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 MlrSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{LMS2lvcGmkaYTpc44hd2ZiaIXtZY4hWliIM{mzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xOTF3NDFOwG0> MontV2FPT0WU
human SW982 cell M1jMe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml;LTY5pcWKrdHnvckBw\iCqdX3hckBUXzl6MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFM2QDRizszN NHTuS5FUSU6JRWK=
human MAD-MB-468 cells NXTIPVVWTnWwY4Tpc44h[XO|YYm= MoPxTY5pcWKrdHnvckBw\iCSSUPLZoV1[SCrbjDoeY1idiCPQVStUWIuPDZ6IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhW2W{NEezJGFsfCCyaH;zdIhwenmuYYTpc44h[nliY3XscJVt[XJicH;0[Y5kgSCjc4PhfUwhUUN3ME2wMlA1KM7:TR?= NHvFW3QzPDl7Mki3OC=>
human KURAMOCHI cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlzSTY5pcWKrdHnvckBw\iCqdX3hckBMXVKDTV;DTGkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjFyNUGg{txO M2\TVnNCVkeHUh?=
human A498 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2HUU2lvcGmkaYTpc44hd2ZiaIXtZY4hSTR7ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNVE4QTVizszN NETKZ2ZUSU6JRWK=
human YT cell NHrNcI1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3TrTmlvcGmkaYTpc44hd2ZiaIXtZY4hYVRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGyNFY3KM7:TR?= M1XkU3NCVkeHUh?=
human VMRC-RCZ cell M3jwZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlTWTY5pcWKrdHnvckBw\iCqdX3hckBXVVKFLWLDXkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTR6OUig{txO NXvUUGVzW0GQR1XS
human MDA-MB-415 cell MlnNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmDkTY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtOFE2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC5zNkezNkDPxE1? MVXTRW5ITVJ?
human J82 cell NV;1TVdRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3K3SGlvcGmkaYTpc44hd2ZiaIXtZY4hUjh{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD60O|c4QSEQvF2= NXrPe48zW0GQR1XS
human SW1710 cell NGn1bohIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXfzRo82UW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3NVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjV{OUKg{txO Mn;OV2FPT0WU
human T47D cell NF;3[IVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGG5ZWNKdmirYnn0bY9vKG:oIHj1cYFvKFR2N1SgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU{OjdizszN MnixV2FPT0WU
human SU-DHL-1 cell M3HVeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4XF[GlvcGmkaYTpc44hd2ZiaIXtZY4hW1VvRFjMMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjV4OEGzJO69VQ>? NXPyN3ZNW0GQR1XS
human BT-20 cell NVfKb4hrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmrzTY5pcWKrdHnvckBw\iCqdX3hckBDXC1{MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOVkzOjJizszN MVTTRW5ITVJ?
human OS-RC-2 cell M3jXVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUHye5hxUW6qaXLpeIlwdiCxZjDoeY1idiCRUz3SR{0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54MkO4PEDPxE1? MVTTRW5ITVJ?
human RPMI-6666 cell NI\wfoZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJHJRVUlvNk[2OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjR|N{mg{txO NEXibYJUSU6JRWK=
human OVCAR-3 cell NETZd|JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1i0fGlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPjd7NE[g{txO NYTYN2w6W0GQR1XS
human NALM-6 cell NGPy[XNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYfXWYVZUW6qaXLpeIlwdiCxZjDoeY1idiCQQVzNMVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjdyNE[1JO69VQ>? NXvr[nYzW0GQR1XS
human RS4-11 cell NF3UUFBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGnhbGdKdmirYnn0bY9vKG:oIHj1cYFvKFKVND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzN6ME[g{txO NFHLNpBUSU6JRWK=
human SK-MES-1 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1n1TWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXTMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd6OU[3JO69VQ>? M2XRN3NCVkeHUh?=
human ES7 cell M1ruXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX7Jcohq[mm2aX;uJI9nKGi3bXHuJGVUPyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwOEGyPFYh|ryP M1rpcHNCVkeHUh?=
human NCI-H2342 cell MmjvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUnJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkO0NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQDR{OUSg{txO MYDTRW5ITVJ?
