2. Protein Tyrosine Kinase/RTK TGF-beta/Smad Stem Cell/Wnt
  3. Anaplastic lymphoma kinase (ALK) TGF-beta/Smad TGF-β Receptor
  4. CDD-2789

CDD-2789 is a potent and selective ALK2 inhibitor with an IC50 0.54 μM and a Kd of 2.1 nM, respectively. CDD-2789 exhibits >120-fold selectivity over ALK3/5/6. CDD-2789 reduces activin A- and BMP2-induced SMAD1/5 phosphorylation in fibroblasts. CDD-2789 can be used for ALK2-related cancer research.

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

CDD-2789

CDD-2789 Chemical Structure

CAS No. : 3052084-77-9

Size Price Stock Quantity
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

CDD-2789 Related Antibodies

Top Publications Citing Use of Products

View All TGF-β Receptor Isoform Specific Products:

View All Isoforms
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CDD-2789 is a potent and selective ALK2 inhibitor with an IC50 0.54 μM and a Kd of 2.1 nM, respectively. CDD-2789 exhibits >120-fold selectivity over ALK3/5/6. CDD-2789 reduces activin A- and BMP2-induced SMAD1/5 phosphorylation in fibroblasts. CDD-2789 can be used for ALK2-related cancer research[1].

IC50 & Target[1]

ALK1

3.9 nM (Kd)

ALK2

2.1 nM (Kd)

BMPR1A

541 nM (Kd)

ALK6

254 nM (Kd)

TGFBR1

847 nM (Kd)

ACVR1

0.54 μM (IC50)

ALK1

10.07 μM (IC50)

In Vitro

CDD-2789 (1 μM) is highly selective for ALK2 and ALK1 over a panel of 403 human kinases[1].
CDD-2789 (2 h) engages with intracellular WT ALK2 (IC50 = 0.54 μM), mutant ALK2R206H (IC50 = 1.13 μM), and WT ALK1 (IC50 = 10.07 μM) in HEK293T cells, with ~19-fold selectivity for WT ALK2 over WT ALK1[1].
CDD-2789 (0.04-25 μM; 30 min) dose-dependently inhibits BMP2-, BMP6-, and BMP7-induced luciferase activity in 293 T-BRE-Luc cells[1].
CDD-2789 (1-25 μM; 30 min) dose-dependently inhibits activin A- and BMP2-induced pSMAD1/5 activation in primary FOP fibroblasts, without affecting pSMAD2/3 activation[1].
CDD-2789 (0-100 μM; 24 h) is nontoxic to HepG2 cells[1].
CDD-2789 binds to the ALK2 kinase domain active site through solvent-mediated hydrogen bonds and van der Waals contacts[1].

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

CDD-2789 Related Antibodies

Western Blot Analysis[1]

Cell Line: WT and FOP fibroblasts
Concentration: 1; 5; 25 μM
Incubation Time: 30 min
Result: Significantly inhibited activin A-induced pSMAD1/5 activation in a dose-dependent manner.
Showed no significant effect on activin A-induced pSMAD2/3 activation.
Significantly reduced BMP2-induced pSMAD1/5 activation in both WT and FOP fibroblasts at all tested concentrations.
Parmacokinetics
Species Dose Route Tmax Cmax T1/2 AUC0-t AUC0-∞ MRT0-t MRT0-∞
Mice[1] 50 mg/kg i.g. 1.75 h 4.59 μM 3.42 h 32.16 μM/L·h 32.42 μM/L·h 4.60 h 4.79 h
In Vivo

CDD-2789 (20, 30 and 50 mg/kg; p.o.; 每日给药或一日两次) does not reduce heterotopic ossification in ALK2Q207D transgenic mice[1].

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

Animal Model: CAG-Z-EGFP-ALK2Q207D transgenic mice with heterotopic
ossification (HO)[1]
Dosage: 20; 30; 50 mg/kg
Administration: i.g.; qd or BID
Result: Resulted in a Faxitron score of 2.58 for 30 mg/kg dose, compared to 1.75 for vehicle control.
Showed no reduction in heterotopic ossification formation relative to vehicle controls for 20 mg/kg and 50 mg/kg doses.
Molecular Weight

466.57

Formula

C26H34N4O4
CAS No.
Appearance

Liquid (Density: 1.228±0.14 g/cm3)

Color

Colorless to light yellow

SMILES

COC1=C(OC)C=C(C2=NC(C=CC(C(NCCCN(C)C)=O)=C3)=C3N2C4CCC4)C=C1OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 200 mg/mL (428.66 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1433 mL 10.7165 mL 21.4330 mL
5 mM 0.4287 mL 2.1433 mL 4.2866 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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: ≥ 5 mg/mL (10.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (10.72 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1433 mL 10.7165 mL 21.4330 mL 53.5825 mL
5 mM 0.4287 mL 2.1433 mL 4.2866 mL 10.7165 mL
10 mM 0.2143 mL 1.0717 mL 2.1433 mL 5.3583 mL
15 mM 0.1429 mL 0.7144 mL 1.4289 mL 3.5722 mL
20 mM 0.1072 mL 0.5358 mL 1.0717 mL 2.6791 mL
25 mM 0.0857 mL 0.4287 mL 0.8573 mL 2.1433 mL
30 mM 0.0714 mL 0.3572 mL 0.7144 mL 1.7861 mL
40 mM 0.0536 mL 0.2679 mL 0.5358 mL 1.3396 mL
50 mM 0.0429 mL 0.2143 mL 0.4287 mL 1.0717 mL
60 mM 0.0357 mL 0.1786 mL 0.3572 mL 0.8930 mL
80 mM 0.0268 mL 0.1340 mL 0.2679 mL 0.6698 mL
100 mM 0.0214 mL 0.1072 mL 0.2143 mL 0.5358 mL
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CDD-2789 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:

CDD-27893052084-77-9CDD2789CDD 2789Anaplastic lymphoma kinase (ALK)TGF-beta/SmadTGF-β ReceptorAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Transforming growth factor betaTransforming growth factor beta receptorsfibroblastsBMP2ALK1BMP6SMAD1/5fibrodysplasia ossificans progressivaHEK293T cellsHepG2 cellsALK2BMP7Inhibitorinhibitorinhibit

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