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Chemical Structure| 1454585-06-8 Chemical Structure| 1454585-06-8

Structure of SR-3029
CAS No.: 1454585-06-8

Chemical Structure| 1454585-06-8

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SR-3029 is a potent and highly specific CK1δ/CK1ε inhibitor with the IC50 of 97 nM.

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Product Details of SR-3029

CAS No. :1454585-06-8
Formula : C23H19F3N8O
M.W : 480.45
SMILES Code : FC1=CC(N2C=NC3=C(NCC4=NC5=CC=C(F)C(F)=C5N4)N=C(N6CCOCC6)N=C23)=CC=C1
MDL No. :MFCD30187527
InChI Key :CEBMEQPREMCWOL-UHFFFAOYSA-N
Pubchem ID :60196195

Safety of SR-3029

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of SR-3029

DNA
Hedgehog

Isoform Comparison

Biological Activity

Target
  • CK1

    CK1δ, IC50:44 nM

    CK1ε, IC50:260 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MDA-MB-231 5-70 nM 72 hours Inhibited cell proliferation and induced apoptosis PMC4809734
UM-UC-3 5-400 nM 72 hours Inhibition of cell proliferation PMC7415672
HCT116 cells 240 nM 24 hours To study the inhibitory effect of SR-3029 on β-catenin acetylation PMC9039669
SW480 cells 240 nM 24 hours To study the inhibitory effect of SR-3029 on β-catenin acetylation PMC9039669
T24 25 nM 24 hours Upregulation of dCK expression PMC7415672
MIAPaCa-2 5-400 nM 72 hours Inhibition of cell proliferation PMC7415672
PANC-1 25 nM 24 hours Upregulation of dCK expression PMC7415672
HCT116 cells 100 nM 24 hours To evaluate the effect of SR3029 on AES protein level, results showed that SR3029 treatment increased AES protein expression. PMC7977458
HEK293T cells 0.2 μM 12 hours SR3029 increased the protein level of Axin1 and attenuated the RSPO1-induced degradation of Axin1 protein. PMC10768284
OPM2 250 nmol/L 24 hours Evaluate the anti-myeloma activity of SR-3029 on OPM2 cells, results showed SR-3029 significantly inhibited cell growth and induced apoptosis PMC10690099
MM.1S 250 nmol/L 24 hours Evaluate the anti-myeloma activity of SR-3029 on MM.1S cells, results showed SR-3029 significantly inhibited cell growth and induced apoptosis PMC10690099
H929 250 nmol/L 24 hours Evaluate the anti-myeloma activity of SR-3029 on H929 cells, results showed SR-3029 significantly inhibited cell growth and induced apoptosis PMC10690099

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice Subcutaneous MM.1S tumor xenograft model Intraperitoneal injection 20 mg/kg Daily until tumors reached 2,000 mm³ or mice became moribund Evaluate the anti-myeloma activity of SR-3029 in vivo, results showed SR-3029 significantly inhibited tumor growth and prolonged survival PMC10690099
Nude mice Orthotopic models of triple negative breast cancer Intraperitoneal injection 20 mg/kg Once daily for 48 days Significantly inhibited tumor growth and induced tumor cell apoptosis PMC4809734
Nude mice Orthotopic pancreatic tumor model Intraperitoneal injection 20 mg/kg Daily for 6 weeks Inhibited tumor growth and upregulated dCK expression PMC7415672
NPG mice Patient-derived colorectal tumor xenografts (PDTX) model Intraperitoneal injection 5 mg/kg Every 3 days for one month To evaluate the effect of SR3029 on tumor growth, results showed that SR3029 significantly inhibited tumor growth and increased AES protein expression. PMC7977458
Mouse Intravenous injection 1 mg/kg Single dose Evaluate the pharmacokinetic properties of SR-3029, with an AUC of 6.35 μM·h, a half-life of 0.90 hours, and brain penetration of 12% PMC3783656

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.41mL

2.08mL

1.04mL

20.81mL

4.16mL

2.08mL

References

 

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