CEP-37440
CEP-37440 Basic information
- Product Name:
- CEP-37440
- Synonyms:
-
- CEP-37440
- 2-[[5-Chloro-2-[[(6S)-6,7,8,9-tetrahydro-6-[4-(2-hydroxyethyl)-1-piperazinyl]-1-methoxy-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-N-methylbenzamide
- 2-(5-chloro-2-{(S)-6-[4-(2-hydroxyethyl)piperazin-1-yl]-1-methoxy-6,7,8,9-tetrahydro-5H-benzocyclohepten-2-ylamino}pyrimidin-4-ylamino)-N-methylbenzamide
- (S)-2-((5-chloro-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-1-methoxy-6,7,8,9-tetrahydro-5H-benzo[7]annulen-2-yl)amino)pyrimidin-4-yl)amino)-N-methylbenzamide
- CEP37440;CEP 37440
- CS-1603
- Benzamide, 2-[[5-chloro-2-[[(6S)-6,7,8,9-tetrahydro-6-[4-(2-hydroxyethyl)-1-piperazinyl]-1-methoxy-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-N-methyl-
- inhibit,Inhibitor,Cluster of differentiation 246,PTK2,triple-negative breast cancer,inflammatory breast cancer,CEP-37440,Anaplastic lymphoma kinase,FAK1,Anaplastic lymphoma kinase (ALK),Focal adhesion kinase,CEP 37440,PTK2 protein tyrosine kinase 2,autophosphorylation kinase,CD246,FAK,ALK tyrosine kinase receptor
- CAS:
- 1391712-60-9
- MF:
- C30H38ClN7O3
- MW:
- 580.12
- EINECS:
- 200-258-5
- Product Categories:
-
- Inhibitors
- Mol File:
- 1391712-60-9.mol
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CEP-37440 Chemical Properties
- Density
- 1.300±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C(protect from light)
- solubility
- DMF: 12 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml
- form
- A crystalline solid
- pka
- 14.57±0.46(Predicted)
- color
- Light yellow to yellow
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CEP-37440 Usage And Synthesis
Uses
CEP-37440 is a highly potent, selective and orally active inhibitor of ALK.
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[2].
CEP-37440 (30 mg/kg; p.o; once, for 24 h) inhibits tyrosine phosphorylation in Sup-M2 xenografts mice[2].
CEP-37440 (55 mg/kg; p.o; once, for 24 h) inhibits FAK phosphorylation in CWR22 xenografts in Nude mice[2].
CEP-37440 (1-10 mg/kg; p.o and i.v.; CD-1 mouse, Sprague-Dawley (SD) rats) has good pharmacokinetic parameters[2].
Pharmacokinetic parameters in CD-1 mouse and Sprague-Dawley (SD) rats[2]
| PK parameter | CD-1 mouse | SD rat | |
| iv | dose (mg/kg) | 1 | 1 |
| iv | t1/2 (h) | 3.0 | 2 |
| iv | AUC0-∞ (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 | Cmax (ng/mL) | 1533 | 1340 |
| Animal Model: | SCID/Beige with Sup-M2 xenografts[2] |
| 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[2] |
| 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[2] |
| Dosage: | 55 mg/kg |
| Administration: | Oral administration; once, for 24 hours |
| Result: | Inhibited FAK phosphorylation in a time-dependent manner. |
CEP-37440Supplier
Shanghai Boyle Chemical Co., Ltd.
- Tel
- sales@boylechem.com
Chembest Research Laboratories Limited
- Tel
- +86-21-20908456
- sales@BioChemBest.com
BOC Sciences
- Tel
- 1-631-485-4226; 16314854226
- info@bocsci.com
Haoyuan Chemexpress Co., Ltd.
- Tel
- 021-58950125
- info@chemexpress.com
MedChemexpress LLC
- Tel
- 021-58955995
- sales@medchemexpress.cn