AZD6482

Catalog No.S1462 Synonyms: KIN-193

For research use only.

AZD6482 (KIN-193) 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.

AZD6482 Chemical Structure

CAS No. 1173900-33-8

Selleck's AZD6482 has been cited by 23 publications

Purity & Quality Control

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Biological Activity

Description AZD6482 (KIN-193) 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 NIfIS5FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVLNUnRoUW6qaXLpeIlwdiCxZjDoeY1idiCUWF[zPVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjBzMUW0JO69VQ>? MUXTRW5ITVJ?
human SW982 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlX5TY5pcWKrdHnvckBw\iCqdX3hckBUXzl6MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFM2QDRizszN MknhV2FPT0WU
human MAD-MB-468 cells NFvqfZBHfW6ldHnvckBie3OjeR?= NXHHOXk5UW6qaXLpeIlwdiCxZjDQTVNM[mW2YTDpckBpfW2jbjDNRWQuVUJvNE[4JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiU3XyOFc{KEGtdDDwbI9{eGixconsZZRqd25iYomgZ4VtdHWuYYKgdI91\W6leTDhd5NigSxiSVO1NF0xNjB2IN88US=> NX6zRoEyOjR7OUK4O|Q>
human KURAMOCHI cell NELV[WZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGCyfm1KdmirYnn0bY9vKG:oIHj1cYFvKEuXUlHNU2NJUSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUC1NUDPxE1? MW\TRW5ITVJ?
human A498 cell MnvqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3;QOGlvcGmkaYTpc44hd2ZiaIXtZY4hSTR7ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE4QTVizszN MUHTRW5ITVJ?
human YT cell MoXaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3HvTGlvcGmkaYTpc44hd2ZiaIXtZY4hYVRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGyNFY3KM7:TR?= NGfmcZJUSU6JRWK=
human VMRC-RCZ cell NIrld3RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVTJcohq[mm2aX;uJI9nKGi3bXHuJHZOWkNvUlPaJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yPDh7ODFOwG0> NVTRfmFYW0GQR1XS
human MDA-MB-415 cell NGDkfWhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3S2ZWlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVQyPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMU[3N|Ih|ryP M4\PfnNCVkeHUh?=
human J82 cell MofJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEDo[JZKdmirYnn0bY9vKG:oIHj1cYFvKEp6MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFc4PzlizszN MVfTRW5ITVJ?
human SW1710 cell MlTCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYnJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVI6OiEQvF2= NXfHOppvW0GQR1XS
human T47D cell M3\tUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHrHbGhKdmirYnn0bY9vKG:oIHj1cYFvKFR2N1SgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU{OjdizszN MnHDV2FPT0WU
human SU-DHL-1 cell M{TT[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUD2eJhYUW6qaXLpeIlwdiCxZjDoeY1idiCVVT3ETGwuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNU[4NVMh|ryP M2XKeHNCVkeHUh?=
human BT-20 cell M1XQPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{n2[GlvcGmkaYTpc44hd2ZiaIXtZY4hSlRvMkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU6OjJ{IN88US=> NIr1ZZdUSU6JRWK=
human OS-RC-2 cell M4i0Zmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4TJZmlvcGmkaYTpc44hd2ZiaIXtZY4hV1NvUlOtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjJ|OEig{txO Mnz4V2FPT0WU
human RPMI-6666 cell NXXxbmNpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlTPTY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLU[2OlYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ2M{e5JO69VQ>? MkTtV2FPT0WU
human OVCAR-3 cell M4XUTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVXJcohq[mm2aX;uJI9nKGi3bXHuJG9XS0GULUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlY4QTR4IN88US=> MoLnV2FPT0WU
human NALM-6 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mon4TY5pcWKrdHnvckBw\iCqdX3hckBPSUyPLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlcxPDZ3IN88US=> MlvhV2FPT0WU
human RS4-11 cell M3rsSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUjJcohq[mm2aX;uJI9nKGi3bXHuJHJUPC1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|M5ODZizszN MoDGV2FPT0WU
human SK-MES-1 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{P1fmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXTMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd6OU[3JO69VQ>? Mki2V2FPT0WU
human ES7 cell NITR[lBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{n3TmlvcGmkaYTpc44hd2ZiaIXtZY4hTVN5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD64NVI5PiEQvF2= MX\TRW5ITVJ?
human NCI-H2342 cell NI\lW3dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWDhSXpLUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFI{PDJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLki0Nlk1KM7:TR?= NHXQelBUSU6JRWK=
human SCC-9 cell NFXOS4hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVX2TWo1UW6qaXLpeIlwdiCxZjDoeY1idiCVQ1OtPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQDV5NzFOwG0> MYrTRW5ITVJ?
human EW-7 cell MmrsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mny4TY5pcWKrdHnvckBw\iCqdX3hckBGXy15IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD64OlM2PiEQvF2= M2\oR3NCVkeHUh?=
human HH cell MlnRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVPqNFVRUW6qaXLpeIlwdiCxZjDoeY1idiCKSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuPVYzOjJizszN NWfiWY9xW0GQR1XS
human A427 cell NHrOZ2FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFSwWIFKdmirYnn0bY9vKG:oIHj1cYFvKEF2MkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlk6PTB3IN88US=> NFnTUWxUSU6JRWK=
human Daudi cell NVvkUpM6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVXJfWZkUW6qaXLpeIlwdiCxZjDoeY1idiCGYYXkbUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvODZ6OEig{txO M2XzTHNCVkeHUh?=
human P30-OHK cell NIDOfXlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVu5fldCUW6qaXLpeIlwdiCxZjDoeY1idiCSM{CtU2hMKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5yN{GzPEDPxE1? MlH6V2FPT0WU
human HGC-27 cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1ywVWlvcGmkaYTpc44hd2ZiaIXtZY4hUEeFLUK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF0yNjF6MU[g{txO NWrNWWtmW0GQR1XS
human CAMA-1 cell NG\NSVBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXzHXXVWUW6qaXLpeIlwdiCxZjDoeY1idiCFQV3BMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjJyMEGg{txO MlLPV2FPT0WU
human SK-OV-3 cell NUXjc|hsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVPJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU:YLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlIxPDR2IN88US=> M4joeHNCVkeHUh?=
human NCI-H1048 cell NGmyTItIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWLoNHNJUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFExPDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkKyOVc6KM7:TR?= M1zQfXNCVkeHUh?=
human MEL-HO cell NFnBSnVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4\y[2lvcGmkaYTpc44hd2ZiaIXtZY4hVUWOLVjPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4zPDJ|ODFOwG0> NWnBdHNNW0GQR1XS
human NKM-1 cell M3zn[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoDITY5pcWKrdHnvckBw\iCqdX3hckBPU01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNlg3OzZizszN MVLTRW5ITVJ?
human NCI-H650 cel NUDC[nIxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnruTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSE[1NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzByN{[g{txO NFLUV4dUSU6JRWK=
human HAL-01 cell NXPlW|JqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH[3NIxKdmirYnn0bY9vKG:oIHj1cYFvKEiDTD2wNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzBzN{Wg{txO M{OwOXNCVkeHUh?=
human 786-0 cell NXvGdHQ{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYHJcohq[mm2aX;uJI9nKGi3bXHuJFc5Pi1yIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zNVI5OyEQvF2= NX\rUGVoW0GQR1XS
human GI-1 cell MoPkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHi3dWFKdmirYnn0bY9vKG:oIHj1cYFvKEeLLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlMyQDB6IN88US=> MlzwV2FPT0WU
human Becker cell M4nqSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXTwc3ZIUW6qaXLpeIlwdiCxZjDoeY1idiCEZXPr[ZIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjN4M{G1JO69VQ>? M1\xNXNCVkeHUh?=
human CCF-STTG1 cell M3zJ[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHf5bJdKdmirYnn0bY9vKG:oIHj1cYFvKEOFRj3TWHRIOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEK1NlUh|ryP NHfwNIZUSU6JRWK=
human MC116 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVHEWYF4UW6qaXLpeIlwdiCxZjDoeY1idiCPQ{GxOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPDZzMkKg{txO NWrNUodEW0GQR1XS
human MDA-MB-468 cell M1qwcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NI\1XFRKdmirYnn0bY9vKG:oIHj1cYFvKE2GQT3NRk01PjhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkWzO|M3KM7:TR?= NUK3S4RmW0GQR1XS
human NB12 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4K5SmlvcGmkaYTpc44hd2ZiaIXtZY4hVkJzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVQ5PDJizszN MVTTRW5ITVJ?
human LXF-289 cell NHXZe|RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVfheHF6UW6qaXLpeIlwdiCxZjDoeY1idiCOWF[tNlg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS53NUGwOEDPxE1? MUjTRW5ITVJ?
human MFE-296 cell M2XSb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NG[wOJpKdmirYnn0bY9vKG:oIHj1cYFvKE2IRT2yPVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjV4OEO2JO69VQ>? MUTTRW5ITVJ?
