AZD6482

Catalog No.S1462 Synonyms: KIN-193

AZD6482 Chemical Structure

Molecular Weight(MW): 408.45

AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. Phase 1.

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4 Customer Reviews

  • Collagen-embedded melanoma spheroids were treated for 72 h with SGI-1776 [5 μM] or AZD6482 [10 μM] as single agents or in combination before staining for live (green) and dead (red) cells. Experiments were conducted in triplicate and representative images are shown. Scale bar represents 150 microns.

    Oncotarget, 2016, 7(34):54897-54912. AZD6482 purchased from Selleck.

    Cells treated with either control or INPP4B siRNA and following a 1-hour treatment with either DMSO or 1 mmol/L inhibitor; pPRAS40T246 and total PRAS40 were run on a separate blot for which the bottom Ku-86 panel is the loading control(pan-PI3Ki: GDC-0941, PI3K-ai: BYL719,PI3K-bi: AZD6482)

    Mol Cancer Res, 2017, 15(6):765-775. AZD6482 purchased from Selleck.

  • Dose response curve of compound on melanoma cell lines.  Compound was dissolved in DMSO, added in a 5-fold dilution series, starting with 10 μM, and incubated for 72 hours.  Fluorescence was measured after 8 hours incubation in resazurin.  Data was normalized to DMSO (maximal viability) and Doxorubicin (minimum viability).

    One customer. AZD6482 purchased from Selleck.

    After starved in serum-free medium for 24h,A549 cells incubated with the indicated concentrations of AZD6482 for 3h,followed by 20-minute stimolation of 100ng/ml EGF.

    Dr. Zhang of Tianjin Medical University. AZD6482 purchased from Selleck.

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. Phase 1.
Targets
PI3Kβ [1]
(Cell-free assay)
PI3Kδ [1]
(Cell-free assay)
DNA-PK [1]
(Cell-free assay)
PI3Kα [1]
(Cell-free assay)
10 nM 80 nM 420 nM 870 nM
In vitro

