Basic information Safety Supplier Related

SR 3029

Basic information Safety Supplier Related

SR 3029 Basic information

Product Name:
SR 3029
Synonyms:
  • N-((4,5-difluoro-1H-benzo[d]imidazol-2-yl)methyl)-9-(3-fluorophenyl)-2-morpholino-9H-purin-6-amine
  • SR-3029
  • N-[(6,7-Difluoro-1H-benzimidazol-2-yl)methyl]-9-(3-fluorophenyl)-2-(4-morpholinyl)-9H-purin-6-amine
  • N-((6,7-Difluoro-1H-benzo[d]imidazol-2-yl)methyl)-9-(3-fluorophenyl)-2-morpholino-9H-purin-6-amine
  • CS-2390
  • SR-3029 (SR 3029
  • SR-3029, >98%
  • 9H-Purin-6-amine, N-[(6,7-difluoro-1H-benzimidazol-2-yl)methyl]-9-(3-fluorophenyl)-2-(4-morpholinyl)-
CAS:
1454585-06-8
MF:
C23H19F3N8O
MW:
480.45
Mol File:
1454585-06-8.mol
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SR 3029 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
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SR 3029 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.

SR 3029Supplier

Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Email
info@chemlin.com.cn
Shanghai JiYi Biotechnology Co. Ltd.
Tel
13621943973
Email
sales@shjiyipharmatech.com
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Email
info@efebio.com
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Email
3008007409@qq.com
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SR 3029(1454585-06-8)Related Product Information