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.
Registration of APIs CMC information required for an IND
IND and NDA support Drug master files (DMF) filing
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; |
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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