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 MlX3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXnJcohq[mm2aX;uJI9nKGi3bXHuJHJZTjN7MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNFEyPTRizszN M1HaU3NCVkeHUh?=
human SW982 cell Moq4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYfJcohq[mm2aX;uJI9nKGi3bXHuJHNYQTh{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6wN|U5PCEQvF2= NHOxNlhUSU6JRWK=
human MAD-MB-468 cells MkPXSpVv[3Srb36gZZN{[Xl? NWXOXI1oUW6qaXLpeIlwdiCxZjDQTVNM[mW2YTDpckBpfW2jbjDNRWQuVUJvNE[4JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiU3XyOFc{KEGtdDDwbI9{eGixconsZZRqd25iYomgZ4VtdHWuYYKgdI91\W6leTDhd5NigSxiSVO1NF0xNjB2IN88US=> M2LnWFI1QTl{OEe0
human KURAMOCHI cell NVHkTnNPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoDFTY5pcWKrdHnvckBw\iCqdX3hckBMXVKDTV;DTGkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjFyNUGg{txO MWTTRW5ITVJ?
human A498 cell Mlq5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkjZTY5pcWKrdHnvckBw\iCqdX3hckBCPDl6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNVc6PSEQvF2= NIDic5JUSU6JRWK=
human YT cell M2PYZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3jFW2lvcGmkaYTpc44hd2ZiaIXtZY4hYVRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkGyNFY3KM7:TR?= M4nXPXNCVkeHUh?=
human VMRC-RCZ cell NXiy[ZFFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoGzTY5pcWKrdHnvckBw\iCqdX3hckBXVVKFLWLDXkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTR6OUig{txO M4HFWnNCVkeHUh?=
human MDA-MB-415 cell NWDIZ4h1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{[5dWlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVQyPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMU[3N|Ih|ryP Mo\pV2FPT0WU
human J82 cell MnWxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUTLSpJHUW6qaXLpeIlwdiCxZjDoeY1idiCMOEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlQ4Pzd7IN88US=> M2HBTnNCVkeHUh?=
human SW1710 cell NYnDdmJCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHPlTZpKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTJ7MjFOwG0> MkPHV2FPT0WU
human T47D cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUXJcohq[mm2aX;uJI9nKGi3bXHuJHQ1P0RiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkWzNlch|ryP Ml3GV2FPT0WU
human SU-DHL-1 cell M{eyOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmLTTY5pcWKrdHnvckBw\iCqdX3hckBUXS2GSFytNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTZ6MUOg{txO Mn3NV2FPT0WU
human BT-20 cell NFXJZmNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2HFWWlvcGmkaYTpc44hd2ZiaIXtZY4hSlRvMkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU6OjJ{IN88US=> NYfIPWE4W0GQR1XS
human OS-RC-2 cell NHG1U2FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXTJcohq[mm2aX;uJI9nKGi3bXHuJG9UNVKFLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYzOzh6IN88US=> MYDTRW5ITVJ?
human RPMI-6666 cell NEXlZ5lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4rzVWlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST22OlY3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54NEO3PUDPxE1? NXvTUm5XW0GQR1XS
human OVCAR-3 cell NYrDU45qT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFXQZldKdmirYnn0bY9vKG:oIHj1cYFvKE:YQ1HSMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ5OUS2JO69VQ>? M{nXfnNCVkeHUh?=
human NALM-6 cell NUfncmg4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVjIWGNHUW6qaXLpeIlwdiCxZjDoeY1idiCQQVzNMVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjdyNE[1JO69VQ>? Mn\6V2FPT0WU
human RS4-11 cell NHzUNW5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1XBdWlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44OzhyNjFOwG0> MVrTRW5ITVJ?
human SK-MES-1 cell NH;oNItIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVvpbFFqUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwN{i5Olch|ryP NGLUOHZUSU6JRWK=
human ES7 cell M3z1TGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlP4TY5pcWKrdHnvckBw\iCqdX3hckBGWzdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkixNlg3KM7:TR?= MULTRW5ITVJ?
