I-BET151 (GSK1210151A)

For research use only.

Catalog No.S2780

27 publications

I-BET151 (GSK1210151A) Chemical Structure

Molecular Weight(MW): 415.44

I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively.

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Selleck's I-BET151 (GSK1210151A) has been cited by 27 publications

Purity & Quality Control

Choose Selective Epigenetic Reader Domain Inhibitors

Biological Activity

Description I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively.
Features Optimized to retain excellent BET target potency and selectivity while enhancing the in vivo pharmacokinetics and terminal half-life to enable prolonged in vivo studies.
Targets
BRD3 [1]
(Cell-free assay)
BRD2 [1]
(Cell-free assay)
BRD4 [1]
(Cell-free assay)
0.25 μM 0.5 μM 0.79 μM
In vitro

I-BET151 exhibits potent selectivity over an extensive range of diverse protein types such as COX-2, P450, Aurora B, GSK3β, PI3K-γ, GPCR, ion channels, and transporters. Similar to I-BET762 (GSK525762A), I-BET151 displays potent binding affinity to BRD2, BRD3 and BRD4 with KD of 0.02-0.1 μM, and significantly inhibits lipopolysaccharide-stimulated IL-6 cytokine production in human peripheral blood mononuclear cells (PBMC) and whole blood (WB) as well as rat WB with IC50 of 0.16 μM, 1.26 μM, and 1.26 μM, respectively. I-BET151 (0.5 or 5 μM) inhibits the binding of BETs (BRD2, BRD3, BRD4, and BRD9) but not the binding of 23 other bromodomain proteins in HL60 nuclear extract to acetylated histone peptides. I-BET151 has potent efficacy against cell lines harboring different MLL-fusions such as MV4;11, RS4;11, MOLM13, and NOMO1 cells with IC50 of 15-192 nM. Consistently, I-BET151 completely ablates the colony-forming potential of MLL-fusion-driven leukaemias (MOLM13) but not leukaemias driven by tyrosine kinase activation (K562). I-BET151 also displays potent efficacy in both liquid culture and clonogenic assays using primary murine progenitors transformed with either MLL-ENL or MLL-AF9. I-BET151 treatment significantly induces apoptosis and prominent G0/G1 arrest in MLL-fusion cell lines driven by distinct MLL fusions (MOLM13 and MV4;11 containing MLL-AF9 and MLL-AF4, respectively) but not the K562 cells, probably due to the inhibition of transcription of BCL2, C-MYC and CDK6 by blocking the recruitment of BRD3/4, PAFc and SEC components into transcriptional start site (TSS). [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV4;11 MYPjfZRwfG:6aXPpeJkh[XO|YYm= NUToTYFYhjFyMDFOwG0> M2DyOWROW09? MkDaTWM2OD1{NjDuUS=> NVrsTG9VOjF7NkSzOFA>
RS4;11 MmmzZ5l1d3SxeHnjbZR6KGG|c3H5 MYH+NVAxKM7:TR?= NVrwe3RKTE2VTx?= NHzZVHFKSzVyPUG5NkBvVQ>? MlLyNlE6PjR|NEC=
MOLM13 NUfYXnVo[3m2b4TvfIlkcXS7IHHzd4F6 NH;wXJZ,OTByIN88US=> MmHlSG1UVw>? MWTJR|UxRTF{MDDuUS=> MV:yNVk3PDN2MB?=
NOMO1 NFXqe4VkgXSxdH;4bYNqfHliYYPzZZk> MUT+NVAxKM7:TR?= MUnEUXNQ NXn1U3lXUUN3ME2xOUBvVQ>? MUCyNVk3PDN2MB?=
