Ricolinostat (ACY-1215)

Catalog No.S8001 Synonyms: Rocilinostat

For research use only.

Ricolinostat (ACY-1215, Rocilinostat) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Ricolinostat (ACY-1215) suppresses cell proliferation and promotes apoptosis. Phase 2.

Ricolinostat (ACY-1215)  Chemical Structure

CAS No. 1316214-52-4

Selleck's Ricolinostat (ACY-1215) has been cited by 56 publications

Purity & Quality Control

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Biological Activity

Description Ricolinostat (ACY-1215, Rocilinostat) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Ricolinostat (ACY-1215) suppresses cell proliferation and promotes apoptosis. Phase 2.
Features Induced less cytotoxicity in PHA-stimulated PBMCs from 4 healthy donors compared with the pan-HDAC inhibitor SAHA.
Targets
HDAC6 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC8 [1]
(Cell-free assay)
4.7 nM 48 nM 51 nM 58 nM 100 nM
In vitro

ACY-1215 is a hydroxamic acid derivative. ACY-1215 is 12-, 10-, and 11-fold less active against HDAC1, HDAC2, and HDAC3 (class I HDACs), respectively. ACY-1215 has minimal activity (IC50 > 1μM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2, and has slight activity against HDAC8 (IC50 = 0.1μM). The IC50 values for ACY-1215 for T-cell toxicity is 2.5μM. ACY-1215 overcomes tumor cell growth and survival conferred by BMSCs and cytokines in the BM milieu. ACY-1215 in combination with bortezomib induces synergistic anti-MM activity. ACY-1215 induces potent acetylation of α-tubulin at very low doses and triggers acetylation of lysine on histone H3 and histone H4 only at higher doses, confirming its specific inhibitory effect on HDAC6 activity. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A-172 NIT5e2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fFS|ExyqCwTR?= NUPme|JXOjRxNEigbC=> MV\pcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 NYDid4xHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xOVA{PDBpPkK2NVUxOzRyPD;hQi=>
U87MG MoDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWixNOKhdk1? NUHK[4I3OjRxNEigbC=> M2nsTYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> M3X6UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUWwN|QxLz5{NkG1NFM1ODxxYU6=
Hbl-1 NXHGRlZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVm0PEBp MYPJR|UxRTFwNjFOwG0> NGnTb5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
OCI-Ly10 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3f3OVQ5KGh? NHXM[WdKSzVyPUCuPUDPxE1? NUTQO5RqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
Riva MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[0PEBp MnewTWM2OD1{LkKg{txO M2TFOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
Su-DHL2 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\iOFghcA>? MWrJR|UxRTNwMzFOwG0> M3XkTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUG2NlcxLz5{NkGxOlI4ODxxYU6=
OCI-Ly1 Mk\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfudnE1QCCq M3jsOGlEPTB;Mj60JO69VQ>? NWXJZ2lxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
OCI-Ly7 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfxOFghcA>? NX\ldWxpUUN3ME2xMlIh|ryP NYjxZ2trRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
Su-DHL4 NEGxWlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWX1eod2PDhiaB?= MlHqTWM2OD12Lkeg{txO NHLkNZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
Su-DHL6 M2T2WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorrOFghcA>? Mlu0TWM2OD1|LkKg{txO MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
Hbl-2 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHz5SII1QCCq MUHJR|UxRTFwOTFOwG0> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
Jeko-1 M3HvUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUC0PEBp NVvmdoZ5UUN3ME2xMlUh|ryP NWfie2cyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
Jvm-2 NVr1bodkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUe0PEBp MUPJR|UxRTRwMDFOwG0> NIDHWlg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkGxOlI4OCd-Mk[xNVYzPzB:L3G+
Rec-1  NEHncndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\sNVQ5KGh? MmDYTWM2OD1{LkOg{txO NVnRXmx[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
CCL-119 NYPvUoF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XMeFQ5KGh? MVnJR|UxRTFwNzFOwG0> MoPFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO|AoRjJ4MUG2NlcxRC:jPh?=
H9 MoTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLvOFghcA>? NV;QbIQ1UUN3ME2xMlIh|ryP MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFzNkK3NEc,OjZzMU[yO|A9N2F-
HH NV;a[pJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYi0PEBp MWfJR|UxRTJwNTFOwG0> NXzpOFhIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVYzPzBpPkK2NVE3OjdyPD;hQi=>
Sup-T1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHz1bWY1QCCq MU\JR|UxRTFwNjFOwG0> MljxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMU[yO|AoRjJ4MUG2NlcxRC:jPh?=