human NCI-H2342 cell MlLxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVPJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkO0NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQDR{OUSg{txO NU\STm4xW0GQR1XS
human SCC-9 cell M3rFW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkW2TY5pcWKrdHnvckBw\iCqdX3hckBUS0NvOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuPFU4PyEQvF2= MWjTRW5ITVJ?
human EW-7 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWTnXGFyUW6qaXLpeIlwdiCxZjDoeY1idiCHVz23JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE45PjN3NjFOwG0> M{LreHNCVkeHUh?=
human HH cell MorDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M37iRWlvcGmkaYTpc44hd2ZiaIXtZY4hUEhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkm2NlIzKM7:TR?= NGfhdIRUSU6JRWK=
human A427 cell M3Xpdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIGzNFdKdmirYnn0bY9vKG:oIHj1cYFvKEF2MkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlk6PTB3IN88US=> NWXxVJVPW0GQR1XS
human Daudi cell NF7KSmFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYGycGV[UW6qaXLpeIlwdiCxZjDoeY1idiCGYYXkbUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvODZ6OEig{txO M2LHOXNCVkeHUh?=
human P30-OHK cell M37VeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWHJcohq[mm2aX;uJI9nKGi3bXHuJHA{OC2RSFugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA4OTN6IN88US=> Mmr6V2FPT0WU
human HGC-27 cell NVLtfnJHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXnJV|VlUW6qaXLpeIlwdiCxZjDoeY1idiCKR1OtNlch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5Nige,:jDDJR|UxRTFwMUixOkDPxE1? NEnkWoxUSU6JRWK=
human CAMA-1 cell M4iz[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYqwT|NnUW6qaXLpeIlwdiCxZjDoeY1idiCFQV3BMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjJyMEGg{txO MoHvV2FPT0WU
human SK-OV-3 cell MnLyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3LaT2lvcGmkaYTpc44hd2ZiaIXtZY4hW0tvT2[tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOjB2NESg{txO M3vk[HNCVkeHUh?=
human NCI-H1048 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmfaTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEGwOFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjJ{NUe5JO69VQ>? NHL3fGdUSU6JRWK=
human MEL-HO cell MlzNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnXSTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlI1OjN6IN88US=> MWrTRW5ITVJ?
human NKM-1 cell NXPlfm5zT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkX6TY5pcWKrdHnvckBw\iCqdX3hckBPU01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNlg3OzZizszN Mom0V2FPT0WU
human NCI-H650 cel MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KNkWwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{ODB5NjFOwG0> NWmyd2t7W0GQR1XS
human HAL-01 cell M2HVcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4rYTmlvcGmkaYTpc44hd2ZiaIXtZY4hUEGOLUCxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{ODF5NTFOwG0> MUXTRW5ITVJ?
human 786-0 cell Ml;JS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{X5WWlvcGmkaYTpc44hd2ZiaIXtZY4hPzh4LUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlMyOjh|IN88US=> MVXTRW5ITVJ?
human GI-1 cell NGf3OW9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXTJcohq[mm2aX;uJI9nKGi3bXHuJGdKNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkOxPFA5KM7:TR?= NEHm[IlUSU6JRWK=
human Becker cell NFnJdXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHvVOXZKdmirYnn0bY9vKG:oIHj1cYFvKEKnY3vldkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzZ|MUWg{txO MWPTRW5ITVJ?
human CCF-STTG1 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGNETi2VVGTHNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPDJ3MkWg{txO NYXXcG1tW0GQR1XS
human MC116 cell MmrJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkHFTY5pcWKrdHnvckBw\iCqdX3hckBOSzFzNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOFYyOjJizszN MWnTRW5ITVJ?
human MDA-MB-468 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnXBTY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtOFY5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS53M{ezOkDPxE1? M{XO[XNCVkeHUh?=
human NB12 cell Mk\aS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHv5[XdKdmirYnn0bY9vKG:oIHj1cYFvKE6EMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlU1QDR{IN88US=> NXnhcZp3W0GQR1XS
human LXF-289 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH21NGlKdmirYnn0bY9vKG:oIHj1cYFvKEy[Rj2yPFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjV3MUC0JO69VQ>? MYjTRW5ITVJ?