AZD6482 also inhibits PI3Kα, γ, and δ, with IC50 of 80 nM to 1.09 μM, which are significantly lower than its (+)-enantiomer (S-form). AZD6482 is an antiplatelet agent; it blocks platelet activation adhesion/aggregation and promotes platelet disaggregation in assay of washed platelet aggregation (WPA), with an IC50 value of 6 nM. Furthermore, by targeting PI3Kβ, AZD6482 specifically inhibits thrombosis without interfering with normal haemostasis. Therefore, AZD6482 is used as an anti-thrombotic drug for the prophylaxis of thrombotic disorders. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human RXF393 cell NEfXdYVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWrscIZOUW6qaXLpeIlwdiCxZjDoeY1idiCUWF[zPVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjBzMUW0JO69VQ>? MX3TRW5ITVJ?
human SW982 cell Mn\FS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1\GSWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7OEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA{PTh2IN88US=> MnzDV2FPT0WU
human MAD-MB-468 cells M2PxWmZ2dmO2aX;uJIF{e2G7 NFLzR5ZKdmirYnn0bY9vKG:oIGDJN2tj\XSjIHnuJIh2dWGwIF3BSE1OSi12NkigZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCVZYK0O|MhSWu2IIDoc5NxcG:{eXzheIlwdiCkeTDj[YxtfWyjcjDwc5RmdmO7IHHzd4F6NCCLQ{WwQVAvODRizszN MlfCNlQ6QTJ6N{S=
human KURAMOCHI cell NXrWfWVyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEnSSItKdmirYnn0bY9vKG:oIHj1cYFvKEuXUlHNU2NJUSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUC1NUDPxE1? M2DQSHNCVkeHUh?=
human A498 cell MlXLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGE1QThiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGxO|k2KM7:TR?= M{XoSHNCVkeHUh?=
human YT cell M2fpO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYTJcohq[mm2aX;uJI9nKGi3bXHuJHlVKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zMkC2OkDPxE1? M2DXTXNCVkeHUh?=
human VMRC-RCZ cell MnXPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkDKTY5pcWKrdHnvckBw\iCqdX3hckBXVVKFLWLDXkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTR6OUig{txO NIn6WYdUSU6JRWK=
human MDA-MB-415 cell MmDMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWXNc3NlUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuPDF3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOlc{OiEQvF2= MVjTRW5ITVJ?
human J82 cell M2TsU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnLnTY5pcWKrdHnvckBw\iCqdX3hckBLQDJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkS3O|c6KM7:TR?= MWTTRW5ITVJ?
human SW1710 cell MmTYS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkT6TY5pcWKrdHnvckBw\iCqdX3hckBUXzF5MUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUzQTJizszN M2jN[HNCVkeHUh?=
human T47D cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXqxUnBsUW6qaXLpeIlwdiCxZjDoeY1idiCWNEfEJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42OzJ5IN88US=> MWHTRW5ITVJ?
human SU-DHL-1 cell MojZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJHNWNUSKTD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42PjhzMzFOwG0> MlXFV2FPT0WU
human BT-20 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3\TeWlvcGmkaYTpc44hd2ZiaIXtZY4hSlRvMkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU6OjJ{IN88US=> MVjTRW5ITVJ?
human OS-RC-2 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2Lk[mlvcGmkaYTpc44hd2ZiaIXtZY4hV1NvUlOtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjJ|OEig{txO NVT0ZpNpW0GQR1XS
human RPMI-6666 cell NH;yUGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUfJcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvNk[2OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjR|N{mg{txO NHLJRZlUSU6JRWK=
human OVCAR-3 cell M2\6VGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmftTY5pcWKrdHnvckBw\iCqdX3hckBQXkODUj2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE43Pzl2NjFOwG0> NHq2THdUSU6JRWK=
human NALM-6 cell NU[z[W5YT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXTJcohq[mm2aX;uJI9nKGi3bXHuJG5CVE1vNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|A1PjVizszN M161TnNCVkeHUh?=
human RS4-11 cell Ml[xS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFfPN3BKdmirYnn0bY9vKG:oIHj1cYFvKFKVND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzN6ME[g{txO NXX5WnNqW0GQR1XS
human SK-MES-1 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHfYRppKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC55OEm2O{DPxE1? MlH4V2FPT0WU
human ES7 cell NHew[plIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWrJcohq[mm2aX;uJI9nKGi3bXHuJGVUPyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwOEGyPFYh|ryP NEjOUI9USU6JRWK=
human NCI-H2342 cell Ml\JS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWDPb3FmUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI{PDJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLki0Nlk1KM7:TR?= NW[xTIw{W0GQR1XS
human SCC-9 cell MnzBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFf0fXhKdmirYnn0bY9vKG:oIHj1cYFvKFOFQz25JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE45PTd5IN88US=> M1;3RXNCVkeHUh?=
human EW-7 cell NYT1SlgzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXniSJFWUW6qaXLpeIlwdiCxZjDoeY1idiCHVz23JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE45PjN3NjFOwG0> MWrTRW5ITVJ?
human HH cell NFfjdnlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3fqb2lvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkm2NlIzKM7:TR?= MlPtV2FPT0WU
human A427 cell NUez[VM4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUfJcohq[mm2aX;uJI9nKGi3bXHuJGE1OjdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkm5OVA2KM7:TR?= NFOxboNUSU6JRWK=
human Daudi cell Mn70S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mlq2TY5pcWKrdHnvckBw\iCqdX3hckBF[XWmaTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNFY5QDhizszN M1vrOnNCVkeHUh?=
human P30-OHK cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NELOS|RKdmirYnn0bY9vKG:oIHj1cYFvKFB|MD3PTGsh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjB5MUO4JO69VQ>? MX;TRW5ITVJ?
human HGC-27 cell NVvJN5Z2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3HK[GlvcGmkaYTpc44hd2ZiaIXtZY4hUEeFLUK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF0yNjF6MU[g{txO MkDNV2FPT0WU
human CAMA-1 cell NHHGTVFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWLJcohq[mm2aX;uJI9nKGi3bXHuJGNCVUFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNlAxOSEQvF2= NUTYdoU6W0GQR1XS
human SK-OV-3 cell M{jrN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{XNSWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvT2[tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOjB2NESg{txO NIj6XHNUSU6JRWK=
