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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.

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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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M.F/FormulaC24H36N4O6S2
M.W/Mr.540.69584
Labeling TargetHistone deacetylase
ApplicationRomidepsin 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.
Appearancewhite to off-white solid powder
Purity>98% (or refer to the Certificate of Analysis)
ActivityInhibitor
Biological ActivityRomidepsin (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 InterestCutaneous T-cell lymphoma; peripheral T-cell lymphoma
FunctionsTranscription regulatory region sequence-specific dna binding
TargetHDAC
Source#Synthetic
Long-term Storage ConditionsSoluble in DMSO, not in water
Shipping ConditionShipped 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 ConditionsDry, dark and at 0 - 4 °C
Solubility-20 °C
OrganismHuman
InChIInChI=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 KeyOHRURASPPZQGQM-GCCNXGTGSA-N
Isomeric SMILESC/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
BoilingPoint942.8±65.0 °C at 760 mmHg
ShelfLife>2 years if stored properly
Melting PointN/A
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