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Chemical Structure| 627536-09-8 Chemical Structure| 627536-09-8

Structure of SD-208
CAS No.: 627536-09-8

Chemical Structure| 627536-09-8

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SD-208 is a potent, orally active ATP-competitive transforming growth factor-β receptor 1 (TGF-βRI) inhibitor (IC50= 49 nM) and displays > 100-fold and > 17-fold selectivity over TGF-βRII and other common kinases respectively.

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Product Details of SD-208

CAS No. :627536-09-8
Formula : C17H10ClFN6
M.W : 352.75
SMILES Code : FC1=CC=C(Cl)C=C1C2=NC(NC3=CC=NC=C3)=C4N=CC=NC4=N2
MDL No. :MFCD11519969
InChI Key :BERLXWPRSBJFHO-UHFFFAOYSA-N
Pubchem ID :10316032

Safety of SD-208

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • TGFβRI/ALK5

    TGF-βRI (ALK5), IC50:48 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2 liver cells 1 or 5 μM 1 hour To evaluate whether SD-208 affects MCT-induced megalocytosis in liver cells, results showed that SD-208 did not affect MCT-induced megalocytosis. PMC2292828
1205Lu human melanoma cells 0.5 μM 1 hour SD-208 dose-dependently inhibited TGF-β-induced Smad3 phosphorylation PMC3225124
bone marrow-derived dendritic cells (BMDCs) 100 µM 24 hours To evaluate the effect of DA-L-DSA on dendritic cell maturation, it was found that DA-L-DSA-treated dendritic cells expressed CD80/86 similar to the LPS-treated group, indicating effective promotion of dendritic cell maturation. PMC11423174
1205Lu human melanoma cells 1 μM 24 hours SD-208 reduced the capacity of 1205Lu human melanoma cells to invade Matrigel? PMC3225124
Adult rat cardiac fibroblasts 3 µM 4 days SD-208 inhibited fibroblast differentiation into myofibroblasts, as evidenced by the absence of stress fibers, low α-SMA expression, and high proliferation levels. PMC3928002

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice murine melanoma model and spontaneous breast cancer metastasis model subcutaneous injection 20 μg administered on days 7 and 10 post-tumor inoculation To evaluate the antitumor and antimetastatic effects of DA-L-DSA in melanoma and breast cancer models, it was found that DA-L-DSA significantly reduced tumor volume and decreased the number of metastatic nodules in the breast cancer model. PMC11423174
Sprague-Dawley rats Monocrotaline-induced pulmonary hypertension model Oral gavage 20 mg/kg or 60 mg/kg Twice daily for 4 weeks To evaluate the effect of SD-208 on monocrotaline-induced pulmonary hypertension, results showed that SD-208 significantly attenuated the development of PH and reduced pulmonary vascular remodeling. PMC2292828
Mice Myocardial infarction model Intraperitoneal injection 10 mg/kg Once daily for 1 month SD-208 significantly reduced RyR2 phosphorylation, oxidation/nitrosylation, and enabled rebinding of calstabin2 to the channels, reducing ER Ca2+ leak and improving cognitive function in MI mice. PMC10400432
Nude mice human melanoma bone metastasis model Oral gavage 60 mg/kg/day daily for 5 weeks SD-208 significantly reduced osteolytic lesion area and increased survival in mice PMC3225124
C57BL/6 mice DMM-induced osteoarthritis model Intraarticular injection 20 μM Twice a week for 8 weeks To investigate the effect of PPM1A inhibition on OA progression, results showed PPM1A deletion or inhibition significantly alleviated cartilage degeneration and subchondral sclerosis PMC9926971
Mouse RPS19-insufficient mouse model In vitro culture 5 µM 8 days To evaluate the ability of SD208 to increase erythropoiesis in mouse DBA models, results showed that SD208 significantly improved erythroid expansion in RPS19-insufficiency. PMC7334220

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.83mL

0.57mL

0.28mL

14.17mL

2.83mL

1.42mL

28.35mL

5.67mL

2.83mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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