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 NGTydGZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUTJcohq[mm2aX;uJI9nKGi3bXHuJHJZTjN7MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFEyPTRizszN NVL5WVFrW0GQR1XS
human SW982 cell Mk[3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVfJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTh{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wN|U5PCEQvF2= M1HmRnNCVkeHUh?=
human MAD-MB-468 cells NF:0cFVHfW6ldHnvckBie3OjeR?= M4nJWGlvcGmkaYTpc44hd2ZiUFmzT4JmfGFiaX6gbJVu[W5iTVHEMW1DNTR4ODDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKFOnckS3N{BCc3RicHjvd5Bpd3K7bHH0bY9vKGK7IHPlcIx2dGG{IIDveIVv[3liYYPzZZktKEmFNUC9NE4xPCEQvF2= MoLaNlQ6QTJ6N{S=
human KURAMOCHI cell NYDsbnc5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWnJcohq[mm2aX;uJI9nKGi3bXHuJGtWWkGPT1PITUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTB3MTFOwG0> NXrle4w3W0GQR1XS
human A498 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoSzTY5pcWKrdHnvckBw\iCqdX3hckBCPDl6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNVc6PSEQvF2= M2fpdXNCVkeHUh?=
human YT cell NWHEfGxyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1PuXWlvcGmkaYTpc44hd2ZiaIXtZY4hYVRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGyNFY3KM7:TR?= MniyV2FPT0WU
human VMRC-RCZ cell M1zaVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGe1b29KdmirYnn0bY9vKG:oIHj1cYFvKF[PUlOtVmNbKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zNEi5PEDPxE1? M1PTU3NCVkeHUh?=
human MDA-MB-415 cell MlvhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NW\iVZZZUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuPDF3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOlc{OiEQvF2= M3HvNnNCVkeHUh?=
human J82 cell MkjUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXXtfmU1UW6qaXLpeIlwdiCxZjDoeY1idiCMOEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ4Pzd7IN88US=> NHz6UWlUSU6JRWK=
human SW1710 cell M122PWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUPuNmxCUW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjV{OUKg{txO Mn;LV2FPT0WU
human T47D cell M3HVdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUTJcohq[mm2aX;uJI9nKGi3bXHuJHQ1P0RiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkWzNlch|ryP NHiyeoJUSU6JRWK=
human SU-DHL-1 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHL6ZXRKdmirYnn0bY9vKG:oIHj1cYFvKFOXLVTIUE0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC53NkixN{DPxE1? MUTTRW5ITVJ?
human BT-20 cell NIT2Z5pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFjJSJdKdmirYnn0bY9vKG:oIHj1cYFvKEKWLUKwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42QTJ{MjFOwG0> M1Xud3NCVkeHUh?=
human OS-RC-2 cell M32zU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2nEO2lvcGmkaYTpc44hd2ZiaIXtZY4hV1NvUlOtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjJ|OEig{txO MnXuV2FPT0WU
human RPMI-6666 cell NVfNb4hKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIfoZ3RKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtOlY3PiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwNkSzO|kh|ryP MULTRW5ITVJ?
