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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  • 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. 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 M1PXe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmjsTY5pcWKrdHnvckBw\iCqdX3hckBTYEZ|OUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlAyOTV2IN88US=> MlrBV2FPT0WU
human SW982 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MW\Jcohq[mm2aX;uJI9nKGi3bXHuJHNYQTh{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wN|U5PCEQvF2= M3S3OnNCVkeHUh?=
human MAD-MB-468 cells MXfGeY5kfGmxbjDhd5NigQ>? M2nhbWlvcGmkaYTpc44hd2ZiUFmzT4JmfGFiaX6gbJVu[W5iTVHEMW1DNTR4ODDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFOnckS3N{BCc3RicHjvd5Bpd3K7bHH0bY9vKGK7IHPlcIx2dGG{IIDveIVv[3liYYPzZZktKEmFNUC9NE4xPCEQvF2= MmfFNlQ6QTJ6N{S=
human KURAMOCHI cell MnvFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NG\zWZpKdmirYnn0bY9vKG:oIHj1cYFvKEuXUlHNU2NJUSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUC1NUDPxE1? Mn7aV2FPT0WU
human A498 cell M17pWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYnJcohq[mm2aX;uJI9nKGi3bXHuJGE1QThiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGxO|k2KM7:TR?= NHP5ZndUSU6JRWK=
human YT cell M2DGU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4r1XmlvcGmkaYTpc44hd2ZiaIXtZY4hYVRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGyNFY3KM7:TR?= MUHTRW5ITVJ?
human VMRC-RCZ cell MoexS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmnNTY5pcWKrdHnvckBw\iCqdX3hckBXVVKFLWLDXkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTR6OUig{txO NHjnTVVUSU6JRWK=
human MDA-MB-415 cell NGnab4pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3PCVWlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVQyPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMU[3N|Ih|ryP NX;sSY1{W0GQR1XS
human J82 cell NGDkUGtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHHPVWtKdmirYnn0bY9vKG:oIHj1cYFvKEp6MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFc4PzlizszN NX7uWlFZW0GQR1XS
human SW1710 cell M2LHU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml3hTY5pcWKrdHnvckBw\iCqdX3hckBUXzF5MUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUzQTJizszN MnriV2FPT0WU
human T47D cell M2q5O2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHnUfWdKdmirYnn0bY9vKG:oIHj1cYFvKFR2N1SgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU{OjdizszN NHT4NnNUSU6JRWK=
human SU-DHL-1 cell NFyzb|NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXSwNnB2UW6qaXLpeIlwdiCxZjDoeY1idiCVVT3ETGwuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNU[4NVMh|ryP MUHTRW5ITVJ?
human BT-20 cell Mlr0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{LVOWlvcGmkaYTpc44hd2ZiaIXtZY4hSlRvMkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU6OjJ{IN88US=> NX;JcYVrW0GQR1XS
human OS-RC-2 cell Mn;ZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NI\HbHpKdmirYnn0bY9vKG:oIHj1cYFvKE:VLWLDMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ{M{i4JO69VQ>? NHyzfIFUSU6JRWK=
human RPMI-6666 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV7md|U5UW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVY3PjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLk[0N|c6KM7:TR?= M2[wS3NCVkeHUh?=
human OVCAR-3 cell MmT3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIDTV5lKdmirYnn0bY9vKG:oIHj1cYFvKE:YQ1HSMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ5OUS2JO69VQ>? MlHNV2FPT0WU
human NALM-6 cell NUfwTpljT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MULJcohq[mm2aX;uJI9nKGi3bXHuJG5CVE1vNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuO|A1PjVizszN MkPzV2FPT0WU
human RS4-11 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2H5cGlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OzhyNjFOwG0> Mn31V2FPT0WU
human SK-MES-1 cell M1\DR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHKzRm9KdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FV{0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC55OEm2O{DPxE1? MoXnV2FPT0WU
human ES7 cell M4jaRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWXoUW8zUW6qaXLpeIlwdiCxZjDoeY1idiCHU{egZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlgyOjh4IN88US=> MoOyV2FPT0WU
human NCI-H2342 cell NITqTFBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Moe3TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKzOFIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjh2Mkm0JO69VQ>? NW\RbIE1W0GQR1XS
human SCC-9 cell MljlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3Lwe2lvcGmkaYTpc44hd2ZiaIXtZY4hW0OFLUmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlg2PzdizszN NITUZ4lUSU6JRWK=
human EW-7 cell M2naTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIfyXHNKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlg3OzV4IN88US=> NXKy[VJoW0GQR1XS
human HH cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4niTmlvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkm2NlIzKM7:TR?= MXnTRW5ITVJ?
human A427 cell NYLsZWZiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2PNfWlvcGmkaYTpc44hd2ZiaIXtZY4hSTR{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuPVk2ODVizszN MUTTRW5ITVJ?
human Daudi cell NVfobXhoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4[2S2lvcGmkaYTpc44hd2ZiaIXtZY4hTGG3ZHmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA3QDh6IN88US=> M365SXNCVkeHUh?=
human P30-OHK cell NFiySmdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1;lTGlvcGmkaYTpc44hd2ZiaIXtZY4hWDNyLV;IT{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvODdzM{ig{txO NEPWbW9USU6JRWK=
human HGC-27 cell MlTPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2noZ2lvcGmkaYTpc44hd2ZiaIXtZY4hUEeFLUK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF0yNjF6MU[g{txO NG\T[2xUSU6JRWK=
human CAMA-1 cell NHnDOnBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUnocldmUW6qaXLpeIlwdiCxZjDoeY1idiCFQV3BMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjJyMEGg{txO NVL0OnFoW0GQR1XS
human SK-OV-3 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmHVTY5pcWKrdHnvckBw\iCqdX3hckBUUy2RVj2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4zODR2NDFOwG0> Ml33V2FPT0WU
human NCI-H1048 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUC0PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOjJ3N{mg{txO NGrFc3lUSU6JRWK=
human MEL-HO cell Ml\QS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1;VSWlvcGmkaYTpc44hd2ZiaIXtZY4hVUWOLVjPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4zPDJ|ODFOwG0> MUHTRW5ITVJ?
human NKM-1 cell M2K5WWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4jqcWlvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlI5PjN4IN88US=> MX;TRW5ITVJ?
human NCI-H650 cel MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIDTbohKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IOlUxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5|MEC3OkDPxE1? M{W3OnNCVkeHUh?=
human HAL-01 cell NY\OTIFbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWrJcohq[mm2aX;uJI9nKGi3bXHuJGhCVC1yMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|AyPzVizszN NE\BW2ZUSU6JRWK=
human 786-0 cell NX7wfWlmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYXJcohq[mm2aX;uJI9nKGi3bXHuJFc5Pi1yIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zNVI5OyEQvF2= NILRT5hUSU6JRWK=
human GI-1 cell M{TNZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlKzTY5pcWKrdHnvckBw\iCqdX3hckBIUS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zNVgxQCEQvF2= MYHTRW5ITVJ?
human Becker cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUHJcohq[mm2aX;uJI9nKGi3bXHuJGJm[2uncjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|Y{OTVizszN NXTzOnprW0GQR1XS
human CCF-STTG1 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEnJ[VdKdmirYnn0bY9vKG:oIHj1cYFvKEOFRj3TWHRIOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEK1NlUh|ryP M1fsNXNCVkeHUh?=
human MC116 cell M{X5OWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4LOc2lvcGmkaYTpc44hd2ZiaIXtZY4hVUNzMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlQ3OTJ{IN88US=> NYnsXVdnW0GQR1XS
human MDA-MB-468 cell NY[1Om0zT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2jKd2lvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVQ3QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNUO3N|Yh|ryP MUHTRW5ITVJ?