human MFE-296 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVHJcohq[mm2aX;uJI9nKGi3bXHuJG1HTS1{OU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlU3QDN4IN88US=> M3TRdXNCVkeHUh?=
human SNU-423 cell NIrWNZFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJHNPXS12MkOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlU4OTl{IN88US=> M{\sNnNCVkeHUh?=
human NCI-H2291 cell MkfKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWnEdWRNUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIzQTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkW3OlEh|ryP M2jM[nNCVkeHUh?=
human OCUB-M cell M{H5SGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXrJcohq[mm2aX;uJI9nKGi3bXHuJG9EXUJvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVg{OTRizszN NWPPTY97W0GQR1XS
human KU812 cell NFv3XlRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoTiTY5pcWKrdHnvckBw\iCqdX3hckBMXThzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVk3OjhizszN NH7rdG9USU6JRWK=
human HuO9 cell NHztO5JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVfJcohq[mm2aX;uJI9nKGi3bXHuJGh2VzliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLk[xNlgh|ryP MlKzV2FPT0WU
human 639-V cell NFPOdVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4Li[WlvcGmkaYTpc44hd2ZiaIXtZY4hPjN7LW[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlY{OTR2IN88US=> MoDSV2FPT0WU
human HCC70 cell NGrGfZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{nie2lvcGmkaYTpc44hd2ZiaIXtZY4hUEOFN{CgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlY3OTR4IN88US=> NV;yZYNFW0GQR1XS
human SNB75 cell NFLvSHRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHPpWFJKdmirYnn0bY9vKG:oIHj1cYFvKFOQQke1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43PjVyODFOwG0> NYfHSplSW0GQR1XS
human D-336MG cell MnvHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4rafmlvcGmkaYTpc44hd2ZiaIXtZY4hTC1|M{\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjZ6ODFOwG0> NHKwUYVUSU6JRWK=
human LoVo cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYXJcohq[mm2aX;uJI9nKGi3bXHuJGxwXm9iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkezPFI2KM7:TR?= MV7TRW5ITVJ?
human EB2 cell NEDXcYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3L5dWlvcGmkaYTpc44hd2ZiaIXtZY4hTUJ{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63OVAyQSEQvF2= NHvTO5JUSU6JRWK=
human HSC-2 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{TlcGlvcGmkaYTpc44hd2ZiaIXtZY4hUFOFLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlc2PzJ5IN88US=> NVHJSJF3W0GQR1XS
human D-542MG cell M1X2TWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUjJcohq[mm2aX;uJI9nKGi3bXHuJGQuPTR{TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlg2ODd5IN88US=> NVnFb4V1W0GQR1XS
human COLO-684 cell NGDRfIxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYP0THZQUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVY5PCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJwMkCwN|Ih|ryP MYPTRW5ITVJ?
human GDM-1 cell NILVc5lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmiwTY5pcWKrdHnvckBw\iCqdX3hckBITE1vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNlQzODZizszN NEjZd5FUSU6JRWK=
human SW1088 cell NFSzW|JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4L3N2lvcGmkaYTpc44hd2ZiaIXtZY4hW1dzMEi4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk41QDF2MzFOwG0> M3fp[XNCVkeHUh?=
human SF295 cell NIXYeIlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVnJcohq[mm2aX;uJI9nKGi3bXHuJHNHOjl3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj63Olk2PSEQvF2= NIPVNYNUSU6JRWK=
human NCI-H2030 cell NEfjNZlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVHaZ5lMUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxOzBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkmwNlg5KM7:TR?= NEKwb|VUSU6JRWK=
human NCI-H1755 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2rpdWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixO|U2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy5{N{C2N{DPxE1? NH3BfHZUSU6JRWK=
human MDA-MB-361 cell NGf3N|FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYLJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2zOlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjV{N{C5JO69VQ>? MWLTRW5ITVJ?

... 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID