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Romidepsin

Romidepsin is a selective inhibitor of histone deacetylase, approved in the US in 2009 for the treatment of cutaneous T-cell lymphoma (CTCL) or/and peripheral T-cell lymphoma (PTCL) in patients who have received at least one prior systemic therapy. These indications are based on response rate. Clinical benefit such as improvement in overall survival has not been demonstrated.

Designed for biological research and industrial applications, not intended for individual clinical or medical purposes.

CAT No: 10-101-186

CAS No:128517-07-7

Synonyms/Alias:Romidepsin; FK 228; 128517-07-7; AKOS024457654; KB-80417; Cyclo[(2Z)-2-amino-2-butenoyl-L-valyl-(3S;4E)-3-hydroxy-7-mercapto-4-heptenoyl-D-valyl-D-cysteinyl]; cyclic (3-5) disulfide;

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cGMP Peptide
  • Registration of APIs
  • CMC information required for an IND
  • IND and NDA support
  • Drug master files (DMF) filing
M.F/Formula
C24H36N4O6S2
M.W/Mr.
540.69584
Labeling Target
Histone deacetylase
Application
Romidepsin is for the treatment of cutaneous T-cell lymphoma (CTCL) or/and peripheral T-cell lymphoma (PTCL) in patients who have received at least one prior systemic therapy. These indications are based on response rate. Clinical benefit such as improvement in overall survival has not been demonstrated.
Appearance
white to off-white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Activity
Inhibitor
Biological Activity
Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.
Areas of Interest
Cutaneous T-cell lymphoma; peripheral T-cell lymphoma
Functions
Transcription regulatory region sequence-specific dna binding
Target
HDAC
Source#
Synthetic
Long-term Storage Conditions
Soluble in DMSO, not in water
Shipping Condition
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.
Short-term Storage Conditions
Dry, dark and at 0 - 4 °C
Solubility
-20 °C
Organism
Human
InChI
InChI=1S/C24H36N4O6S2/c1-6-16-21(30)28-20(14(4)5)24(33)34-15-9-7-8-10-35-36-12-17(22(31)25-16)26-23(32)19(13(2)3)27-18(29)11-15/h6-7,9,13-15,17,19-20H,8,10-12H2,1-5H3,(H,25,31)(H,26,32)(H,27,29)(H,28,30)/b9-7+,16-6-/t15-,17-,19-,20+/m1/s1
InChI Key
OHRURASPPZQGQM-GCCNXGTGSA-N
Isomeric SMILES
C/C=C\1/C(=O)N[C@H](C(=O)O[C@H]\2CC(=O)N[C@@H](C(=O)N[C@H](CSSCC/C=C2)C(=O)N1)C(C)C)C(C)C
BoilingPoint
942.8±65.0 °C at 760 mmHg
ShelfLife
>2 years if stored properly
Melting Point
N/A

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