human NCI-H1048 cell NXnJd5FjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3rmU2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixNFQ5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5{MkW3PUDPxE1? MYPTRW5ITVJ?
human MEL-HO cell NYPPbHdPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MorpTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlI1OjN6IN88US=> MUTTRW5ITVJ?
human NKM-1 cell NGnPW21Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGfJWnFKdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4zQDZ|NjFOwG0> MmnDV2FPT0WU
human NCI-H650 cel MmHoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWHWcXViUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFY2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwM{CwO|Yh|ryP MmXrV2FPT0WU
human HAL-01 cell Mn;YS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHjBOlBKdmirYnn0bY9vKG:oIHj1cYFvKEiDTD2wNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzBzN{Wg{txO NWLUWZR[W0GQR1XS
human 786-0 cell Mmn2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF3FOGtKdmirYnn0bY9vKG:oIHj1cYFvKDd6Nj2wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{OTJ6MzFOwG0> NGL5d|FUSU6JRWK=
human GI-1 cell M4DyTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXzJcohq[mm2aX;uJI9nKGi3bXHuJGdKNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkOxPFA5KM7:TR?= MXnTRW5ITVJ?
human Becker cell M1f1S2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoX1TY5pcWKrdHnvckBw\iCqdX3hckBD\WOtZYKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlM3OzF3IN88US=> NUTm[pZ[W0GQR1XS
human CCF-STTG1 cell M4HyXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYrJcohq[mm2aX;uJI9nKGi3bXHuJGNETi2VVGTHNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPDJ3MkWg{txO NES5ZZlUSU6JRWK=
human MC116 cell NGnFWZdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{LvO2lvcGmkaYTpc44hd2ZiaIXtZY4hVUNzMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlQ3OTJ{IN88US=> MYHTRW5ITVJ?
human MDA-MB-468 cell M2\hR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYDBbWVyUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuPDZ6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT61N|c{PiEQvF2= NWTzUJNEW0GQR1XS
human NB12 cell MlO1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4fSRmlvcGmkaYTpc44hd2ZiaIXtZY4hVkJzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVQ5PDJizszN NWjteFY3W0GQR1XS
human LXF-289 cell MnLqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUDJcohq[mm2aX;uJI9nKGi3bXHuJGxZTi1{OEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlU2OTB2IN88US=> M1vTNXNCVkeHUh?=
human MFE-296 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWjJcohq[mm2aX;uJI9nKGi3bXHuJG1HTS1{OU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlU3QDN4IN88US=> NGLrdXVUSU6JRWK=
human SNU-423 cell MlXxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml;lTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42PzF7MjFOwG0> MmHRV2FPT0WU
human NCI-H2291 cell M{j2Umdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUDIeINyUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIzQTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkW3OlEh|ryP NV;xZoloW0GQR1XS
human OCUB-M cell MkLNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUDJcohq[mm2aX;uJI9nKGi3bXHuJG9EXUJvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVg{OTRizszN MYrTRW5ITVJ?
human KU812 cell M2\5UWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NI\CR4VKdmirYnn0bY9vKG:oIHj1cYFvKEuXOEGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42QTZ{ODFOwG0> NX21VnFiW0GQR1XS
human HuO9 cell M1PnXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4P0WmlvcGmkaYTpc44hd2ZiaIXtZY4hUHWROTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlEzQCEQvF2= MnvhV2FPT0WU
human 639-V cell MmfZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVnJcohq[mm2aX;uJI9nKGi3bXHuJFY{QS2YIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62N|E1PCEQvF2= M2LxenNCVkeHUh?=
human HCC70 cell M1K4[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYDNN3N[UW6qaXLpeIlwdiCxZjDoeY1idiCKQ1O3NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjZzNE[g{txO MmXZV2FPT0WU
human SNB75 cell M{PSWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHLsPY5KdmirYnn0bY9vKG:oIHj1cYFvKFOQQke1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43PjVyODFOwG0> MXfTRW5ITVJ?
human D-336MG cell MmCwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYjJcohq[mm2aX;uJI9nKGi3bXHuJGQuOzN4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlY3QDhizszN MmHBV2FPT0WU
human LoVo cell M1fWWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2DkNmlvcGmkaYTpc44hd2ZiaIXtZY4hVG:YbzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuO|M5OjVizszN NW\kflc3W0GQR1XS
human EB2 cell NFvoV3hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXX0OmszUW6qaXLpeIlwdiCxZjDoeY1idiCHQkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlc2ODF7IN88US=> NXnuclNZW0GQR1XS
human HSC-2 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWHEfWVCUW6qaXLpeIlwdiCxZjDoeY1idiCKU1OtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzV5Mkeg{txO NG\wSVRUSU6JRWK=
human D-542MG cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEWyXXlKdmirYnn0bY9vKG:oIHj1cYFvKERvNUSyUWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjh3MEe3JO69VQ>? M4PGOnNCVkeHUh?=
human COLO-684 cell MnjlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NI[0d4ZKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tOlg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi5{MECzNkDPxE1? M3;wWHNCVkeHUh?=
human GDM-1 cell M2nNe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFXKbo9KdmirYnn0bY9vKG:oIHj1cYFvKEeGTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4zPDJyNjFOwG0> NYLVfYJEW0GQR1XS
human SW1088 cell MonlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJHNYOTB6ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuOFgyPDNizszN NGO5ZVJUSU6JRWK=
human SF295 cell NUHzc3VJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2PzV2lvcGmkaYTpc44hd2ZiaIXtZY4hW0Z{OUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlc3QTV3IN88US=> NGHrVVRUSU6JRWK=
human NCI-H2030 cell MkDLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUjJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkCzNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTB{OEig{txO NGKyOWVUSU6JRWK=
human NCI-H1755 cell MlfuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3;kXmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixO|U2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy5{N{C2N{DPxE1? NUP0N4FjW0GQR1XS
human MDA-MB-361 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYrJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2zOlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjV{N{C5JO69VQ>? MUHTRW5ITVJ?

