| Identification | Back Directory | [Name]
BAY 61-3606 (dihydrochloride) | [CAS]
648903-57-5 | [Synonyms]
BAY 61-3606(HCl)
BAY 61-3606 (dihydrochloride)
BAY61-3606; BAY-61-3606; BAY-613606
BAY61-3606 DIHYDROCHLORIDE;BAY 61-3606
2-[[7-(3,4-Dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]-3-pyridinecarboxamide dihydrochloride | [Molecular Formula]
C20H20Cl2N6O3 | [MOL File]
648903-57-5.mol | [Molecular Weight]
463.317 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
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