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  4. DCLK1-IN-1

DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1+ pancreatic ductal adenocarcinoma (PDAC).

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

DCLK1-IN-1 Chemical Structure

DCLK1-IN-1 Chemical Structure

CAS No. : 2222635-15-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 325 In-stock
Solution
10 mM * 1 mL in DMSO USD 325 In-stock
Solid
1 mg USD 120 In-stock
5 mg USD 255 In-stock
10 mg USD 450 In-stock
25 mg USD 860 In-stock
50 mg USD 1370 In-stock
100 mg USD 2150 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

DCLK1-IN-1 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE DCLK1-IN-1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1+ pancreatic ductal adenocarcinoma (PDAC)[1].

Cellular Effect
Cell Line Type Value Description References
HeLa IC50
3350 nM
Compound: FMF-03-146-1; DCLK1-IN-1
Inhibition of ERK5 in human HeLa cells assessed as reduction in EGF-induced ERK5 autophosphorylation pretreated for 1 hr followed by EGF stimulation and measured after 17 mins by 32p kinase assay
Inhibition of ERK5 in human HeLa cells assessed as reduction in EGF-induced ERK5 autophosphorylation pretreated for 1 hr followed by EGF stimulation and measured after 17 mins by 32p kinase assay
[PMID: 32530623]
In Vitro

DCLK1-IN-1 shows no significant activity against ERK5, ACK, and LRRK2. DCLK1-IN-1 potently binds DCLK1 in HCT116 cells (IC50?=?279?nM). DCLK1-IN-1 significantly inhibited DCLK1, and weakly inhibited ERK5, in PATU-8988T cell lysates and live cells[1].

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

DCLK1-IN-1 Related Antibodies
In Vivo

DCLK1-IN-1 has a favorable pharmacokinetic profile in mice, with a half-life of 2.09?hours, an area under the curve of 5506?h/ng?mL and 81% oral bioavailability[1].

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

527.54

Formula

C26H28F3N7O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(CC(F)(F)F)C2=CN=C(NC3=CC=C(N4CCN(C)CC4)C=C3OC)N=C2N(C)C5=CC=CC=C15
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 : 35.71 mg/mL (67.69 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 1.8956 mL 9.4780 mL 18.9559 mL
5 mM 0.3791 mL 1.8956 mL 3.7912 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

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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: ≥ 2.08 mg/mL (3.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

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(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
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 1.8956 mL 9.4780 mL 18.9559 mL 47.3898 mL
5 mM 0.3791 mL 1.8956 mL 3.7912 mL 9.4780 mL
10 mM 0.1896 mL 0.9478 mL 1.8956 mL 4.7390 mL
15 mM 0.1264 mL 0.6319 mL 1.2637 mL 3.1593 mL
20 mM 0.0948 mL 0.4739 mL 0.9478 mL 2.3695 mL
25 mM 0.0758 mL 0.3791 mL 0.7582 mL 1.8956 mL
30 mM 0.0632 mL 0.3159 mL 0.6319 mL 1.5797 mL
40 mM 0.0474 mL 0.2369 mL 0.4739 mL 1.1847 mL
50 mM 0.0379 mL 0.1896 mL 0.3791 mL 0.9478 mL
60 mM 0.0316 mL 0.1580 mL 0.3159 mL 0.7898 mL
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DCLK1-IN-1 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:

DCLK1-IN-12222635-15-4OthersPDAClowtoxicityKRASERKsignalingselectivecancerInhibitorinhibitorinhibit

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