human SNU-423 cell NHHMcHNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVyzR203UW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFI{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS53N{G5NkDPxE1? MWrTRW5ITVJ?
human NCI-H2291 cell NFzDW3lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn\ZTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKyPVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjV5NkGg{txO M2S0WnNCVkeHUh?=
human OCUB-M cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHjwV5ZKdmirYnn0bY9vKG:oIHj1cYFvKE:FVVKtUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPTh|MUSg{txO NV3mS5RVW0GQR1XS
human KU812 cell MkWyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVnCVHVPUW6qaXLpeIlwdiCxZjDoeY1idiCNVUixNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPTl4Mkig{txO M3rRc3NCVkeHUh?=
human HuO9 cell NYK3e2Z1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3fpSmlvcGmkaYTpc44hd2ZiaIXtZY4hUHWROTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlEzQCEQvF2= M3W1eHNCVkeHUh?=
human 639-V cell NXzrfXFzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYDJcohq[mm2aX;uJI9nKGi3bXHuJFY{QS2YIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62N|E1PCEQvF2= NIDjTGNUSU6JRWK=
human HCC70 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NY[wbo5uUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1O3NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjZzNE[g{txO MXHTRW5ITVJ?
human SNB75 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFW0SWhKdmirYnn0bY9vKG:oIHj1cYFvKFOQQke1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43PjVyODFOwG0> NUjrRpBQW0GQR1XS
human D-336MG cell MoTPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkDETY5pcWKrdHnvckBw\iCqdX3hckBFNTN|Nl3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43Pjh6IN88US=> M4jlOnNCVkeHUh?=
human LoVo cell MljlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYfJcohq[mm2aX;uJI9nKGi3bXHuJGxwXm9iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkezPFI2KM7:TR?= M{DTUHNCVkeHUh?=
human EB2 cell M1zCWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFn3[XRKdmirYnn0bY9vKG:oIHj1cYFvKEWEMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuO|UxOTlizszN MmjVV2FPT0WU
human HSC-2 cell NUSxXIFmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUXJcohq[mm2aX;uJI9nKGi3bXHuJGhUSy1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63OVczPyEQvF2= M2\0XXNCVkeHUh?=
human D-542MG cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M13uR2lvcGmkaYTpc44hd2ZiaIXtZY4hTC13NELNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQDVyN{eg{txO NFHNOZNUSU6JRWK=
human COLO-684 cell NF3PWJVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2j2VGlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22PFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjJyMEOyJO69VQ>? NEDYZZBUSU6JRWK=
human GDM-1 cell M3WyUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYXJcohq[mm2aX;uJI9nKGi3bXHuJGdFVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6yOFIxPiEQvF2= MoTOV2FPT0WU
human SW1088 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnjaTY5pcWKrdHnvckBw\iCqdX3hckBUXzFyOEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlQ5OTR|IN88US=> MlzuV2FPT0WU
human SF295 cell NWPs[5ZHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mly5TY5pcWKrdHnvckBw\iCqdX3hckBUTjJ7NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuO|Y6PTVizszN NF;OeI1USU6JRWK=
human NCI-H2030 cell NIDGWYtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWqwPXdKUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxOzBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkmwNlg5KM7:TR?= NFfLbWhUSU6JRWK=
human NCI-H1755 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUnJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUe1OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOjdyNkOg{txO NE\YZ2pUSU6JRWK=
human MDA-MB-361 cell NYD2[Gl6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXvxOXI2UW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOzZzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz61NlcxQSEQvF2= M37TVXNCVkeHUh?=

Protocol (from reference)

Kinase Assay:[1]
  • 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]
  • 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.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 408.45
Formula

C22H24N4O4

CAS No. 1173900-33-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CN2C(=O)C=C(N=C2C(=C1)C(C)NC3=CC=CC=C3C(=O)O)N4CCOCC4

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

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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