human OVCAR-3 cell Mo[yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NE\aSmhKdmirYnn0bY9vKG:oIHj1cYFvKE:YQ1HSMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ5OUS2JO69VQ>? MlXLV2FPT0WU
human NALM-6 cell NYfIeWQ3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnT5TY5pcWKrdHnvckBw\iCqdX3hckBPSUyPLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlcxPDZ3IN88US=> M{TFcXNCVkeHUh?=
human RS4-11 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{L6b2lvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OzhyNjFOwG0> M3;3[3NCVkeHUh?=
human SK-MES-1 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWTJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44QDl4NzFOwG0> NFzJNnNUSU6JRWK=
human ES7 cell NVvhVox6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGVUPyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwOEGyPFYh|ryP M1XzZnNCVkeHUh?=
human NCI-H2342 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWfJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkO0NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQDR{OUSg{txO NEnYTWZUSU6JRWK=
human SCC-9 cell M{LjcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYDJcohq[mm2aX;uJI9nKGi3bXHuJHNESy17IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD64OVc4KM7:TR?= M1r0dHNCVkeHUh?=
human EW-7 cell NHrZOZpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYrZdIFKUW6qaXLpeIlwdiCxZjDoeY1idiCHVz23JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE45PjN3NjFOwG0> NFjtUYtUSU6JRWK=
human HH cell MoXDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{XCXWlvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkm2NlIzKM7:TR?= M37VR3NCVkeHUh?=
human A427 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYf4O2dVUW6qaXLpeIlwdiCxZjDoeY1idiCDNEK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE46QTVyNTFOwG0> MmDIV2FPT0WU
human Daudi cell M2Cz[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MULJcohq[mm2aX;uJI9nKGi3bXHuJGRifWSrIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wOlg5QCEQvF2= NH;t[GZUSU6JRWK=
human P30-OHK cell MoWxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{Pt[GlvcGmkaYTpc44hd2ZiaIXtZY4hWDNyLV;IT{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvODdzM{ig{txO MnjrV2FPT0WU
human HGC-27 cell NFHVenBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmTjTY5pcWKrdHnvckBw\iCqdX3hckBJT0NvMkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4Phfg+9lCCLQ{WwQVEvOThzNjFOwG0> NFzBNJNUSU6JRWK=
human CAMA-1 cell NFXJOotIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXPJcohq[mm2aX;uJI9nKGi3bXHuJGNCVUFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNlAxOSEQvF2= NFrs[G1USU6JRWK=
human SK-OV-3 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MonmTY5pcWKrdHnvckBw\iCqdX3hckBUUy2RVj2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4zODR2NDFOwG0> MlfUV2FPT0WU
human NCI-H1048 cell M1Tie2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{PObWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixNFQ5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5{MkW3PUDPxE1? MXzTRW5ITVJ?
human MEL-HO cell M13q[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX;Jcohq[mm2aX;uJI9nKGi3bXHuJG1GVC2KTzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNlQzOzhizszN MonhV2FPT0WU
human NKM-1 cell NIT5S5pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlvCTY5pcWKrdHnvckBw\iCqdX3hckBPU01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNlg3OzZizszN MWPTRW5ITVJ?
human NCI-H650 cel NHfMcXdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYK0OHJXUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFY2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwM{CwO|Yh|ryP MWnTRW5ITVJ?
human HAL-01 cell NWrBOm9GT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYm1W3pNUW6qaXLpeIlwdiCxZjDoeY1idiCKQVytNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjNyMUe1JO69VQ>? MV;TRW5ITVJ?
human 786-0 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml7lTY5pcWKrdHnvckBw\iCqdX3hckA4QDZvMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|EzQDNizszN MUTTRW5ITVJ?
human GI-1 cell MmrGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHf3WGlKdmirYnn0bY9vKG:oIHj1cYFvKEeLLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlMyQDB6IN88US=> MmT5V2FPT0WU
human Becker cell NV61Z2V6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGS3fHFKdmirYnn0bY9vKG:oIHj1cYFvKEKnY3vldkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzZ|MUWg{txO MnjJV2FPT0WU
human CCF-STTG1 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWHJcohq[mm2aX;uJI9nKGi3bXHuJGNETi2VVGTHNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPDJ3MkWg{txO MXXTRW5ITVJ?
