PCI-24781An HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 inhibitor

PCI-24781 (CAS 783355-60-2)

PCI-24781 | CAS 783355-60-2 is rated 5.0 out of 5 by 1.
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Application: An HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 inhibitor
CAS Number: 783355-60-2
Purity: ≥98%
Molecular Weight: 397.42
Molecular Formula: C21H23N3O5
* Refer to Certificate of Analysis for lot specific data (including water content).
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PCI-24781 is a broad spectrum hydroxamic acid-based inhibitor of HDAC that shows antitumor activity in vitro. PCI-24781 inhibited pure recombinant HDAC1 with a Ki of 0.007 Mmol/L, as well as HDAC2, HDAC3/SMRT, HDAC6, HDAC8, and HDAC10 in the nanomolar range. Antitumor activity of PCI-24781 was observed in all 10 tumor cell lines tested, with GI50% values ranging from 0.15 to 3.09 μmol/L.

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in water (<1 mg/ml at 25 °C), DMSO (80 mg/ml at 25 °C), ethanol (<1 mg/ml at 25 °C), and methanol (sparingly).
Storage :
Store at -20° C
Melting Point :
200-202 °C (dec.)
Boiling Point :
670.41 °C (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.62 (Predicted)
Ki Data :
HDAC1: Ki= 7 nM; HDAC3: Ki= 8.2 nM; HDAC6: Ki= 17 nM; HDAC2: Ki= 19 nM
pK Values :
pKb: 7.49 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
11749858
MDL Number :
MFCD10565969
SMILES :
CN(C)CC1=C(OC2=CC=CC=C21)C(=O)NCCOC3=CC=C(C=C3)C(=O)NO

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Certificate of Analysis

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Rated 5 out of 5 by from Choy et al Choy et al. (PubMed ID 25536954) found that the HDAC inhibitor PCI-24781 (abexinostat) blocked histone acetylation in peripheral blood mononuclear cells of patients with metastatic sarcoma. -SCBT Publication Review
Date published: 2015-03-03
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