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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

    CK1ε, IC50:260 nM

    CK1δ, IC50:44 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MDA-MB-231 5-70 nM 72 hours Inhibited cell proliferation and induced apoptosis Sci Transl Med. 2015 Dec 16;7(318):318ra202.
UM-UC-3 5-400 nM 72 hours Inhibition of cell proliferation Mol Cancer Ther. 2020 Aug;19(8):1623-1635.
MIAPaCa-2 5-400 nM 72 hours Inhibition of cell proliferation Mol Cancer Ther. 2020 Aug;19(8):1623-1635.
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. Theranostics. 2021 Mar 4;11(9):4421-4435.
HEK293T cells 0.2 μM 12 hours SR3029 increased the protein level of Axin1 and attenuated the RSPO1-induced degradation of Axin1 protein. Cell Commun Signal. 2024 Jan 5;22(1):14.
HCT116 cells 240 nM 24 hours To study the inhibitory effect of SR-3029 on β-catenin acetylation Front Oncol. 2022 Apr 12;12:844477.
SW480 cells 240 nM 24 hours To study the inhibitory effect of SR-3029 on β-catenin acetylation Front Oncol. 2022 Apr 12;12:844477.
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 Cancer Res. 2023 Dec 1;83(23):3901-3919.
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 Cancer Res. 2023 Dec 1;83(23):3901-3919.
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 Cancer Res. 2023 Dec 1;83(23):3901-3919.
T24 25 nM 24 hours Upregulation of dCK expression Mol Cancer Ther. 2020 Aug;19(8):1623-1635.
PANC-1 25 nM 24 hours Upregulation of dCK expression Mol Cancer Ther. 2020 Aug;19(8):1623-1635.

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 Cancer Res. 2023 Dec 1;83(23):3901-3919.
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 Sci Transl Med. 2015 Dec 16;7(318):318ra202.
Nude mice Orthotopic pancreatic tumor model Intraperitoneal injection 20 mg/kg Daily for 6 weeks Inhibited tumor growth and upregulated dCK expression Mol Cancer Ther. 2020 Aug;19(8):1623-1635.
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. Theranostics. 2021 Mar 4;11(9):4421-4435.
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% Bioorg Med Chem Lett. 2013 Aug 1;23(15):4374-80

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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