ACY-1215 free base · Synonyms: Ricolinostat | Rocilinostat

Ricolinostat is a potent and selective HDAC6 inhibitor.

For research use only. Not for human or veterinary use.

Target HDAC Apoptosis

Research area Cancer

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Data Sheet SDS COA

ACY-1215 structure

CAS No.: 1316214-52-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
1 g	USD 558.00	BP-01866-1g	In stock	Get quote
5 g	USD 2,058.00	BP-01866-5g	In stock	Get quote
10 g	Inquire	BP-01866-10g	In stock	Inquire

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Description

Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.

Biological activity

In Vitro Ricolinostat (ACY-1215) has slight activity against HDAC8 (IC50=0.1 μM), and has minimal activity (IC50>1 μM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2. The effect of Ricolinostat (ACY-1215) on multiple myeloma (MM) cell viability is determined with MTT assays using MM cell lines. Exposure of MM cell lines for 48 hours results in dose-dependent decreased viability, with IC50 values ranging from 2-8μM. Ricolinostat (ACY-1215) demonstrates significant activity in the MM PS-341-resistant cell line (ANBL-6.BR), demonstrating the ability of Ricolinostat (ACY-1215) to overcome PS-341 resistance. 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.

Identifiers

SMILES: Cl.ONC(=O)CCCCCCNC(=O)C1=CN=C(N=C1)N(C1=CC=CC=C1)C1=CC=CC=C1
InChIKey: QHVNXNABQMIUFB-UHFFFAOYSA-N

Specifications

MW (average): 469.9640
Formula: C₂₄H₂₈ClN₅O₃
CAS No.: 1316214-52-4
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Santo L, et al. Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with PS-341 in multiple myeloma. Blood. 2012 Mar 15;119(11):2579-89.

Same target

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Same research area

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