| Company Name: |
ShangHai Caerulum Pharma Discovery Co., Ltd.
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| Tel: |
18149758185 18149758185; |
| Email: |
sales-cpd@caerulumpharma.com |
| Products Intro: |
Product Name:BMS-986260
CAS:2001559-19-7
Purity:98% Package:10mg;100mg;1g;10g;100g;1kg
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| | BMS-986260 Basic information |
| Product Name: | BMS-986260 | | Synonyms: | BMS-986260;6-(4-(3-Chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidazol-5-yl)imidazo[1,2-b]pyridazine-3-carbonitrile;nuclear translocation,TGFβR1,BMS-986260,FOXP3 expression,MINK,Transforming growth factor beta receptors,oral,NHLF cells,BMS986260,inhibit,Inhibitor,CD25,TGF-β Receptor,pSMAD2/3,selective,BMS 986260;Imidazo[1,2-b]pyridazine-3-carbonitrile, 6-[4-(3-chloro-4-fluorophenyl)-1-(2-hydroxyethyl)-1H-imidazol-5-yl]-;BMS986260, 10 mM in DMSO | | CAS: | 2001559-19-7 | | MF: | C18H12ClFN6O | | MW: | 382.78 | | EINECS: | | | Product Categories: | | | Mol File: | 2001559-19-7.mol |  |
| | BMS-986260 Chemical Properties |
| density | 1.52±0.1 g/cm3(Predicted) | | solubility | DMSO: Sparingly soluble: 1-10 mg/ml
Ethanol: Slightly soluble: 0.1-1 mg/ml | | form | Solid | | pka | 14.46±0.10(Predicted) | | color | Light yellow to brown |
| | BMS-986260 Usage And Synthesis |
| Uses | BMS-986260, an immuno-oncology agent, is a potent, selective, and orally active TGFβR1 inhibitor (IC50=1.6 nM). BMS-986260 displays exquisite selectivity for TGFβR1 over its isozyme TGFβR2, as well as in a panel of more than 200 kinases examined. BMS-986260 inhibits TGFβ mediated nuclear translocation of pSMAD2/3 in MINK and NHLF cells lines with an IC50 of 350 nM and 190 nM, respectively[1]. | | References | [1] Velaparthi U, et al. Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent. ACS Med Chem Lett. 2020;11(2):172-178. Published 2020 Jan 28. DOI:10.1021/acsmedchemlett.9b00552
[2] GREGORY D. RAK. Intermittent dosing of the transforming growth factor beta receptor 1 inhibitor, BMS-986260, mitigates class-based cardiovascular toxicity in dogs but not rats[J]. Journal of Applied Toxicology, 2020, 40 7: 931-946. DOI: 10.1002/jat.3954 |
| | BMS-986260 Preparation Products And Raw materials |
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