human SCC-9 cell NILFd4tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX\Jcohq[mm2aX;uJI9nKGi3bXHuJHNESy17IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD64OVc4KM7:TR?= NF3qdnhUSU6JRWK=
human EW-7 cell NWnHbnlDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGXWXGJKdmirYnn0bY9vKG:oIHj1cYFvKEWZLUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlg3OzV4IN88US=> NELDbVZUSU6JRWK=
human HH cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUHvOlVTUW6qaXLpeIlwdiCxZjDoeY1idiCKSDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuPVYzOjJizszN MonMV2FPT0WU
human A427 cell MlrDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{n4W2lvcGmkaYTpc44hd2ZiaIXtZY4hSTR{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuPVk2ODVizszN MYnTRW5ITVJ?
human Daudi cell NUjxeJVRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWfJcohq[mm2aX;uJI9nKGi3bXHuJGRifWSrIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6wOlg5QCEQvF2= M3i4NnNCVkeHUh?=
human P30-OHK cell NFPM[IVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NET1PJZKdmirYnn0bY9vKG:oIHj1cYFvKFB|MD3PTGsh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjB5MUO4JO69VQ>? NFHXelhUSU6JRWK=
human HGC-27 cell MojyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1L5dmlvcGmkaYTpc44hd2ZiaIXtZY4hUEeFLUK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZnwxIxiSVO1NF0yNjF6MU[g{txO M1foNXNCVkeHUh?=
human CAMA-1 cell M2DxN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NInyfWVKdmirYnn0bY9vKG:oIHj1cYFvKEODTVGtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOjByMTFOwG0> NHPvdoRUSU6JRWK=
human SK-OV-3 cell MljDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1myVmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvT2[tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOjB2NESg{txO MYfTRW5ITVJ?
human NCI-H1048 cell NV;0T2FMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4rXbGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixNFQ5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5{MkW3PUDPxE1? NXftdWY6W0GQR1XS
human MEL-HO cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUHVcFFQUW6qaXLpeIlwdiCxZjDoeY1idiCPRVytTG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjJ2MkO4JO69VQ>? NVfyfldnW0GQR1XS
human NKM-1 cell NF\6bGZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmS1TY5pcWKrdHnvckBw\iCqdX3hckBPU01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNlg3OzZizszN MULTRW5ITVJ?
human NCI-H650 cel M2DNSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NY\Q[HJRUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFY2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwM{CwO|Yh|ryP MlXkV2FPT0WU
human HAL-01 cell MnPFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn\ITY5pcWKrdHnvckBw\iCqdX3hckBJSUxvMEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlMxOTd3IN88US=> NHHvfpBUSU6JRWK=
human 786-0 cell NHPwbVNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUfJcohq[mm2aX;uJI9nKGi3bXHuJFc5Pi1yIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zNVI5OyEQvF2= NUHRTJlwW0GQR1XS
human GI-1 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkXzTY5pcWKrdHnvckBw\iCqdX3hckBIUS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zNVgxQCEQvF2= M{WxbnNCVkeHUh?=
human Becker cell M4C5V2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUXJcohq[mm2aX;uJI9nKGi3bXHuJGJm[2uncjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|Y{OTVizszN MUHTRW5ITVJ?
human CCF-STTG1 cell M2\PPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWe1PW83UW6qaXLpeIlwdiCxZjDoeY1idiCFQ1[tV3RVTzFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkSyOVI2KM7:TR?= MVzTRW5ITVJ?
human MC116 cell M2fGcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3PSOGlvcGmkaYTpc44hd2ZiaIXtZY4hVUNzMU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlQ3OTJ{IN88US=> M3\uXnNCVkeHUh?=
human MDA-MB-468 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXnJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj20Olgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjV|N{O2JO69VQ>? NXizeZJ1W0GQR1XS
human NB12 cell NX\DUFQ5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYnwVWVvUW6qaXLpeIlwdiCxZjDoeY1idiCQQkGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42PDh2MjFOwG0> NV73R2l{W0GQR1XS
human LXF-289 cell NVW2[lF4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnSzTY5pcWKrdHnvckBw\iCqdX3hckBNYEZvMki5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42PTFyNDFOwG0> MoLhV2FPT0WU
human MFE-296 cell M1XWUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWXJPW1TUW6qaXLpeIlwdiCxZjDoeY1idiCPRlWtNlk3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS53NkizOkDPxE1? MX;TRW5ITVJ?
