产品
编 号：F148065
分子式：C30H38ClN7O3
分子量：580.12
分子式：C30H38ClN7O3
分子量：580.12
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规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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询价
10mg
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询价
50mg
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询价
结构图
CAS No: 1391712-60-9
产品详情
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).
体内研究：
CEP-37440 (3-55 mg/kg；口服 bid 和 qd，持续 12 天) 抑制 Sup-M2 异种移植蛋白 SCID 小鼠的乳腺肿瘤生长。CEP-37440 (30 mg/kg；口服一次，持续 24 小时) 抑制 Sup-M2 异种移植小鼠中的酪氨酸磷酸化。CEP-37440 (55 mg/kg；口服一次，持续 24 小时) 抑制裸鼠 CWR22 异种移植肿瘤中的 FAK 磷酸化。CEP-37440 (1-10 mg/kg；po 和静脉注射；CD-1 小鼠，Sprague-Dawley (SD) 大鼠) 具有良好的药代动力学参数。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:PK parameterCD-1 mouseSD rat
ivdose (mg/kg)11
ivt1/2 (h)3.02
ivAUC0-∞ (ng*h/mL)16124005
ivVd (L/kg)2.70.8
ivCL (mL/min/kg)104
podose (mg/kg)105
poCmax (ng/mL)15331340
体外研究：
CEP-37440 (0-3000 nM；0-192 h) 以剂量依赖性方式降低炎症性乳腺癌 (IBC) 细胞的增殖。CEP-37440 (1000 nM；0-120 h) 降低磷酸化 FAK1 (Tyr 397) 并在 FC-IBC02、SUM 190 和 KPL4 中随时间保持其低水平。CEP- 37440 (0-3000 nM；Sup-M2 和 Karpas-299 细胞) 以剂量依赖性方式诱导促凋亡半胱天冬酶。
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).
体内研究：
CEP-37440 (3-55 mg/kg；口服 bid 和 qd，持续 12 天) 抑制 Sup-M2 异种移植蛋白 SCID 小鼠的乳腺肿瘤生长。CEP-37440 (30 mg/kg；口服一次，持续 24 小时) 抑制 Sup-M2 异种移植小鼠中的酪氨酸磷酸化。CEP-37440 (55 mg/kg；口服一次，持续 24 小时) 抑制裸鼠 CWR22 异种移植肿瘤中的 FAK 磷酸化。CEP-37440 (1-10 mg/kg；po 和静脉注射；CD-1 小鼠，Sprague-Dawley (SD) 大鼠) 具有良好的药代动力学参数。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:PK parameterCD-1 mouseSD rat
ivdose (mg/kg)11
ivt1/2 (h)3.02
ivAUC0-∞ (ng*h/mL)16124005
ivVd (L/kg)2.70.8
ivCL (mL/min/kg)104
podose (mg/kg)105
poCmax (ng/mL)15331340
体外研究：
CEP-37440 (0-3000 nM；0-192 h) 以剂量依赖性方式降低炎症性乳腺癌 (IBC) 细胞的增殖。CEP-37440 (1000 nM；0-120 h) 降低磷酸化 FAK1 (Tyr 397) 并在 FC-IBC02、SUM 190 和 KPL4 中随时间保持其低水平。CEP- 37440 (0-3000 nM；Sup-M2 和 Karpas-299 细胞) 以剂量依赖性方式诱导促凋亡半胱天冬酶。
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