human NB12 cell NYq3XoJYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnT1TY5pcWKrdHnvckBw\iCqdX3hckBPSjF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT61OFg1OiEQvF2= NULFT5MxW0GQR1XS
human LXF-289 cell NWrCSItQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NW\6bJY5UW6qaXLpeIlwdiCxZjDoeY1idiCOWF[tNlg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS53NUGwOEDPxE1? NE\MVYFUSU6JRWK=
human MFE-296 cell M2nyVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkXDTY5pcWKrdHnvckBw\iCqdX3hckBOTkVvMkm2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42Pjh|NjFOwG0> NYS4WnliW0GQR1XS
human SNU-423 cell M4jWXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUPINW54UW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtOFI{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS53N{G5NkDPxE1? MYjTRW5ITVJ?
human NCI-H2291 cell M4HSZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV\wRVJiUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIzQTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkW3OlEh|ryP MkDMV2FPT0WU
human OCUB-M cell NYDh[JltT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3f6PWlvcGmkaYTpc44hd2ZiaIXtZY4hV0OXQj3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42QDNzNDFOwG0> MknhV2FPT0WU
human KU812 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXG3cGNnUW6qaXLpeIlwdiCxZjDoeY1idiCNVUixNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPTl4Mkig{txO MnP1V2FPT0WU
human HuO9 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoTiTY5pcWKrdHnvckBw\iCqdX3hckBJfU97IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62NVI5KM7:TR?= M1\pT3NCVkeHUh?=
human 639-V cell M4P6[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4HF[WlvcGmkaYTpc44hd2ZiaIXtZY4hPjN7LW[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlY{OTR2IN88US=> MWPTRW5ITVJ?
human HCC70 cell NGftTGdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYnlcXZjUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1O3NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjZzNE[g{txO MWjTRW5ITVJ?
human SNB75 cell NF;hWllIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWnCVYo3UW6qaXLpeIlwdiCxZjDoeY1idiCVTlK3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjZ3MEig{txO M4HUXnNCVkeHUh?=
human D-336MG cell MojUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1;EXGlvcGmkaYTpc44hd2ZiaIXtZY4hTC1|M{\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjZ6ODFOwG0> NWnKO4JXW0GQR1XS
human LoVo cell MnfJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYnQWmdQUW6qaXLpeIlwdiCxZjDoeY1idiCOb2\vJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44Ozh{NTFOwG0> NYrVd|gyW0GQR1XS
human EB2 cell M1TEXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVrJcohq[mm2aX;uJI9nKGi3bXHuJGVDOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwN{WwNVkh|ryP NYT3RVlJW0GQR1XS
human HSC-2 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVf2XI52UW6qaXLpeIlwdiCxZjDoeY1idiCKU1OtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPzV5Mkeg{txO Mon4V2FPT0WU
human D-542MG cell NH3vdGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFf3SnFKdmirYnn0bY9vKG:oIHj1cYFvKERvNUSyUWch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjh3MEe3JO69VQ>? MYPTRW5ITVJ?
human COLO-684 cell NXzCW3BZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MorUTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[4OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvOjByM{Kg{txO NI\IclNUSU6JRWK=
human GDM-1 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEHN[mhKdmirYnn0bY9vKG:oIHj1cYFvKEeGTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4zPDJyNjFOwG0> NEPHPYxUSU6JRWK=
human SW1088 cell NXLF[mZ5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3HSSmlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzMEi4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk41QDF2MzFOwG0> MYLTRW5ITVJ?
human SF295 cell M2\wTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{jZXmlvcGmkaYTpc44hd2ZiaIXtZY4hW0Z{OUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlc3QTV3IN88US=> NH\Pc5dUSU6JRWK=
human NCI-H2030 cell MlnzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NY\HR|FJUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxOzBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkmwNlg5KM7:TR?= M4PUO3NCVkeHUh?=
human NCI-H1755 cell NIfuc5BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHGxVlNKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVc2PSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwMkewOlMh|ryP MWHTRW5ITVJ?
human MDA-MB-361 cell NYHhNW44T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoWyTY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtN|YyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy53MkewPUDPxE1? NXzwS4d2W0GQR1XS

... 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 individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
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
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
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    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

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