HEL MVnjfZRwfG:6aXPpeJkh[XO|YYm= MXf+NVAxKM7:TR?= NGe0fItFVVOR MmLwTWM2OD1zIN88US=> M2rpdlIyQTZ2M{Sw
K562 MYPjfZRwfG:6aXPpeJkh[XO|YYm= NGHhTZZ,OTByIN88US=> M1jKOGROW09? MULJR|UxRjFyMDFOwG0> M4fsNVIyQTZ2M{Sw
MEG01 MmrUZ5l1d3SxeHnjbZR6KGG|c3H5 MofIglExOCEQvF2= NWe2cnlJTE2VTx?= MYPJR|UxRTJ3IN88US=> NYi2UoNPOjF7NkSzOFA>
HL60 NXzodJRw[3m2b4TvfIlkcXS7IHHzd4F6 MlS2glExOCEQvF2= M17J[WROW09? MWTJR|UxRTh7MDDuUS=> MmPqNlE6PjR|NEC=
MV4;11 MkDoRZBweHSxc3nzJIF{e2G7 M1rWc54yODBizszN M4G1XmROW09? MVLpcoR2[2W|IHHwc5B1d3Orcx?= M{TYbFIyQTZ2M{Sw
MOLM13 MmnjRZBweHSxc3nzJIF{e2G7 M3my[p4yODBizszN MXTEUXNQ MVHpcoR2[2W|IHHwc5B1d3Orcx?= NYrnNFBMOjF7NkSzOFA>
MV4;11 MWLGeY5kfGmxbjDhd5NigQ>? NHO2dldFVVOR M4jEUoRm[3KnYYPld{B1cGVicnXjdpVqfG2nboSgc4YhSlKGMz:0JIFv\CCrbYDhbZJm\CC{ZXPyeYl1dWWwdDDv[kBETEt7IHHu[EBRSUZzIITvJJRp\SC2cnHud4NzcXC2aX;uZYwhe3SjcoSgd4l1\Q>? MVuyNVk3PDN2MB?=
PBMC MYjGeY5kfGmxbjDhd5NigQ>? NWniXZdZTE2VTx?= MVXpcohq[mm2czDJUE03KHerdHigdGlEPTBib3[gOk44 MVqyNlQ{PzFzNR?=
A2 MY\GeY5kfGmxbjDhd5NigQ>? MUf+NVAh|ryP MlLISG1UVw>? MmjVdoVi[3SrdnH0[ZMhdGG2ZX70JGhKXi1z NGD1c3MzOzJ3NUKxPC=>
A72 NVfxSYNyTnWwY4Tpc44h[XO|YYm= MofOglExKM7:TR?= M2LWbWROW09? NYjOSm9nemWjY4TpeoF1\XNibHH0[Y51KEiLVj2x MXiyN|I2PTJzOB?=
BC1 M2fRcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUi1UWZohjFizszN M4L5W2ROW09? NXrzTpZtUUN3ME2yNlAhdk1? MXOyN|c6OjR2OB?=
BC3 MnLwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGP1Unp,OSEQvF2= MmTDSG1UVw>? NEPjcllKSzVyPUS2NEBvVQ>? MViyN|c6OjR2OB?=
BCBL1 MWnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVr+NUDPxE1? M{S0VmROW09? MWrJR|UxRTN|MDDuUS=> NGLyb20zOzd7MkS0PC=>
BJAB MkD2S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYn+NUDPxE1? NFnnNoNFVVOR M3u2fWlEPTB;OUewJI5O NY\BT45LOjN5OUK0OFg>
Namalwa MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXvlbFI4hjFizszN NUHSeYFHTE2VTx?= NXnLWWhIUUN3ME25O|Ahdk1? NF6xSpEzOzd7MkS0PC=>
Jurkat NFGybGtIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVX+NUDPxE1? NIXrOFNFVVOR NEfU[VRKSzVyPUGyNlAhdk1? MVmyN|c6OjR2OB?=
MM1S MnTCS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWW2NYxEhjFizszN M4T6N2ROW09? MlfpTWM2OD15NkCgcm0> NF\KZoEzOzd7MkS0PC=>
U266 Mn7MS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF[xToV,OSEQvF2= NWjEWoY3TE2VTx?= MWnJR|UxRTl3MDDuUS=> NE\afpczOzd7MkS0PC=>
UM-PEL-1 NUmz[ZBqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVvySWNMhjFizszN M2LJd2ROW09? MnXHTWM2OD1{MUCgcm0> Mn\QNlM4QTJ2NEi=
UM-PEL-3 NX;GeZp7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYPHeGI{hjFizszN MnHlSG1UVw>? NWLrZXJMUUN3ME2xPFAhdk1? MYqyN|c6OjR2OB?=
BC1 M1;W[WZ2dmO2aX;uJIF{e2G7 NX\Hb|hsPTByIH7N NEfWV2hFVVOR Mle0bY5lfWOnczDj[YxtNWO7Y3zlJIFzemW|dB?= MV:yN|c6OjR2OB?=
BC3 MV7GeY5kfGmxbjDhd5NigQ>? MmHQOVAxKG6P M1HwTWROW09? MVPpcoR2[2W|IHPlcIwu[3mlbHWgZZJz\XO2 NXG1WIhJOjN5OUK0OFg>
BC1 MWDGeY5kfGmxbjDhd5NigQ>? MUK4NFAhdk1? NW\6S5IzTE2VTx?= NWLCbZR3emWmdXPld{BkNU27YzDwdo91\WmwIHzleoVtew>? Mn7wNlM4QTJ2NEi=