MM.1S MV;GeY5kfGmxbjDBd5NigQ>? NFq0NpcxNTYQvF2= NFnRVI43KGh? NH7vVYpqdmO{ZXHz[ZMh[WOndInsZZRm\CEQsT30eYJ2dGmw M1\yflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Mk[yO|YxLz5{MkK2Nlc3ODxxYU6=
MM.1S NVLyPXU3TnWwY4Tpc44hSXO|YYm= NEPrdVcxNjJ3L{JOwG0> MUSxPEBp NUjhdI43cW6lcnXhd4V{KGGlZYT5cIF1\WRizsGteJVjfWyrbh?= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ4Mke2NEc,OjJ{NkK3OlA9N2F-
MM.1R M3HZSmZ2dmO2aX;uJGF{e2G7 NIXNUIIxNjJ3L{JOwG0> Ml:wNVghcA>? MYnpcoNz\WG|ZYOgZYNmfHmuYYTl[EDPuS22dXL1cIlv NWHGR3ZXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlI4PjBpPkKyNlYzPzZyPD;hQi=>
RPMI8226  NUTWZlZPTnWwY4Tpc44hSXO|YYm= MUCwMlI2NzIQvF2= M1TQeVE5KGh? MkfpbY5kemWjc3XzJIFk\XS7bHH0[YQh|rFvdIXieYxqdg>? NIT6NVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2Nlc3OCd-MkKyOlI4PjB:L3G+
MM.1S NVjhOWtKS2WubDDWbYFjcWyrdImgRZN{[Xl? MknJNE05|ryP MnXtOFghcA>? M3[4bIRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ4Mke2NEc,OjJ{NkK3OlA9N2F-
OPM1 NFfOZXJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NYqxWnExOC16zszN NEnGRWQ1QCCq MYfk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NUDvXpU3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyOlI4PjBpPkKyNlYzPzZyPD;hQi=>
RPMI MXrD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXiwS|RwOC16zszN MY[0PEBp MkjH[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M1;idFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{Mk[yO|YxLz5{MkK2Nlc3ODxxYU6=
MM.1R NXH5WmN6S2WubDDWbYFjcWyrdImgRZN{[Xl? NX3lTlBrOC16zszN M334ZVQ5KGh? M4PabIRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mk\EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkK3OlAoRjJ{Mk[yO|YxRC:jPh?=
LR5 Mk\uR4VtdCCYaXHibYxqfHliQYPzZZk> M1LFclAuQM7:TR?= M2\odVQ5KGh? M4e2dIRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NF;yXFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkK2Nlc3OCd-MkKyOlI4PjB:L3G+
OPM2 M2LqNmNmdGxiVnnhZoltcXS7IFHzd4F6 M4rFZlAuQM7:TR?= Mln5OFghcA>? M{S3OIRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mmm5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{NkK3OlAoRjJ{Mk[yO|YxRC:jPh?=
Sf9 MYrGeY5kfGmxbjDhd5NigQ>? NUPGWmZ6OTBibXnudy=> MoDJTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDoeY1idiC{ZXPvcYJqdmGwdDDOMZRmem2rbnHsJGdUXC22YXfn[YQhUESDQ{[g[ZhxemW|c3XkJIlvKFOoOTDj[YxteyC3c3nu[{BHXFNiYYOgd5Vje3S{YYTlJJBz\WmwY4XiZZRm\CCob4KgNVAhdWmwczDmc4xtd3enZDDifUB{fWK|dILheIUh[WSmaYTpc44hdWWjc4Xy[YQhd3[ncjCzNEBucW6|LDDJR|UxKD1iMD6wNFQ4KM7:TT6= NG\LU3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECzPFMzPCd-MkiwN|g{OjR:L3G+
Sf9 NWTP[phjTnWwY4Tpc44h[XO|YYm= MoLLNVUhdWmwcx?= MoS4TY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDy[YNwdWKrbnHueEBpfW2jbjDOMZRmem2rbnHsJGdUXC22YXfn[YQhUESDQ{[g[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIIPmPUBk\WyuczD1d4lv\yCEb3OtUJl{NSiDYzmtRW1EKGG|IIP1ZpN1emG2ZTDwdoVqdmO3YnH0[YQh\m:{IEG1JI1qdnNiZn;scI94\WRiYomgd5Vje3S{YYTlJIFl\Gm2aX;uJI1m[XO3cnXkJIFnfGW{IE[wJI1qdnNiYomg[ox2d3Knc3PlcoNmKGG|c3H5MEBKSzVyIE2gNE4xODlizszNMi=> NEfXV4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUWwNFE{OCd-Mkm1NFAyOzB:L3G+
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Sf9 MlKzSpVv[3Srb36gZZN{[Xl? M4nsRlExKG2rboO= M13JZWlvcGmkaYTpc44hd2ZiZoXscEBt\W6pdHigbJVu[W5icnXjc41jcW6jboSgR{11\XKvaX7hcEBHVEGJLYTh[4dm\CCKRFHDNkBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|IIXzbY5oKE[WUzDhd{B{fWK|dILheIUheHKnaX7jeYJifGWmIH\vdkAyOCCvaX7zJIZwdGyxd3XkJIJ6KHO3YoP0doF1\SCjZHTpeIlwdiCvZXHzeZJm\CCxdnXyJFMxKG2rboOsJGlEPTBiPTCwMlA1QCEQvF2u M4rUclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEO4N|I1Lz5{OECzPFMzPDxxYU6=
Sf9 MmTsSpVv[3Srb36gZZN{[Xl? MV:xNEBucW6| MlHTTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDoeY1idiC{ZXPvcYJqdmGwdDDDMZRmem2rbnHsJGZNSUdvSHnzMZRi\2enZDDISGFEOSCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJJV{cW6pIF\UV{BieyC|dXLzeJJifGVicILlbY5kfWKjdHXkJIZweiBzMDDtbY5{KG[xbHzve4VlKGK7IIP1ZpN1emG2ZTDh[IRqfGmxbjDt[YF{fXKnZDDveoVzKDNyIH3pcpMtKEmFNUCgQUAxNjB3ODFOwG0v NETW[W09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECzPFMzPCd-MkiwN|g{OjR:L3G+
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Assay
Methods Test Index PMID
Western blot Ac-α-tubulin / Ac-Histone H4 ; Survivin / P21 / CDC2 / p53 / p-p53(S392) / Cyclin A2 / Cyclin B1 ; Bax / Bim / Bcl2 / Cleaved caspase-3 / Cleaved caspase-9 / Cleaved PARP ; PI3K(p85) / AKT / p-AKT(S473) / PRAS40 / Rag C / mTOR / p-mTOR / ERK / p-ERK ; Ac-β-catenin(K49) / p-β-catenin / β-catenin 31015208 30050135 25546293
Immunofluorescence β-tubulin / β-catenin 25546293
Growth inhibition assay Cell viability 31015208
In vivo ACY-1215 in combination with bortezomib triggered more significant anti-MM activity than either agent alone in suppressing tumor growth and prolonging survival in both plasmacytoma model and disseminated MM model without significant adverse effects. ACY-1215 is readily absorbed by tumor tissue. Moreover, the drug does not accumulate in tumor tissue, as evidenced by the parallel decline of acetylated α-tubulin in blood cells and tumor tissue by 24 hours after dose. [1]

Protocol (from reference)

Kinase Assay:

[1]

  • HDAC enzymatic assays:

    ACY-1215 is dissolved and subsequently diluted in assay buffer [50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine] to 6-fold the final concentration. HDAC enzymes are diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with ACY-1215 for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction is calculated.

Cell Research:

[1]

  • Cell lines: MM cell lines, patient MM cells, and PBMCs
  • Concentrations: ~8 μM
  • Incubation Time: 48 hours
  • Method:

    PBMCs from healthy donors are isolated and stimulated with 2.5 μg/mL of phytohemagglutinin (PHA) for 48 hours in the presence of increasing concentrations of ACY-1215. DNA synthesis is measured by tritiated thymidine uptake. CD4+T cells are purified from human blood with the Rosette Sep negative-selection kit. Cells are stimulated by CD3/CD28 Dynabeads for 7 days in the presence of compounds. Cell viability is assessed using alamarBlue. MM cells (2-3 × 104cells/well) are incubated in 96-well culture plates with medium and different concentrations of ACY-1215, bortezomib, and/or recombinant IL-6 (10 ng/mL) or insulin-like growth factor-1 (IGF-1; 50 ng/mL) for 24 hours at 37°C, and tritiated thymidine incorporation is measured.

Animal Research:

[1]

  • Animal Models: MM xenograft SCID mouse model
  • Dosages: 50 mg/kg
  • Administration: ip

Solubility (25°C)

In vitro

DMSO 86 mg/mL
(198.38 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+ 40% PEG 300+ 5% Tween 80+ 50% ddH2O
For best results, use promptly after mixing.

0.62mg/mL

Chemical Information

Molecular Weight 433.5
Formula

C24H27N5O3

CAS No. 1316214-52-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)N(C2=CC=CC=C2)C3=NC=C(C=N3)C(=O)NCCCCCCC(=O)NO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02632071 Completed Drug: ACY-1215|Drug: Nab-paclitaxel Metastatic Breast Cancer|Breast Carcinoma Columbia University|Acetylon Pharmaceuticals Incorporated|National Cancer Institute (NCI) March 1 2016 Phase 1
NCT01583283 Active not recruiting Drug: ACY-1215|Drug: lenalidomide|Drug: Dexamethasone Multiple Myeloma Celgene July 12 2012 Phase 1|Phase 2
NCT01323751 Completed Drug: ACY-1215 Multiple Myeloma Celgene|The Leukemia and Lymphoma Society July 2011 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
What would you suggest to obtain a clear solution?

Answer:
S8001 ACY-1215 can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 5 mg/ml clearly while it in 1% DMSO/30% polyethylene glycol/1% Tween 80 at 30 mg/ml is a suspension for oral administration. Please note that the precipitation will go out from the clear solution after stayed for about half an hour, So it is recommended to prepare the solution just before use.

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