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

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).

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CEP-37440 Chemical Structure

CEP-37440 Chemical Structure

CAS No. : 1391712-60-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 115 In-stock
Solution
10 mM * 1 mL in DMSO USD 115 In-stock
Solid
1 mg USD 36 In-stock
5 mg USD 90 In-stock
10 mg USD 160 In-stock
50 mg USD 630 In-stock
100 mg USD 1023 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

CEP-37440 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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

CEP-37440 Related Antibodies

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].

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

MedChemExpress (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.
Clinical Trial
Molecular Weight

580.12

Formula

C30H38ClN7O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (172.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.58%

COA (248 KB) LCMS (89 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7238 mL 8.6189 mL 17.2378 mL 43.0945 mL
5 mM 0.3448 mL 1.7238 mL 3.4476 mL 8.6189 mL
10 mM 0.1724 mL 0.8619 mL 1.7238 mL 4.3095 mL
15 mM 0.1149 mL 0.5746 mL 1.1492 mL 2.8730 mL
20 mM 0.0862 mL 0.4309 mL 0.8619 mL 2.1547 mL
25 mM 0.0690 mL 0.3448 mL 0.6895 mL 1.7238 mL
30 mM 0.0575 mL 0.2873 mL 0.5746 mL 1.4365 mL
40 mM 0.0431 mL 0.2155 mL 0.4309 mL 1.0774 mL
50 mM 0.0345 mL 0.1724 mL 0.3448 mL 0.8619 mL
60 mM 0.0287 mL 0.1436 mL 0.2873 mL 0.7182 mL
80 mM 0.0215 mL 0.1077 mL 0.2155 mL 0.5387 mL
100 mM 0.0172 mL 0.0862 mL 0.1724 mL 0.4309 mL
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CEP-37440 Related Classifications

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.

Keywords:

CEP-374401391712-60-9CEP37440CEP 37440Anaplastic lymphoma kinase (ALK)FAKAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246PTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseFAK1inflammatory breast cancertriple-negative breast cancerautophosphorylation kinaseInhibitorinhibitorinhibit

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