I-BET151 (GSK1210151A)

Catalog No.S2780

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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I-BET151 (GSK1210151A) Chemical Structure

I-BET151 (GSK1210151A) Chemical Structure
Molecular Weight: 415.44

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Quality Control & MSDS

Epigenetic Reader Domain Inhibitors with Unique Features

  • Selective BET Inhibitor

    PFI-1 (PF-6405761) BRD4-selective, IC50=0.22 μM.

  • Most Potent BET Inhibitor

    I-BET-762 BET proteins, IC50=~35 nM.

  • BET Inhibitor in Clinical Trial

    RVX-208 Phase II for Dyslipidemia.

  • Newest BET Inhibitor

    Bromosporine Broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.

Product Information

  • Compare Epigenetic Reader Domain Inhibitors
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  • Research Area

Product Description

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.
Targets BRD3 [1]
(Cell-free assay)
BRD2 [1]
(Cell-free assay)
BRD4 [1]
(Cell-free assay)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
MV4;11NGPLUFZkgXSxdH;4bYNqfHliYYPzZZk>MlraglExOCEQvF2=M{jIbGROW09?NYTH[4RvUUN3ME2yOkBvVQ>?NELKUIszOTl4NEO0NC=>
RS4;11MWnjfZRwfG:6aXPpeJkh[XO|YYm=M{jQNZ4yODBizszNNGHYZ5BFVVORNY[5[YNbUUN3ME2xPVIhdk1?M3jqblIyQTZ2M{Sw
MOLM13Mmn2Z5l1d3SxeHnjbZR6KGG|c3H5M{HhcJ4yODBizszNM1LO[2ROW09?NX\sRZl2UUN3ME2xNlAhdk1?Mlq5NlE6PjR|NEC=
NOMO1NHvYTGpkgXSxdH;4bYNqfHliYYPzZZk>NEWzd2R,OTByIN88US=>NGC2WFJFVVORMkXXTWM2OD1zNTDuUS=>M1vB[VIyQTZ2M{Sw
HELNE\rdoNkgXSxdH;4bYNqfHliYYPzZZk>M1vHU54yODBizszNMX7EUXNQM3PibWlEPTB;MTFOwG0>M{XaZ|IyQTZ2M{Sw
K562MnXzZ5l1d3SxeHnjbZR6KGG|c3H5NFLHUXl,OTByIN88US=>NWTzU3ZDTE2VTx?=NYDwVI95UUN3ME6xNFAh|ryPNYDhO2drOjF7NkSzOFA>
MEG01NFmzTXVkgXSxdH;4bYNqfHliYYPzZZk>MmXtglExOCEQvF2=NIX4[2xFVVORMY\JR|UxRTJ3IN88US=>NHnWTWwzOTl4NEO0NC=>
HL60MYLjfZRwfG:6aXPpeJkh[XO|YYm=MoLNglExOCEQvF2=NFO2SlJFVVORMl33TWM2OD16OUCgcm0>NVnt[phMOjF7NkSzOFA>
MV4;11NIrEfndCeG:ydH;zbZMh[XO|YYm=Ml\qglExOCEQvF2=NXq5NG1YTE2VTx?=NHXaR3VqdmS3Y3XzJIFxd3C2b4Ppdy=>MUmyNVk3PDN2MB?=
MOLM13MUXBdI9xfG:|aYOgZZN{[Xl?NVq5ZXI{hjFyMDFOwG0>NUGz[nVlTE2VTx?=MnXJbY5lfWOnczDhdI9xfG:|aYO=MkfDNlE6PjR|NEC=
MV4;11NGDyO|NHfW6ldHnvckBie3OjeR?=MWPEUXNQMnqy[IVkemWjc3XzJJRp\SC{ZXPyeYl1dWWwdDDv[kBDWkR|L{SgZY5lKGmvcHHpdoVlKHKnY4L1bZRu\W62IH;mJGNFUzliYX7kJHBCTjFidH:geIhmKHS{YX7zZ5JqeHSrb37hcEB{fGG{dDDzbZRmNWXROnNtOjF7NkSzOFA>
PBMCMk\1SpVv[3Srb36gZZN{[Xl?NYH5bXd3TE2VTx?=NIfsem9qdmirYnn0d{BKVC14IIfpeIgheEmFNUCgc4YhPi55MoXCNlI1OzdzMUW=
A2M1G5Z2Z2dmO2aX;uJIF{e2G7NHnjSnZ,OTBizszNM3XvdWROW09?NV3oOYhTemWjY4TpeoF1\XNibHH0[Y51KEiLVj2xNWrUVG1XOjN{NUWyNVg>
A72M3XCe2Z2dmO2aX;uJIF{e2G7M1r2dJ4yOCEQvF2=M2fX[mROW09?NXzZbWM1emWjY4TpeoF1\XNibHH0[Y51KEiLVj2xMo\UNlMzPTV{MUi=