human MC116 cell NGLBfXpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmDnTY5pcWKrdHnvckBw\iCqdX3hckBOSzFzNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOFYyOjJizszN MmTKV2FPT0WU
human MDA-MB-468 cell NXXzd2M5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mlv5TY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtOFY5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS53M{ezOkDPxE1? M2XMcHNCVkeHUh?=
human NB12 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkKwTY5pcWKrdHnvckBw\iCqdX3hckBPSjF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT61OFg1OiEQvF2= NGr4eFZUSU6JRWK=
human LXF-289 cell Ml;qS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2OxR2lvcGmkaYTpc44hd2ZiaIXtZY4hVFiILUK4PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPTVzMESg{txO M1THU3NCVkeHUh?=
human MFE-296 cell Mn;xS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmXFTY5pcWKrdHnvckBw\iCqdX3hckBOTkVvMkm2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42Pjh|NjFOwG0> M1jDdXNCVkeHUh?=
human SNU-423 cell NVWzc3duT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn;1TY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42PzF7MjFOwG0> MnLpV2FPT0WU
human NCI-H2291 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYXJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkK5NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPTd4MTFOwG0> MV\TRW5ITVJ?
human OCUB-M cell NHHvfWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJG9EXUJvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVg{OTRizszN NVPpOJk3W0GQR1XS
human KU812 cell NFizcmdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGrWXJZKdmirYnn0bY9vKG:oIHj1cYFvKEuXOEGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42QTZ{ODFOwG0> MmqxV2FPT0WU
human HuO9 cell M1q4UWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV3iflJPUW6qaXLpeIlwdiCxZjDoeY1idiCKdV:5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43OTJ6IN88US=> NGq5eWRUSU6JRWK=
human 639-V cell NXziS3FYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXTJcohq[mm2aX;uJI9nKGi3bXHuJFY{QS2YIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62N|E1PCEQvF2= M3zM[3NCVkeHUh?=
human HCC70 cell Mn2wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUTJcohq[mm2aX;uJI9nKGi3bXHuJGhESzdyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62OlE1PiEQvF2= NUjSZmVNW0GQR1XS
human SNB75 cell MnLKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXS5OWRvUW6qaXLpeIlwdiCxZjDoeY1idiCVTlK3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjZ3MEig{txO M1TJbHNCVkeHUh?=
human D-336MG cell M1;u[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUfJcohq[mm2aX;uJI9nKGi3bXHuJGQuOzN4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlY3QDhizszN NYS1VmpFW0GQR1XS
human LoVo cell MlexS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV;YOHNwUW6qaXLpeIlwdiCxZjDoeY1idiCOb2\vJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44Ozh{NTFOwG0> NVGwPXB3W0GQR1XS
human EB2 cell NI\5VHFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXvROXl3UW6qaXLpeIlwdiCxZjDoeY1idiCHQkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlc2ODF7IN88US=> NED4SodUSU6JRWK=
human HSC-2 cell MlHWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUjJcohq[mm2aX;uJI9nKGi3bXHuJGhUSy1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63OVczPyEQvF2= MmjBV2FPT0WU
human D-542MG cell MoHzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M33BU2lvcGmkaYTpc44hd2ZiaIXtZY4hTC13NELNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQDVyN{eg{txO MVnTRW5ITVJ?
human COLO-684 cell NUPjVlB2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVrOZpF3UW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVY5PCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwMkCwN|Ih|ryP NHrCOmdUSU6JRWK=
human GDM-1 cell NGDSTFRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIrGRlhKdmirYnn0bY9vKG:oIHj1cYFvKEeGTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4zPDJyNjFOwG0> MXjTRW5ITVJ?
human SW1088 cell NITGSo9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEPsZnFKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUC4PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPDhzNEOg{txO NXSyVlFYW0GQR1XS
human SF295 cell NX3i[IJLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3PodmlvcGmkaYTpc44hd2ZiaIXtZY4hW0Z{OUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlc3QTV3IN88US=> NICwb2ZUSU6JRWK=
human NCI-H2030 cell M1S3Umdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NG\sRYtKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlA{OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwOUCyPFgh|ryP MmrkV2FPT0WU
human NCI-H1755 cell NYH5ZYxUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXnJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUe1OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOjdyNkOg{txO MV\TRW5ITVJ?
human MDA-MB-361 cell MkS4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVrJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2zOlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjV{N{C5JO69VQ>? MWrTRW5ITVJ?

... 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
    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

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