Benzamide, 4-chloro-N-[(1R)-1-[cis-4-(6-fluoro-4-quinolinyl)cyclohexyl]ethyl]-
- Product Name
- Benzamide, 4-chloro-N-[(1R)-1-[cis-4-(6-fluoro-4-quinolinyl)cyclohexyl]ethyl]-
- CAS No.
- 1923844-48-7
- Chemical Name
- Benzamide, 4-chloro-N-[(1R)-1-[cis-4-(6-fluoro-4-quinolinyl)cyclohexyl]ethyl]-
- Synonyms
- BMS-986242;BMS-986242, 10 mM in DMSO;4-Chloro-N-((R)-1-(cis-4-(6-fluoroquinolin-4-yl)cyclohexyl)ethyl)benzamide;Benzamide, 4-chloro-N-[(1R)-1-[cis-4-(6-fluoro-4-quinolinyl)cyclohexyl]ethyl]-;4-chloro-N-[(1R)-1-[(1s,4S)-4-(6-fluoroquinolin-4-yl)cyclohexyl]ethyl]benzamide;glucuronidation,potent,Indoleamine 2,3-Dioxygenase (IDO),cancer,Inhibitor,BMS 986242,inhibit,BMS-986242,active,selective,orally
- CBNumber
- CB39008426
- Molecular Formula
- C24H24ClFN2O
- Formula Weight
- 410.91
- MOL File
- 1923844-48-7.mol
Benzamide, 4-chloro-N-[(1R)-1-[cis-4-(6-fluoro-4-quinolinyl)cyclohexyl]ethyl]- Property
- Boiling point:
- 593.0±40.0 °C(Predicted)
- Density
- 1.228±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 250 mg/mL (608.41 mM; Need ultrasonic)
- form
- Solid
- pka
- 14.09±0.46(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
Benzamide, 4-chloro-N-[(1R)-1-[cis-4-(6-fluoro-4-quinolinyl)cyclohexyl]ethyl]- Chemical Properties,Usage,Production
Uses
BMS-986242 is an orally active, potent and selective indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor. BMS-986242 can be used for the research of cancer[1].
Biological Activity
BMS-986242 is an orally active, potent and selective indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor. BMS-986242 can be used for the research of cancer[1]. BMS-986242 is more prone to oxidative metabolism and less susceptible to glucuronidation. BMS-986242 shows IC50>25 μM for all targets except nAChR a1 (IC50=12.3 μM) and nAChR a7 (IC50>6 μM with ~20 % max inhibition)[1]. BMS-986242 (3~30 mg/kg; p.o.; 0~24 hours) exhibits dose-proportional exposure and a statistically significant reduction in kynurenine concentration in the tumor at all three doses[1].
in vivo
BMS-986242 (3~30 mg/kg; p.o.; 0~24 hours) exhibits dose-proportional exposure and a statistically significant reduction in kynurenine concentration in the tumor at all three doses[1].
| Animal Model: | nu/nu Mouse[1] |
| Dosage: | 3~30 mg/kg |
| Administration: | P.o. |
| Result: | Exhibited dose-proportional exposure and a statistically significant reduction in kynurenine concentration in the tumor at all three doses. |
IC 50
IDO1
References
[1]. Cherney EC, et al. Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1. ACS Med Chem Lett. 2021;12(2):288-294. Published 2021 Jan 28.
Benzamide, 4-chloro-N-[(1R)-1-[cis-4-(6-fluoro-4-quinolinyl)cyclohexyl]ethyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
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