BC1MoTaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?M4XkXJ4yKM7:TR?=MX7EUXNQMkHzTWM2OD1{MkCgcm0>M{nFcFI{Pzl{NES4
BC3NWS1RW04T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=M1LoTZ4yKM7:TR?=NHTwTGpFVVORM33MSWlEPTB;NE[wJI5ONEPo[mkzOzd7MkS0PC=>
BCBL1NV3h[JpbT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=NEfNZmt,OSEQvF2=M2nVOWROW09?M174OWlEPTB;M{OwJI5OMm[3NlM4QTJ2NEi=
BJABNFPPW2dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=MVf+NUDPxE1?MoXBSG1UVw>?NV;1RpZ6UUN3ME25O|Ahdk1?NHfOU40zOzd7MkS0PC=>
NamalwaM3S0Vmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7NYX5fHhNhjFizszNNHfYV2lFVVORNI\5N29KSzVyPUm3NEBvVQ>?NF;qOIwzOzd7MkS0PC=>
JurkatM1nhXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7Mn3nglEh|ryPNV3IeJo5TE2VTx?=NFXk[IRKSzVyPUGyNlAhdk1?NHLaRlkzOzd7MkS0PC=>
MM1SMY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?NXzWS5VihjFizszNNVu3fFBMTE2VTx?=NX3sXWZIUUN3ME23OlAhdk1?NHvyV3QzOzd7MkS0PC=>
U266MV7Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?Mm\MglEh|ryPMm\zSG1UVw>?MUnJR|UxRTl3MDDuUS=>MnTZNlM4QTJ2NEi=
UM-PEL-1Mmj5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?NEPGb|d,OSEQvF2=MVPEUXNQNHHIdWtKSzVyPUKxNEBvVQ>?MVOyN|c6OjR2OB?=
UM-PEL-3NUPic49NT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=MVL+NUDPxE1?MmXRSG1UVw>?M{jjT2lEPTB;MUiwJI5ONHT4bZgzOzd7MkS0PC=>
BC1NV;aR5RmTnWwY4Tpc44h[XO|YYm=M3PSelUxOCCwTR?=NV2xelRGTE2VTx?=NEXBOJNqdmS3Y3XzJINmdGxvY4njcIUh[XK{ZYP0Mnu5NlM4QTJ2NEi=
BC3NVjPc4JWTnWwY4Tpc44h[XO|YYm=NUC0S3hMPTByIH7NM1PwcmROW09?MoOwbY5lfWOnczDj[YxtNWO7Y3zlJIFzemW|dB?=NFvhWHEzOzd7MkS0PC=>
BC1M1\PfWZ2dmO2aX;uJIF{e2G7MVu4NFAhdk1?NIrLOnpFVVORMlHydoVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=>M{jR[FI{Pzl{NES4
BC3MnfISpVv[3Srb36gZZN{[Xl?MnvaPFAxKG6PNGnvPWJFVVORMnjFdoVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=>M2HjdFI{Pzl{NES4
H929M1nqVGZ2dmO2aX;uJIF{e2G7MVn+NUDPxE1?NWDXXJVyTE2VTx?=NUjCdHlkcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=>M1;VOFI1OzN3NEm5
KMS12PEM3vIcWZ2dmO2aX;uJIF{e2G7NFXRT3Z,OSEQvF2=NH60cYZFVVORMX7pcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2M{DjcVI1OzN3NEm5
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KMS18MnHtSpVv[3Srb36gZZN{[Xl?M{LsfJ4yKM7:TR?=NXiyNGpoTE2VTx?=MYDpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2M2LaZlI1OzN3NEm5
KMS11M1rkcmZ2dmO2aX;uJIF{e2G7MUL+NUDPxE1?NV2wN4VqTE2VTx?=NVHG[FNycW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=>NUXFSmZUOjR|M{W0PVk>
RPMI8226MYrGeY5kfGmxbjDhd5NigQ>?NIHVRYp,OSEQvF2=NEnveHpFVVORMWrpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2M4PWVVI1OzN3NEm5
H929M{fmUWFxd3C2b4Ppd{Bie3OjeR?=NYLqPYtYhjFizszNM1HIeGROW09?NGiwTWVqdmS3Y3XzJINmdGxiYYDvdJRwe2m|MUGyOFM{PTR7OR?=
KMS12PEMVfBdI9xfG:|aYOgZZN{[Xl?NWnu[FhGhjFizszNNULYXXRPTE2VTx?=M3LjVolv\HWlZYOgZ4VtdCCjcH;weI9{cXN?NFHqTYozPDN|NUS5PS=>
