ACY-1215
- Product Name
- ACY-1215
- CAS No.
- 1316214-52-4
- Chemical Name
- ACY-1215
- Synonyms
- ACY 63;CS-583;ACY-1215;Propane-1;Ricolinostat;Rocilinostat;ACY-1215 98%;ACY-1215/ACY1215;Rocilinostat, >=99%;3-tricarboxylic acid
- CBNumber
- CB82627292
- Molecular Formula
- C24H27N5O3
- Formula Weight
- 433.5
- MOL File
- 1316214-52-4.mol
ACY-1215 Property
- Melting point:
- 189 - 191°C
- Density
- 1.239±0.06 g/cm3(Predicted)
- storage temp.
- -20°C Freezer
- solubility
- DMSO (Slightly), Methanol (Slightly)
- pka
- 9.47±0.20(Predicted)
- form
- Solid
- color
- White to Off-White
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 21531
- Product name
- ACY-1215
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $72
- Updated
- 2024/03/01
- Product number
- 21531
- Product name
- ACY-1215
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $129
- Updated
- 2024/03/01
- Product number
- 21531
- Product name
- ACY-1215
- Purity
- ≥98%
- Packaging
- 100mg
- Price
- $228
- Updated
- 2024/03/01
- Product number
- 21531
- Product name
- ACY-1215
- Purity
- ≥98%
- Packaging
- 250mg
- Price
- $494
- Updated
- 2024/03/01
- Product number
- D486990
- Product name
- 2-(Diphenylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]-5-pyrimidinecarboxamide
- Packaging
- 250mg
- Price
- $275
- Updated
- 2021/12/16
ACY-1215 Chemical Properties,Usage,Production
Description
ACY-1215 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 5 nM). It is at least 10-fold less active against other HDACs in enzymatic assays. ACY-1215 shows synergistic activity with the proteasome inhibitor bortezomib against multiple myeloma (MM) cells, inducing protracted endoplasmic reticulum stress and apoptosis. ACY-1215 combined with proteasome inhibitors suppresses tumor growth and increases survival in mice with MM and mantle cell lymphoma xenografts. A multicenter phase I trial examining ACY-1215 combined with the E3 ligase inhibitor lenalidomide and dexamethasone in multiple myeloma found inhibition of HDAC6 in vivo. ACY-1215 also diminishes liver cyst development and fibrosis in a rat model of polycystic liver disease.
Uses
This compound acts as a selective HDAC-6 (histone deacetylase) inihibitor. HDAC is linked to the transcription of DNA in cancers, including multiple myeloma (MM).
Definition
ChEBI: N-[7-(hydroxyamino)-7-oxoheptyl]-2-(N-phenylanilino)-5-pyrimidinecarboxamide is a pyrimidinecarboxylic acid.
Synthesis
1316216-07-5
1316214-52-4
Compound 6 (CAS:1316216-07-5) (2.0 g, 4.6 mmol) was taken as raw material and stirred with sodium hydroxide (2N, 20 mL) in a solvent mixture of methanol (50 mL) and dichloromethane (25 mL) for 10 minutes at 0°C. Subsequently, hydroxylamine (50%, 10 mL) pre-cooled to 0°C was added to the above mixture. The reaction mixture was continued to be stirred at room temperature for 20 minutes. Upon completion of the reaction, the solvent was removed by distillation under reduced pressure and the resulting mixture was neutralized with 1 M hydrochloric acid to produce a white precipitate. The crude product was filtered and purified by preparative high performance liquid chromatography (pre-HPLC) to give the final target product 2-(diphenylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]pyrimidine-5-carboxamide as a white solid (950 mg, 48% yield).
in vivo
Mice treated with Ricolinostat (ACY-1215), PS-341, or Ricolinostat plus PS-341 show a significant delay in tumor growth (P=0.01, P=0.006, and P<0.0001, respectively). Combined treatment with Ricolinostat and PS-341 shows significant suppression of tumor growth and significantly prolonged overall survival (OS) compare with the control group (17 days in the control vs 40 days in the combination-treated group, P<0.0001) and the Ricolinostat (ACY-1215)-treated group (22 days in the PS-341 group vs 40 days in the combination-treated group, P<0.0001). Weight loss in the combination-treated group is between 4% and 12% compare with the same-day control group values during treatment, with complete recovery after the last injection. As is observed in the plasmacytoma model, a significant therapeutic advantage is found by combining Ricolinostat with PS-341 compare with either agent alone[1].
target
HDAC6
IC 50
HDAC6: 4.7 nM (IC50); HDAC2: 48 nM (IC50); HDAC3: 51 nM (IC50); HDAC1: 58 nM (IC50); HDAC8: 100 nM (IC50); HDAC7: 1400 nM (IC50); HDAC5: 5000 nM (IC50); HDAC4: 7000 nM (IC50)
References
[1] Patent: WO2011/91213, 2011, A2. Location in patent: Page/Page column 73; 75-76
[2] Patent: WO2013/13113, 2013, A2. Location in patent: Page/Page column 70
[3] Patent: US2015/99744, 2015, A1. Location in patent: Paragraph 0237
[4] Patent: US2015/105384, 2015, A1. Location in patent: Paragraph 0406
[5] Patent: US2015/105358, 2015, A1. Location in patent: Paragraph 0396-0397
ACY-1215 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from ACY-1215 manufacturers
- Product
- ACY-1215 1316214-52-4
- Price
- US $0.00-0.00/KG
- Min. Order
- 1KG
- Purity
- 98%
- Supply Ability
- 1Ton
- Release date
- 2022-10-13
- Product
- ACY-1215 1316214-52-4
- Price
- US $0.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 2000ton
- Release date
- 2023-08-29