BAY-985
- CAS No.
- 2409479-29-2
- Chemical Name:
- BAY-985
- Synonyms
- BAY-985;BAY-985,IKK,BAY985,IκB kinase,melanoma,IKKε,TBK1,inhibit,I kappa B kinase,Inhibitor,BAY 985,antitumor;1-Propanone, 1-[4-[(1R)-1-[2-[[6-[6-(dimethylamino)-4-pyrimidinyl]-1H-benzimidazol-2-yl]amino]-4-pyridinyl]ethyl]-1-piperazinyl]-3,3,3-trifluoro-;(R)-1-(4-(1-(2-((6-(6-(Dimethylamino)pyrimidin-4-yl)-1H-benzo[d]imidazol-2-yl)amino)pyridin-4-yl)ethyl)piperazin-1-yl)-3,3,3-trifluoropropan-1-one
- CBNumber:
- CB55839640
- Molecular Formula:
- C27H30F3N9O
- Molecular Weight:
- 553.58
- MDL Number:
- MFCD32690108
- MOL File:
- 2409479-29-2.mol
BAY-985 price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-0112070 | BAY-985 99.87% | 2409479-29-2 | 5mg | $550 | 2021-12-16 | Buy |
ChemScene | CS-0112070 | BAY-985 99.87% | 2409479-29-2 | 10mg | $880 | 2021-12-16 | Buy |
ChemScene | CS-0112070 | BAY-985 99.87% | 2409479-29-2 | 50mg | $1950 | 2021-12-16 | Buy |
DC Chemicals | 012784 | BAY-985 | 2409479-29-2 | 002 | $1500 | 2021-12-16 | Buy |
BAY-985 Chemical Properties,Uses,Production
Biological Activity
BAY-985 is a potent and highly selective TBK1/IKKε inhibitor. It is highly potent against TBK1 (IC50 = 2 nM, low ATP assay; 30 nM, high ATP assay) and IKKε (IC50 = 2 nM) and also in mechanocellular phosphorylation of interferon regulatory factor 3 (pIRF3) assays High potency (IC50 = 74 nM) and anti-proliferative effect on SK-MEL-2 cells (IC50 = 900 nM).
in vitro
BAY-985 inhibits FLT3, RSK4, DRAK1, and ULK1 with IC 50 s of 123, 276, 311, and 7930 nM, respectively.
BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 (IRF3) with an IC 50 of 74 nM.
BAY-985 is active in cellular mechanistic assay and shows anti-proliferative activity in a few cancer cells lines with IC 50 s of 900 and 7260 nM for SK-MEL2 (NRAS and TP53 mutated) and ACHN (CDKN2A mutated) cells, respectively.
Cell Proliferation Assay
Cell Line: | ACHN and SK-MEL-2 cell lines |
Concentration: | |
Incubation Time: | td>96 hours |
Result: | Inhibited proliferation i n SK-MEL2 and ACHN cells with IC 50 s of 900 and 7260 nM, respectively. |
in vivo
BAY-985 (200 mg/kg; po; bid; 111 days) results in weak antitumor efficacy.
BAY-985 shows high clearance (CL b = 4.0 L/h/kg, ca. 95% hepatic extraction), large volume of distribution at steady state (V ss =2.9 L/kg) and a short terminal half-life (t 1 /2 =0.79 h).
Animal Model: | Female NMRI nude mice bearing SK-MEL-2 human melanoma xenograft model |
Dosage: | 200 mg/kg |
Administration: | Applied po; twice daily (bid) continuously 111 days |
Result: | Treatment resulted in weak antitumor efficacy with a T/C tumor weight ratio of 0.6. The treatment was well tolerated, with a maximum body weight loss of less than 10%. |
target
Target | Value |
TBK1 (in low ATP assay) | 2 nM |
IKKε (Cell-free assay) | 2 nM |
30 nM | |
pIRF3 (Cell-free assay) td> | 74 nM |
BAY-985 Preparation Products And Raw materials
Raw materials
Preparation Products
BAY-985 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24738 | 58 |
Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 278 | 58 |
Shanghai Topbiochem Technology Co., Ltd | 021-58170097 | info@topbiochem.com | China | 9442 | 58 |
ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3421 | 58 |
Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696,15000506266 15000506266 | China | 4121 | 55 | |
Twochem Co.Ltd | 021-58111628 15800915896 | sales@twochem.com | China | 290 | 55 |