| Identification | Back Directory | [Name]
CEP-37440 | [CAS]
1391712-60-9 | [Synonyms]
CS-1603
CEP-37440
CEP37440;CEP 37440
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
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
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 | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C30H38ClN7O3 | [MDL Number]
MFCD28009441 | [MOL File]
1391712-60-9.mol | [Molecular Weight]
580.12 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
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