependent manner.
CEP-37440 (1000 nM; 0-120 h) decreases phospho-FAK1 (Tyr 397) and maintains its low level over time in FC-IBC02, SUM 190, and KPL4.
CEP-37440 (0-3000 nM; Sup-M2 and Karpas-299 cells) induces proapoptotic caspases in a dose-dependent manner.

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

Cell Viability Assay

Cell Line:	FC-IBC02, KPL4, SUM190, MDA-IBC03 and SUM149 cells
Concentration:	0, 300, 1000, 2000 and 3000 nM
Incubation Time:	0, 24, 48, 72, 96, 120, 144, 168, and 192 hours
Result:	Reduced the proliferation of three out of five IBC cell lines at low concentration. Inhibited the proliferation almost completely at 3000 nM concentration.

Western Blot Analysis

Cell Line:	FC-IBC02, SUM 190, and KPL4 cells
Concentration:	1000 nM
Incubation Time:	0, 48, 72, 96 and 120 hours
Result:	Decreased phospho-FAK1 by half in FC-IBC02, SUM190, and KPL4 cells after 48 hours.

体内研究
(In Vivo)

CEP-37440 (3-55 mg/kg; p.o.; b.i.d and q.d., for 12 d) inhibits breast tumor growth in Sup-M2 xenograftin SCID mice.
CEP-37440 (30 mg/kg; p.o; once, for 24 h) inhibits tyrosine phosphorylation in Sup-M2 xenografts mice.
CEP-37440 (55 mg/kg; p.o; once, for 24 h) inhibits FAK phosphorylation in CWR22 xenografts in Nude mice.
CEP-37440 (1-10 mg/kg; p.o and i.v.; CD-1 mouse, Sprague-Dawley (SD) rats) has good pharmacokinetic parameters.

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

Animal Model:	SCID/Beige with Sup-M2 xenografts
Dosage:	3 mg/kg (b.i.d), 10 mg/kg (b.i.d), 30 mg/kg (b.i.d and q.d. ), and 55 mg/kg (q.d.)
Administration:	Oral administration; b.i.d and q.d., for 12 days
Result:	Inhibited tumor growth in a dose-dependent manner.

Animal Model:	SCID/Beige with Sup-M2 xenografts and Nu/Nu mice female with Sup-M2 xenografts
Dosage:	30 mg/kg
Administration:	Oral administration; once, for 24 hours
Result:	Decreased NPM-ALK phosphorylation (>85%).

Animal Model:	Nu/Nu mice female with CWR22 xenografts
Dosage:	55 mg/kg
Administration:	Oral administration; once, for 24 hours
Result:	Inhibited FAK phosphorylation in a time-dependent manner.

Animal Model:

CD-1 mouse, Sprague-Dawley (SD) rats

Dosage:

1, 5, and 10 mg/kg

Administration:

Oral administration (5, and 10 mg/kg), intravenous injection (1 mg/kg); once

Result:

1.19

	PK parameter	CD-1 mouse	SD rat
iv	dose (mg/kg)	1	1
iv	t_1/2 (h)	3.0	2
iv	AUC_0-∞ (ng*h/mL)	1612	4005
iv	Vd (L/kg)	2.7	0.8
iv	CL (mL/min/kg)	10	4
po	dose (mg/kg)	10	5
po	C_max (ng/mL)	1533	1340
po

体内研究

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

Animal Model:	SCID/Beige with Sup-M2 xenografts
Dosage:	3 mg/kg (b.i.d), 10 mg/kg (b.i.d), 30 mg/kg (b.i.d and q.d. ), and 55 mg/kg (q.d.)
Administration:	Oral administration; b.i.d and q.d., for 12 days
Result:	Inhibited tumor growth in a dose-dependent manner.

Animal Model:	SCID/Beige with Sup-M2 xenografts and Nu/Nu mice female with Sup-M2 xenografts
Dosage:	30 mg/kg
Administration:	Oral administration; once, for 24 hours
Result:	Decreased NPM-ALK phosphorylation (>85%).

Animal Model:	Nu/Nu mice female with CWR22 xenografts
Dosage:	55 mg/kg
Administration:	Oral administration; once, for 24 hours
Result:	Inhibited FAK phosphorylation in a time-dependent manner.

Animal Model:

CD-1 mouse, Sprague-Dawley (SD) rats

Dosage:

1, 5, and 10 mg/kg

Administration:

Oral administration (5, and 10 mg/kg), intravenous injection (1 mg/kg); once

Result:

1.19

	PK parameter	CD-1 mouse	SD rat
iv	dose (mg/kg)	1	1
iv	t_1/2 (h)	3.0	2
iv	AUC_0-∞ (ng*h/mL)	1612	4005
iv	Vd (L/kg)	2.7	0.8
iv	CL (mL/min/kg)	10	4
po	dose (mg/kg)	10	5
po	C_max (ng/mL)	1533	1340
po

体内研究

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

Animal Model:	SCID/Beige with Sup-M2 xenografts
Dosage:	3 mg/kg (b.i.d), 10 mg/kg (b.i.d), 30 mg/kg (b.i.d and q.d. ), and 55 mg/kg (q.d.)
Administration:	Oral administration; b.i.d and q.d., for 12 days
Result:	Inhibited tumor growth in a dose-dependent manner.

Animal Model:	SCID/Beige with Sup-M2 xenografts and Nu/Nu mice female with Sup-M2 xenografts
Dosage:	30 mg/kg
Administration:	Oral administration; once, for 24 hours
Result:	Decreased NPM-ALK phosphorylation (>85%).

Animal Model:	Nu/Nu mice female with CWR22 xenografts
Dosage:	55 mg/kg
Administration:	Oral administration; once, for 24 hours
Result:	Inhibited FAK phosphorylation in a time-dependent manner.

Animal Model:

CD-1 mouse, Sprague-Dawley (SD) rats

Dosage:

1, 5, and 10 mg/kg

Administration:

Oral administration (5, and 10 mg/kg), intravenous injection (1 mg/kg); once

Result:

1.19

	PK parameter	CD-1 mouse	SD rat
iv	dose (mg/kg)	1	1
iv	t_1/2 (h)	3.0	2
iv	AUC_0-∞ (ng*h/mL)	1612	4005
iv	Vd (L/kg)	2.7	0.8
iv	CL (mL/min/kg)	10	4
po	dose (mg/kg)	10	5
po	C_max (ng/mL)	1533	1340
po

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (172.38 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7238 mL	8.6189 mL	17.2378 mL
5 mM	0.3448 mL	1.7238 mL	3.4476 mL
10 mM	0.1724 mL	0.8619 mL	1.7238 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 (4.31 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.31 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 (4.31 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.31 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 (4.31 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.31 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。