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[CAS NO. 1391712-60-9] CEP-37440

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Catalog:	HY-15841
Brand:	MCE
CAS:	1391712-60-9

Overview

MDL	MFCD28009441
Molecular Weight	580.12
Molecular Formula	C₃₀H₃₈ClN₇O₃
SMILES	O=C(C1=CC=CC=C1NC2=NC(NC3=CC=C4C(CCC[C@@H](C4)N5CCN(CC5)CCO)=C3OC)=NC=C2Cl)NC

For research use only. We do not sell to patients.

Summary

CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC ₅₀ 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) ^[1] ^[2] .

IC50 & Target

IC ₅₀ :2.3 nM (FAK) and 3.5 nM (ALK) ^[2]

In Vitro

CEP-37440 (0-3000 nM; 0-192 h) decreases the proliferation of inflammatory breast cancer (IBC) cells in a dose-dependent manner ^[1] .
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 ^[1] .
CEP-37440 (0-3000 nM; Sup-M2 and Karpas-299 cells) induces proapoptotic caspases in a dose-dependent manner ^[2] .

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

Cell Viability Assay ^[1]

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 ^[1]

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.

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] .

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

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.

Animal Model:

CD-1 mouse, Sprague-Dawley (SD) rats ^[2]

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01922752	Teva Branded Pharmaceutical Products R&D, Inc.	Solid Tumors	July 2013	Phase 1

Molecular Weight

580.12

Appearance

Solid

Formula

C ₃₀ H ₃₈ ClN ₇ O ₃

CAS No.

1391712-60-9

SMILES

O=C(NC)C1=CC=CC=C1NC2=NC(NC3=CC=C4C(CCC[C@H](N5CCN(CCO)CC5)C4)=C3OC)=NC=C2Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution

* All of the co-solvents are available by MCE.

Purity & Documentation

Purity : 99.58%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (248 KB) LCMS (89 KB)

Handling Instructions (2659 KB)

References

[1]. Salem I, et, al. The effects of CEP-37440, an inhibitor of focal adhesion kinase, in vitro and in vivo on inflammatory breast cancer cells. Breast Cancer Res. 2016 Mar 24;18(1):37. [Content Brief]

[2]. Ott GR, et, al. Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK). J Med Chem. 2016 Aug 25;59(16):7478-96. [Content Brief]

[1]. Salem I, et, al. The effects of CEP-37440, an inhibitor of focal adhesion kinase, in vitro and in vivo on inflammatory breast cancer cells. Breast Cancer Res. 2016 Mar 24;18(1):37.

[2]. Ott GR, et, al. Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK). J Med Chem. 2016 Aug 25;59(16):7478-96.

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Keywords:

CEP-37440 1391712-60-9 CEP37440 CEP 37440 Anaplastic lymphoma kinase (ALK) FAK Anaplastic lymphoma kinase ALK tyrosine kinase receptor CD246 Cluster of differentiation 246 PTK2 protein tyrosine kinase 2 PTK2 Focal adhesion kinase FAK1 inflammatory breast cancer triple-negative breast cancer autophosphorylation kinase Inhibitor inhibitor inhibit

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References

[1] Salem I, et, al. The effects of CEP-37440, an inhibitor of focal adhesion kinase, in vitro and in vivo on inflammatory breast cancer cells. Breast Cancer Res. 2016 Mar 24;18(1):37.
[2] Ott GR, et, al. Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK). J Med Chem. 2016 Aug 25;59(16):7478-96.

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