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:[1]
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Assay of PI3K enzyme inhibition:

The inhibition of PI3Kβ, PI3Kα, PI3Kγ, and PI3Kδ is evaluated in an AlphaScreen based enzyme activity assay using human recombinant enzymes. The assay measures PI3K-mediated conversion of PIP2 to PIP3. Biotinylated PIP3, a GST-tagged pleckstrin homology (PH) domain and the two AlphaScreen beads form a complex that elicits a signal upon laser excitation at 680 nm. The PIP3 formed in the enzyme reaction competes with the biotinylated PIP3 for binding to the PH domain thus reducing the signal with increasing enzyme product. The AZD6482 is dissolved in DMSO and added to 384 well plates. PBKβ, PBKα, PBKγ, or PBKδ is added in a Tris buffer (50 mM Tris pH 7.6, 0.05% CHAPS, 5 mM DTT, and 24 mM MgCl2) and allowed to preincubate with AZD6482 for 20 minutes prior to the addition of substrate solution containing PIP2 and ATP. The enzyme reaction is stopped after 20 minutes by addition of stop solution containing EDTA and biotin-PIP3, followed by addition of detection solution containing GST-grpl PH and AlphaScreen beads. Plates are left for a minimum of 5 hours in the dark prior to analysis. The final concentration of DMSO, ATP and PIP2 in the assay are, 0.8%, 4 μM, and 40 μM, respectively. IC50 values are calculated according to the equation, y = {a+[(b-a)/(l+(x/IC50)s)]}, where y = % inhibition; a = 0%; b = 100%; s = the slope of the concentration-response curve; x = AZD6482 concentration.
Cell Research:[1]
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  • Cell lines: Human platelet pellet
  • Concentrations: 0–60 nM, dissolved in DMSO
  • Incubation Time: 5 min
  • Method: For assay of washed platelet aggregation (WPA), the platelet pellets are isolated from human blood and re-suspended to 2 × 1015/L in Tyrodes buffer (TB) containing 1 μM hirudin and 0.02 U/mL apyrase. Then, the platelet suspension is left to rest at room temperature for 30 min. Just prior to time for assay, CaCl2 is added to a final concentration of 2 mM. AZD6482, dissolved in DMSO, is added to a 96-well plate prior to the addition of the washed platelet suspension. The platelet suspension is preincubated with AZD6482 for 5 min. Light absorption at 650 nm is recorded before and after a 5 min plate shake and referred to as recording 0 (R0) and Rl. A mouse anti-human CD9 antibody is added (at a donor specific concentration) to each well prior to next 10 min plate shake and light absorption recording; R2. For data analysis, light absorbance in wells with TB are subtracted from all readings before percent aggregation is calculated according the formula: [(R1-R2)/R1] × 100 = % aggregation. Spontaneous aggregation or pro-aggregatory effect of the inhibitor is evaluated by the same formula, [(R0-Rl)/R0] × 100 = % aggregation. IC50 values are calculated according to the equation, y = {a+[(b-a)/(l+(x/IC50)s)]}, where y = % inhibition; a = 0%; b = 100%; s = the slope of the concentration-response curve; x = AZD6482 concentration.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 82 mg/mL (200.75 mM)
Ethanol 10 mg/mL (24.48 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.
30 mg/mL

* 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 408.45
Formula

C22H24N4O4

CAS No. 1173900-33-8
Storage powder
in solvent
Synonyms KIN-193

Bio Calculators

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 (g) = Concentration (mol/L) × Volume (L) × 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
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    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

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00853450 Completed Antiplatelet Effect AstraZeneca February 2009 Phase 1
NCT00688714 Completed Antiplatelet Effect AstraZeneca January 2008 Phase 1

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID