CEP-37440

Name: CEP-37440
Brand: MedChemExpress
SKU: HY-15841
Rating: 4.5 (1 reviews)

Cat. No.: HY-15841 Purity: 99.58%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	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
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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References
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Description

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.

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	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

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.

1391712-60-9

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
10 mM	0.1724 mL	0.8619 mL	1.7238 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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%

Select Batch:

Data Sheet (278 KB) SDS (392 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]

Complete Stock Solution Preparation Table

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

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.

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CEP-37440

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