human SNU-423 cell NWjlW2J3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWPJcohq[mm2aX;uJI9nKGi3bXHuJHNPXS12MkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlU4OTl{IN88US=> MljNV2FPT0WU
human NCI-H2291 cell MoDPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnHGTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKyPVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjV5NkGg{txO MlryV2FPT0WU
human OCUB-M cell MmnPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1i5fGlvcGmkaYTpc44hd2ZiaIXtZY4hV0OXQj3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42QDNzNDFOwG0> MXfTRW5ITVJ?
human KU812 cell NWeweZpwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFPFeVRKdmirYnn0bY9vKG:oIHj1cYFvKEuXOEGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42QTZ{ODFOwG0> MkHFV2FPT0WU
human HuO9 cell NVPUboFxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUftW4JQUW6qaXLpeIlwdiCxZjDoeY1idiCKdV:5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43OTJ6IN88US=> M3LPNHNCVkeHUh?=
human 639-V cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUjwTWxZUW6qaXLpeIlwdiCxZjDoeY1idiB4M{mtWkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjNzNESg{txO NY\IRZdNW0GQR1XS
human HCC70 cell M2PHNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mo\3TY5pcWKrdHnvckBw\iCqdX3hckBJS0N5MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlYyPDZizszN NUXTU3FNW0GQR1XS
human SNB75 cell M3vIemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUGzb5pTUW6qaXLpeIlwdiCxZjDoeY1idiCVTlK3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjZ3MEig{txO NIHIPIdUSU6JRWK=
human D-336MG cell NGHQRY9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGQuOzN4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlY3QDhizszN NUnPTnZIW0GQR1XS
human LoVo cell MoPkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXXnSnNCUW6qaXLpeIlwdiCxZjDoeY1idiCOb2\vJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44Ozh{NTFOwG0> NV7Ve3VbW0GQR1XS
human EB2 cell NGfkeGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4LLPGlvcGmkaYTpc44hd2ZiaIXtZY4hTUJ{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63OVAyQSEQvF2= MoTnV2FPT0WU
human HSC-2 cell NH3LOJdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUfJcohq[mm2aX;uJI9nKGi3bXHuJGhUSy1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63OVczPyEQvF2= NYPNUJVwW0GQR1XS
human D-542MG cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4myOGlvcGmkaYTpc44hd2ZiaIXtZY4hTC13NELNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQDVyN{eg{txO MUDTRW5ITVJ?
human COLO-684 cell Mk\IS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFfa[3pKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tOlg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi5{MECzNkDPxE1? M3nU[3NCVkeHUh?=
human GDM-1 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkPHTY5pcWKrdHnvckBw\iCqdX3hckBITE1vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNlQzODZizszN NFjNcG1USU6JRWK=
human SW1088 cell NYDR[olsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MULJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTB6ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuOFgyPDNizszN M{DsdnNCVkeHUh?=
human SF295 cell MlnPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4rHOGlvcGmkaYTpc44hd2ZiaIXtZY4hW0Z{OUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlc3QTV3IN88US=> NYHmRVFZW0GQR1XS
human NCI-H2030 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVf6[VVpUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxOzBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkmwNlg5KM7:TR?= MXnTRW5ITVJ?
human NCI-H1755 cell M4T6dGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV\Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUe1OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvOjdyNkOg{txO M{fFN3NCVkeHUh?=
human MDA-MB-361 cell NYnkfXZtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFjiSmJKdmirYnn0bY9vKG:oIHj1cYFvKE2GQT3NRk0{PjFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|LkWyO|A6KM7:TR?= MWDTRW5ITVJ?

... 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(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

* 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
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*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