BAY 61-3606 (dihydrochloride)
BAY 61-3606 (dihydrochloride) Basic information
- Product Name:
- BAY 61-3606 (dihydrochloride)
- Synonyms:
-
- 2-[[7-(3,4-Dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]-3-pyridinecarboxamide dihydrochloride
- BAY 61-3606 (dihydrochloride)
- BAY 61-3606(HCl)
- BAY61-3606; BAY-61-3606; BAY-613606
- BAY61-3606 DIHYDROCHLORIDE;BAY 61-3606
- BAY 613606 dihydrochloride,Spleen tyrosine kinase,inhibit,Syk,Inhibitor,Apoptosis,BAY 61 3606 dihydrochloride
- BAY 61-3606 dihydrochloride, 10 mM in DMSO
- BAY 61-3606 dihydrochloride (BAY61-3606 dihydrochloride
- CAS:
- 648903-57-5
- MF:
- C20H20Cl2N6O3
- MW:
- 463.3172
- Mol File:
- 648903-57-5.mol
BAY 61-3606 (dihydrochloride) Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO : 7.14 mg/mL (15.41 mM; Need ultrasonic)
- form
- Yellow solid.
- color
- Off-white to yellow
BAY 61-3606 (dihydrochloride) Usage And Synthesis
Uses
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM[1]. BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell[2]. BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates[3]. Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells[4].
in vivo
Bay 61-3606 (50 mg/kg; administered twice a week for two weeks by intraperitoneal injection) alone leads to more efficacious reductions than that of TNF-related apoptosis-inducing ligand (TRAIL; 10 mg/kg) alone in MCF-7 tumor xenograft-bearing BALB/c nude mice. Bay 61-3606 administered in TRAIL combination significantly reduces the volume of the xenografted tumor[4].
| Animal Model: | Female BALB/c nude mice (5 weeks old) bearing MCF-7 tumor xenograft[4] |
| Dosage: | 50 mg/kg |
| Administration: | Injected intraperitoneally twice a week with Bay 61–3606 (50 mg/kg), TRAIL (10 mg/kg) or a combination of Bay 61-3606 (50 mg/kg) and TRAIL (10 mg/kg); TRAIL was given 2 h after the injection of Bay 61-3606; for two weeks |
| Result: | Led to efficacious reductions in tumor growth. |
References
[1] Yamamoto N, et al. The orally available spleen tyrosine kinase inhibitor 2-[7-(3,4-dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino]nicotinamide dihydrochloride (BAY 61-3606) blocks antigen-induced airway inflammation in rodents. J Pharmacol Exp Ther. 2003 Sep;306(3):1174-81. DOI:10.1124/jpet.103.052316
[2] Tümmler C, et al. SYK Inhibition Potentiates the Effect of Chemotherapeutic Drugs on Neuroblastoma Cells in Vitro. Cancers (Basel). 2019 Feb 10;11(2). pii: E202. DOI:10.3390/cancers11020202
[3] Gioia R, et al. Quantitative phosphoproteomics revealed interplay between Syk and Lyn in the resistance to AMN107 in chronic myeloid leukemia cells. Blood. 2011 Aug 25;118(8):2211-21. DOI:10.1182/blood-2010-10-313692
[4] Kim SY, et al. Bay 61-3606 Sensitizes TRAIL-Induced Apoptosis by Downregulating Mcl-1 in Breast Cancer Cells. PLoS One. 2015 Dec 31;10(12):e0146073. DOI:10.1371/journal.pone.0146073
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