SR 3029

Product NameSR 3029
CAS1454585-06-8
MFC23H19F3N8O
MW480.45
EINECS
MOL File1454585-06-8.mol

Chemical Properties

Boiling point	818.7±75.0 °C(Predicted)
Density	1.62±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMF: 30 mg/ml; DMSO: 30 mg/ml
form	A solid
pka	8.76±0.30(Predicted)
color	White to pink

Usage And Synthesis

Uses

SR-3029 is a potent and selective CK1δ and CK1ε inhibitor (IC50 values are 44 and 260 nM, respectively). Exhibits selectivity for CK1δ and CK1ε over a panel of other kinases. Inhibits proliferation of melanoma and breast cancer cell lines in vitro. Also inhibits growth of breast tumor xenografts in mice.

in vivo

SR-3029 (20 mg/kg daily i.p.) exibits anti-tumor effects in rthotopic MDA-MB-231, MDA-MB-468 (TNBC), SKBR3 and BT474 (HER2+) tumor xenografts with no overt toxicity in mice. SR-3029 (20 mg/kg daily i.p.) also effectively inhibits the growth of tumor in primary patient-derived xenograft (PDX) models. In addition, SR-3029 (20 mg/kg, i.p.) strongly reduces the expression of nuclear β-catenin in tumors of mice^[2].

IC 50

CKIδ: 44 nM (IC₅₀); CDK6/cyclin D3: 427 nM (IC₅₀); CDK6/cyclin D1: 428 nM (IC₅₀); CDK4/cyclin D3: 368 nM (IC₅₀); CDK4/cyclin D1: 576 nM (IC₅₀); FLT3: 3000 nM (IC₅₀)

storage

Store at +4°C

References

[1]. Bibian M, et al. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4374-80.
[2]. Rosenberg LH, et al. Therapeutic targeting of casein kinase 1δ in breast cancer. Sci Transl Med. 2015 Dec 16;7(318):318ra202.
[3]. ELISABETH PEER. Casein Kinase 1D Encodes a Novel Drug Target in Hedgehog-GLI-Driven Cancers and Tumor-Initiating Cells Resistant to SMO Inhibition.[J]. Cancers, 2021. DOI:10.3390/cancers13164227.