1. Protein Tyrosine Kinase/RTK
  2. Anaplastic lymphoma kinase (ALK)
    FAK
  3. CEP-37440

CEP-37440 

Cat. No.: HY-15841 Purity: 99.58%
COA Handling Instructions

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).

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

CEP-37440 Chemical Structure

CEP-37440 Chemical Structure

CAS No. : 1391712-60-9

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 115 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 115 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
50 mg USD 630 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1023 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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Description

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)[1][2].

IC50 & Target

IC50:2.3 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 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
po
Clinical Trial
Molecular Weight

580.12

Formula

C30H38ClN7O3

CAS No.
SMILES

O=C(NC)C1=CC=CC=C1NC2=NC(NC3=CC=C4C(CCC[[email protected]](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
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
CEP-37440
Cat. No.:
HY-15841
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