KMS12BMMXzBdI9xfG:|aYOgZZN{[Xl?Mm\aglEh|ryPMkPHSG1UVw>?NH75U3JqdmS3Y3XzJINmdGxiYYDvdJRwe2m|MWmyOFM{PTR7OR?=
KMS18NWjwdpExSXCxcITvd4l{KGG|c3H5MlPNglEh|ryPNXfTSXYzTE2VTx?=NVTRe4dOcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?=NYfYOpN3OjR|M{W0PVk>
KMS11NIfIOXNCeG:ydH;zbZMh[XO|YYm=NVrnW5pKhjFizszNNFL3R2hFVVORNYPnd2xjcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?=NH\UO2ozPDN|NUS5PS=>
RPMI8226MVvBdI9xfG:|aYOgZZN{[Xl?NVu1foFUhjFizszNMoLYSG1UVw>?M17sUYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN?Mor6NlQ{OzV2OUm=
U87MGM4jBZWZ2dmO2aX;uJIF{e2G7MmXSglExKM7:TR?=MVXEUXNQMX;y[YR2[2W|IGW4O21IKGOnbHz1cIFzKEGWUDD3bZRpKEmFNUCgc4YhOS5yNTFOwG0>MkTtNlQ1QTZ|OEG=
A172NXvtfJAxTnWwY4Tpc44h[XO|YYm=Mmf1glExKM7:TR?=NVK4UIhvTE2VTx?=MYry[YR2[2W|IHPlcIx2dGG{IFHUVEB4cXSqIFnDOVAhd2ZiMT6yPEDPxE1?MXOyOFQ6PjN6MR?=
SW1783M3foWWZ2dmO2aX;uJIF{e2G7M17hVZ4yOCEQvF2=M1nyeGROW09?NFHSZmxz\WS3Y3XzJINmdGy3bHHyJGFVWCC5aYToJGlEPTBib3[gNk43QCEQvF2=M3;0VlI1PDl4M{ix
U87MGNVLzbXVoTnWwY4Tpc44h[XO|YYm=NH7yW|l,OTBizszNM16xT2ROW09?NXv2ZZBCcW6lcnXhd4V{KHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6geIhmKEdzL2OgeJJidnOrdHnvci=>Moi4NlQ1QTZ|OEG=
RAW267.4M3fzU2Z2dmO2aX;uJIF{e2G7MVGxJO69VQ>?MmPISG1UVw>?MlG1doVlfWOnczDJUE03KHC{b3T1Z5Rqd25iaX7keYNm\CCkeTDMVHM>NYroTmh1OjR6NUmwNFg>
RAW267.4M2LNZmZ2dmO2aX;uJIF{e2G7Mlf4NUDPxE1?NHniXXhFVVORMnjQdoVlfWOnczD0bIUh[XO|b3PpZZRqd25iYnX0e4VmdiCEUlS0JIFv\CCjY3X0fYxifGWmIIC2OS=>NFzRT2kzPDh3OUCwPC=>
Me007MYDHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?NXTtPYJ[hjFyMDFOwG0>M4f2bmROW09?MlLlbY5pcWKrdIOgeIhmKGe{b4f0bC=>NEPVbYMzPDlyNkGzOy=>
SK-Mel-28M2q2TWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7MX7+NVAxKM7:TR?=M{\TZ2ROW09?MXvpcohq[mm2czD0bIUh\3Kxd4ToMn3MNlQ6ODZzM{e=
Mel-RMUNXS5doNrT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=MlH1glExOCEQvF2=MkO2SG1UVw>?M2f2d4lvcGmkaYTzJJRp\SCpcn;3eIg>MoTkNlQ6ODZzM{e=
Mel-JDNYXNPGloT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm=MV;+NVAxKM7:TR?=MVTEUXNQMUPpcohq[mm2czD0bIUh\3Kxd4ToNUS1dppvOjR7ME[xN|c>
Mel-RMNGfPcXBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=MlnZglExOCEQvF2=NVPlUox{TE2VTx?=MmXMbY5pcWKrdIOgeIhmKGe{b4f0bC=>NWCxXGpkOjR7ME[xN|c>
Me007NFnVc4dCeG:ydH;zbZMh[XO|YYm=M1;3VZ4yODBizszNNV7aR2tGTE2VTx?=MULpcoR2[2W|IHHwc5B1d3Orcx?=MlizNlQ6ODZzM{e=
SK-Mel-28M3fyUGFxd3C2b4Ppd{Bie3OjeR?=MnLJglExOCEQvF2=NXLlbXl4TE2VTx?=MXTpcoR2[2W|IHHwc5B1d3Orcx?=M{DZS|I1QTB4MUO3
Mel-RMUNFz6SItCeG:ydH;zbZMh[XO|YYm=MmXkglExOCEQvF2=Mn3PSG1UVw>?NXnhTnEycW6mdXPld{BieG:ydH;zbZM>NIrTdJgzPDlyNkGzOy=>
Mel-JDM{PLdGFxd3C2b4Ppd{Bie3OjeR?=NH64fYZ,OTByIN88US=>MnTsSG1UVw>?NUHwb4RJcW6mdXPld{BieG:ydH;zbZM>NVHRPIM6OjR7ME[xN|c>
Mel-RMNX2weZdDSXCxcITvd4l{KGG|c3H5NHzz[5B,OTByIN88US=>M{PCc2ROW09?MXTpcoR2[2W|IHHwc5B1d3Orcx?=MVOyOFkxPjF|Nx?=
Me007MVvGeY5kfGmxbjDhd5NigQ>?M{PwVlExKM7:TR?=M4jUcmROW09?M3L2bYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZpkhfXC{ZXf1cIF1cW:wIH;mJJAzOQ>?MUKyOFkxPjF|Nx?=
SK-Mel-28MWfGeY5kfGmxbjDhd5NigQ>?NYDjT2lqOTBizszNNYLLSXp4TE2VTx?=MV;pcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHL5JJVxemWpdXzheIlwdiCxZjDwNlE>M1rOVFI1QTB4MUO3
Mel-RMUMVjGeY5kfGmxbjDhd5NigQ>?MVKxNEDPxE1?MYTEUXNQMkKwbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDifUB2eHKnZ4XsZZRqd25ib3[gdFIyMV6yOFkxPjF|Nx?=
Mel-JDNWizT|hkTnWwY4Tpc44h[XO|YYm=MUmxNEDPxE1?MlLISG1UVw>?NHXsc5pqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIJ6KHWycnXneYxifGmxbjDv[kBxOjF?Mln6NlQ6ODZzM{e=
Mel-RMNFqx[ZdHfW6ldHnvckBie3OjeR?=MoH0NVAh|ryPNY\RSXB1TE2VTx?=MmfjbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDifUB2eHKnZ4XsZZRqd25ib3[gdFIyNHjtfGwzPDlyNkGzOy=>
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SK-Mel-28NUTrbVBnTnWwY4Tpc44h[XO|YYm=M1HrWFExKM7:TR?=MmDKSG1UVw>?M1HrRZVxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO=M4jKOFI1QTB4MUO3
Mel-RMUMoW0SpVv[3Srb36gZZN{[Xl?NXXvZYZiOTBizszNNF3BeYRFVVORNIHPU|N2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXzNH[1cJgzPDlyNkGzOy=>
Mel-JDMnXPSpVv[3Srb36gZZN{[Xl?MkKzNVAh|ryPNX;INXR4TE2VTx?=NGfEUld2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXzMny4NlQ6ODZzM{e=
Mel-RMMm\aSpVv[3Srb36gZZN{[Xl?NIrr[lYyOCEQvF2=NGjLbWpFVVORMnr5eZBz\We3bHH0[ZMheHKxYYDvdJRwfGmlIHHu[EBk\WyuIHP5Z4xmKGG{cnXzeEBo\W6ncx?=NVzxVGptOjR7ME[xN|c>

... Click to View More Cell Line Experimental Data

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]
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.

Protocol(Only for Reference)

Kinase Assay:

[1]

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 Assay:

[1]

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

Animal Study:

[1]

Animal Models NOD-SCID mice injected intravenously with MV4;11 cells, and C57BL/6 mice injected intravenously with MLL-AF9 cells
Formulation Dissolved in normal saline containing 5% (v/v) DMSO and 10% (w/v) Kleptose HPB
Dosages ~30 mg/kg/day
Administration Intraperitoneal injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Dawson MA, et al. Nature, 2011, 478(7370), 529-533.

Chemical Information

Download I-BET151 (GSK1210151A) SDF
Molecular Weight (MW) 415.44
Formula

C23H21N5O3

CAS No. 1300031-49-5
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro Ethanol 27 mg/mL (64.99 mM)
DMSO <1 mg/mL
Water <1 mg/mL
* <1 mg/ml means slightly soluble or 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 Name 7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-((R)-1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one

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.

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