BC3 NEHzR29HfW6ldHnvckBie3OjeR?= NXnyZZZEQDByIH7N Mli3SG1UVw>? MnOydoVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=> NGWybnQzOzd7MkS0PC=>
H929 MmrDSpVv[3Srb36gZZN{[Xl? MWr+NUDPxE1? NFHSeoVFVVOR NELTNVVqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NIfLU2IzPDN|NUS5PS=>
KMS12PE NUX2PJgyTnWwY4Tpc44h[XO|YYm= Mm\nglEh|ryP NGrtSYZFVVOR MVPpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 M1uyU|I1OzN3NEm5
KMS12BM NWf2d5ZbTnWwY4Tpc44h[XO|YYm= MoDMglEh|ryP MWPEUXNQ MWDpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NGf2UHozPDN|NUS5PS=>
KMS18 MVnGeY5kfGmxbjDhd5NigQ>? NIq4[nF,OSEQvF2= NWX5NoQ1TE2VTx?= MlPabY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NHL4OJYzPDN|NUS5PS=>
KMS11 NFX5NXVHfW6ldHnvckBie3OjeR?= NXr5TJR4hjFizszN NGnFPHlFVVOR NX3nVY9qcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NXfneWFJOjR|M{W0PVk>
RPMI8226 NGTMZ|hHfW6ldHnvckBie3OjeR?= NFvIdlN,OSEQvF2= NFf0VJhFVVOR NHLw[mNqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NEjZO40zPDN|NUS5PS=>
H929 NXXB[XVFSXCxcITvd4l{KGG|c3H5 NWLTUFY3hjFizszN NF;jTWZFVVOR NVPSU5JxcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NU[4Z3FrOjR|M{W0PVk>
KMS12PE NEHhcm9CeG:ydH;zbZMh[XO|YYm= NELQbJh,OSEQvF2= MkXHSG1UVw>? M2L2SIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NEG3SGMzPDN|NUS5PS=>
KMS12BM M2rWbWFxd3C2b4Ppd{Bie3OjeR?= NYX2O5Z4hjFizszN NWjUfHl{TE2VTx?= MYLpcoR2[2W|IHPlcIwh[XCxcITvd4l{ MnPJNlQ{OzV2OUm=
KMS18 MUfBdI9xfG:|aYOgZZN{[Xl? MYT+NUDPxE1? NGWxeFlFVVOR M1\BTIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NXjQe2VWOjR|M{W0PVk>
KMS11 NIPIe3NCeG:ydH;zbZMh[XO|YYm= NH3G[pF,OSEQvF2= M{H3N2ROW09? NGe3[HZqdmS3Y3XzJINmdGxiYYDvdJRwe2m| M4jBbVI1OzN3NEm5
RPMI8226 NXvvR|hMSXCxcITvd4l{KGG|c3H5 NEnCfFN,OSEQvF2= MojtSG1UVw>? NV7v[GVmcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MXeyOFM{PTR7OR?=
U87MG NYnXVY9rTnWwY4Tpc44h[XO|YYm= M3HZc54yOCEQvF2= NX7wR|I6TE2VTx?= NX7sdFJPemWmdXPld{BWQDePRzDj[YxtfWyjcjDBWHAhf2m2aDDJR|UxKG:oIEGuNFUh|ryP NWLNR49LOjR2OU[zPFE>
A172 NH\U[JBHfW6ldHnvckBie3OjeR?= MYD+NVAh|ryP MnPzSG1UVw>? M{nXfZJm\HWlZYOgZ4VtdHWuYYKgRXRRKHerdHigTWM2OCCxZjCxMlI5KM7:TR?= NHPM[nUzPDR7NkO4NS=>
SW1783 NX7hTGJJTnWwY4Tpc44h[XO|YYm= NV\TfFg6hjFyIN88US=> NIDVUIZFVVOR NHjI[ohz\WS3Y3XzJINmdGy3bHHyJGFVWCC5aYToJGlEPTBib3[gNk43QCEQvF2= MXeyOFQ6PjN6MR?=
U87MG MlXkSpVv[3Srb36gZZN{[Xl? M3XUUZ4yOCEQvF2= M3fiVGROW09? MnjjbY5kemWjc3XzJJBzd3CxcoTpc44hd2ZiY3XscJMhcW5idHjlJGcyN1NidILhcpNqfGmxbh?= NUPtOZV7OjR2OU[zPFE>
RAW267.4 MUjGeY5kfGmxbjDhd5NigQ>? NW\jOld3OSEQvF2= NGjQU4VFVVOR MX;y[YR2[2W|IFnMMVYheHKxZIXjeIlwdiCrbnT1Z4VlKGK7IFzQVy=> NGLFfY8zPDh3OUCwPC=>
RAW267.4 NUfIOZk2TnWwY4Tpc44h[XO|YYm= NXjRWY9COSEQvF2= MmezSG1UVw>? NYXuT|BiemWmdXPld{B1cGViYYPzc4Nq[XSrb36gZoV1f2WnbjDCVmQ1KGGwZDDhZ4V1gWyjdHXkJJA3PQ>? NWfWUm9UOjR6NUmwNFg>
Me007 M3y0OGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4DYWp4yODBizszN NInFWmNFVVOR NYXDNXc5cW6qaXLpeJMhfGinIHfyc5d1cA>? M4fnelI1QTB4MUO3
SK-Mel-28 NX7XPGQ1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{HXbJ4yODBizszN MULEUXNQ NF;OV2RqdmirYnn0d{B1cGViZ4Lve5Rp M4TqWlI1QTB4MUO3
Mel-RMU MmXHS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkWwglExOCEQvF2= MofCSG1UVw>? NGjiVJdqdmirYnn0d{B1cGViZ4Lve5Rp MXeyOFkxPjF|Nx?=
Mel-JD MlLES5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF7jPVR,OTByIN88US=> M1W0VGROW09? NGTyWZFqdmirYnn0d{B1cGViZ4Lve5Rp NYDHbI9IOjR7ME[xN|c>
Mel-RM MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV3+NVAxKM7:TR?= MUXEUXNQ M1HKcYlvcGmkaYTzJJRp\SCpcn;3eIg> M{f1OlI1QTB4MUO3
Me007 M13USmFxd3C2b4Ppd{Bie3OjeR?= Mn;WglExOCEQvF2= M1f5TmROW09? NUn5S41KcW6mdXPld{BieG:ydH;zbZM> MmD3NlQ6ODZzM{e=
SK-Mel-28 NIrtZ4tCeG:ydH;zbZMh[XO|YYm= MVj+NVAxKM7:TR?= NEXZUIZFVVOR M4T1O4lv\HWlZYOgZZBweHSxc3nz NHLyXmEzPDlyNkGzOy=>
Mel-RMU MoTqRZBweHSxc3nzJIF{e2G7 NEjuPVl,OTByIN88US=> NX3DXXBmTE2VTx?= M1XUbYlv\HWlZYOgZZBweHSxc3nz MXeyOFkxPjF|Nx?=
Mel-JD NEXDSVJCeG:ydH;zbZMh[XO|YYm= M3u1TJ4yODBizszN MWDEUXNQ NGTXfIdqdmS3Y3XzJIFxd3C2b4Ppdy=> NInBRXQzPDlyNkGzOy=>
Mel-RM MVzBdI9xfG:|aYOgZZN{[Xl? MnLXglExOCEQvF2= MY\EUXNQ NEi0XldqdmS3Y3XzJIFxd3C2b4Ppdy=> NHvJZVQzPDlyNkGzOy=>
Me007 NFr2R4hHfW6ldHnvckBie3OjeR?= NX3i[YlIOTBizszN NInqPIRFVVOR NXf4UnlycW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBjgSC3cILl[5Vt[XSrb36gc4YheDJz NXHSbXk5OjR7ME[xN|c>
SK-Mel-28 M2X4OWZ2dmO2aX;uJIF{e2G7 NHzmWWQyOCEQvF2= M3L1bGROW09? NIr6cnBqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIJ6KHWycnXneYxifGmxbjDv[kBxOjF? M2nQU|I1QTB4MUO3
Mel-RMU Mk\HSpVv[3Srb36gZZN{[Xl? NWHJN5lWOTBizszN NHy1VHBFVVOR MYLpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHL5JJVxemWpdXzheIlwdiCxZjDwNlE> NF62OJkzPDlyNkGzOy=>
Mel-JD M2jDXGZ2dmO2aX;uJIF{e2G7 M1v0[lExKM7:TR?= M3;rZWROW09? MXXpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHL5JJVxemWpdXzheIlwdiCxZjDwNlE> NFfzVZEzPDlyNkGzOy=>
Mel-RM MmPRSpVv[3Srb36gZZN{[Xl? NH\ESogyOCEQvF2= NGfweGVFVVOR NEnBeYFqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIJ6KHWycnXneYxifGmxbjDv[kBxOjF? NFrmb4MzPDlyNkGzOy=>
Me007 NF;BfotHfW6ldHnvckBie3OjeR?= M1HC[FExKM7:TR?= Ml\0SG1UVw>? NX\1Uo1CfXC{ZXf1cIF1\XNicILvZZBweHSxdHnjJIFv\CClZXzsJIN6[2ynIHHydoV{fCCpZX7ldy=> NYTqNZQxOjR7ME[xN|c>
SK-Mel-28 NYC1SVZITnWwY4Tpc44h[XO|YYm= M2PjclExKM7:TR?= NUXuUXFqTE2VTx?= M2LBeZVxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= M2H2clI1QTB4MUO3
Mel-RMU NGXwWGVHfW6ldHnvckBie3OjeR?= MXqxNEDPxE1? MkOySG1UVw>? MnX3eZBz\We3bHH0[ZMheHKxYYDvdJRwfGmlIHHu[EBk\WyuIHP5Z4xmKGG{cnXzeEBo\W6ncx?= NGXEUWYzPDlyNkGzOy=>
Mel-JD MYTGeY5kfGmxbjDhd5NigQ>? MkTZNVAh|ryP MlzySG1UVw>? MkXMeZBz\We3bHH0[ZMheHKxYYDvdJRwfGmlIHHu[EBk\WyuIHP5Z4xmKGG{cnXzeEBo\W6ncx?= MXeyOFkxPjF|Nx?=
Mel-RM MXrGeY5kfGmxbjDhd5NigQ>? NUPwUXY4OTBizszN NX[wW3J6TE2VTx?= NHP2bGt2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz MU[yOFkxPjF|Nx?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
α-SMA / Fibronectin / Collagen-1; 

PubMed: 27732564     


Normally cultured NRK-49F cells were treated with I-BET151 (0-5μM) for 36 h. Then, cell lysates were prepared and subjected to immunoblot analysis with antibodies against α-SMA, collagen-1, fibronectin, and GAPDH.

FoxM1 / AURKB / Survivin / cyclin B / PLK1; 

PubMed: 26877780     


OVTOKO and OVCA420 cells were treated with DMSO, JQ1 (1 μM) or I-BET151 (1 μM). Cell lysates were immunoblotted with indicated antibodies. 

HP1α / HP1β / HP1γ; 

PubMed: 30386240     


Protein expression levels of HP1α, β, and γ in U937, R-U937, HL-60, and R-HL-60 cells after incubation with I-BET151 at indicated dose for 48 h. Typical blots from a representative experiment are shown. The experiments were repeated three times.

27732564 26877780 30386240
In vivo Administration of I-BET151 at 30 mg/kg/day significantly inhibits tumor growth of murine MLL-AF9 and human MLL-AF4 leukaemia in mice, and provides marked survival benefit. [1]

Protocol

Kinase Assay:

[1]

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Fluorescence anisotropy (FP) ligand displacement assay:

All components are dissolved in buffer of composition 50 mM HEPES pH 7.4, 150 mM NaCl and 0.5 mM CHAPS with final concentrations of BRD 2/3/4 75 nM, fluorescent ligand 5 nM. 10 μL of this reaction mixture is added using a micro multidrop to wells containing 100 nL of various concentrations of I-BET151 or DMSO vehicle (1% final) in Greiner 384 well Black low volume microtitre plate and equilibrated in the dark for 60 minutes at room temperature. Fluorescence anisotropy is read in Envision (lex = 485 nm, lEM = 530 nm; Dichroic = 505 nM).
Cell Research:

[1]

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  • Cell lines: MV4;11, MOLM13, NOMO1, RS4;11, HEL, HL60 and K562
  • Concentrations: Dissolved in DMSO, final concentrations ~100 μM
  • Incubation Time: 24, or 72 hours
  • Method:

    Cells are exposed to various concentrations of I-BET151 for 24 or 72 hours in 384-well or 96-well plates. For cell growth inhibition assays, plates are added with CellTiter-Glo reagent using a volume equivalent to the cell culture volume in the wells, shaken for approximately 2 minutes and chemiluminescent signal is read on the Analyst GT or EnVision Plate Reader. For cell proliferation assays, CellTiter-Aqueous One is added to each well and plates are incubated for 4 hours at 37 °C. Absorbance is read at 490 nm on a SpectraMax Gemini reader


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: NOD-SCID mice injected intravenously with MV4;11 cells, and C57BL/6 mice injected intravenously with MLL-AF9 cells
  • Dosages: ~30 mg/kg/day
  • Administration: Intraperitoneal injection
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 27 mg/mL (64.99 mM)
DMSO Insoluble
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 415.44
Formula

C23H21N5O3

CAS No. 1300031-49-5
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=O)N4)C(C)C5=CC=CC=N5)OC

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Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID