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 22 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 NVPuPGtiT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mkn1TY5pcWKrdHnvckBw\iCqdX3hckBTYEZ|OUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlAyOTV2IN88US=> MoG5V2FPT0WU
human SW982 cell NV;rVlJFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2fRXGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d7OEKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA{PTh2IN88US=> MkLwV2FPT0WU
human MAD-MB-468 cells MVHGeY5kfGmxbjDhd5NigQ>? NF;QVpZKdmirYnn0bY9vKG:oIGDJN2tj\XSjIHnuJIh2dWGwIF3BSE1OSi12NkigZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCVZYK0O|MhSWu2IIDoc5NxcG:{eXzheIlwdiCkeTDj[YxtfWyjcjDwc5RmdmO7IHHzd4F6NCCLQ{WwQVAvODRizszN NFLlOHgzPDl7Mki3OC=>
human KURAMOCHI cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkHTTY5pcWKrdHnvckBw\iCqdX3hckBMXVKDTV;DTGkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjFyNUGg{txO MWLTRW5ITVJ?
human A498 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml\TTY5pcWKrdHnvckBw\iCqdX3hckBCPDl6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xNVc6PSEQvF2= NHW0U3ZUSU6JRWK=
human YT cell M1joOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn\aTY5pcWKrdHnvckBw\iCqdX3hckB[XCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwMUKwOlYh|ryP M{S5OnNCVkeHUh?=
human VMRC-RCZ cell M2rrdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MW\Jcohq[mm2aX;uJI9nKGi3bXHuJHZOWkNvUlPaJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yPDh7ODFOwG0> Mk\VV2FPT0WU
human MDA-MB-415 cell NWO0WWo3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXLhdY9ZUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuPDF3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD6xOlc{OiEQvF2= NVfkSVBQW0GQR1XS
human J82 cell NWq1UXdFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF3pb5BKdmirYnn0bY9vKG:oIHj1cYFvKEp6MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuOFc4PzlizszN NFjZdHdUSU6JRWK=
human SW1710 cell M{XyVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NInhUopKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTJ7MjFOwG0> NEHrdmFUSU6JRWK=
human T47D cell NX3XTXRkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoDYTY5pcWKrdHnvckBw\iCqdX3hckBVPDeGIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD61N|I4KM7:TR?= Mmf1V2FPT0WU
human SU-DHL-1 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MofUTY5pcWKrdHnvckBw\iCqdX3hckBUXS2GSFytNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTZ6MUOg{txO MW\TRW5ITVJ?
human BT-20 cell NEnINVZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2ntcmlvcGmkaYTpc44hd2ZiaIXtZY4hSlRvMkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlU6OjJ{IN88US=> M2X3U3NCVkeHUh?=
human OS-RC-2 cell M{H1Nmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXjJcohq[mm2aX;uJI9nKGi3bXHuJG9UNVKFLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlYzOzh6IN88US=> MlP0V2FPT0WU
human RPMI-6666 cell Mn\QS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{T4c2lvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST22OlY3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC54NEO3PUDPxE1? NX2yWmVWW0GQR1XS
human OVCAR-3 cell MmfpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF\BOphKdmirYnn0bY9vKG:oIHj1cYFvKE:YQ1HSMVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjZ5OUS2JO69VQ>? MYrTRW5ITVJ?
human NALM-6 cell NUf6W2dNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnfZTY5pcWKrdHnvckBw\iCqdX3hckBPSUyPLU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlcxPDZ3IN88US=> MorFV2FPT0WU
human RS4-11 cell NW\uNmY2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXnYTFJ[UW6qaXLpeIlwdiCxZjDoeY1idiCUU{StNVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjd|OEC2JO69VQ>? Ml3DV2FPT0WU
human SK-MES-1 cell M1LsZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXzJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE44QDl4NzFOwG0> M3\CWnNCVkeHUh?=
human ES7 cell NF3Xc3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MojoTY5pcWKrdHnvckBw\iCqdX3hckBGWzdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkixNlg3KM7:TR?= NH3mNWNUSU6JRWK=
human NCI-H2342 cell NXrEb2pOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4\zdmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyN|QzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC56NEK5OEDPxE1? NXrjPGZoW0GQR1XS
human SCC-9 cell NVzsVY92T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4rtUmlvcGmkaYTpc44hd2ZiaIXtZY4hW0OFLUmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlg2PzdizszN MX3TRW5ITVJ?
human EW-7 cell NG\zZ|RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn;5TY5pcWKrdHnvckBw\iCqdX3hckBGXy15IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MD64OlM2PiEQvF2= MmrtV2FPT0WU
human HH cell MnXyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlW2TY5pcWKrdHnvckBw\iCqdX3hckBJUCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTBwOU[yNlIh|ryP NEf6blhUSU6JRWK=
human A427 cell NIm5[WhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFXEWZpKdmirYnn0bY9vKG:oIHj1cYFvKEF2MkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlk6PTB3IN88US=> NXXx[WhFW0GQR1XS
human Daudi cell MnXyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4LhbWlvcGmkaYTpc44hd2ZiaIXtZY4hTGG3ZHmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlA3QDh6IN88US=> MmjwV2FPT0WU
human P30-OHK cell NV7ST5JWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGK1eFJKdmirYnn0bY9vKG:oIHj1cYFvKFB|MD3PTGsh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjB5MUO4JO69VQ>? M1v4UHNCVkeHUh?=
human HGC-27 cell M1jmSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlzTTY5pcWKrdHnvckBw\iCqdX3hckBJT0NvMkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4Phfg+9lCCLQ{WwQVEvOThzNjFOwG0> MlfrV2FPT0WU
human CAMA-1 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmjMTY5pcWKrdHnvckBw\iCqdX3hckBESU2DLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlIxODFizszN MnfMV2FPT0WU
human SK-OV-3 cell M3jWOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWDJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU:YLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlIxPDR2IN88US=> NE[0VmtUSU6JRWK=
human NCI-H1048 cell MkDJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4TpfGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixNFQ5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5{MkW3PUDPxE1? MVnTRW5ITVJ?
human MEL-HO cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkTxTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlI1OjN6IN88US=> MXXTRW5ITVJ?
human NKM-1 cell M1;rR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEfUXIhKdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4zQDZ|NjFOwG0> MYHTRW5ITVJ?
human NCI-H650 cel MmP5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVnMUoZiUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFY2OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwM{CwO|Yh|ryP MkLPV2FPT0WU
human HAL-01 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnnTTY5pcWKrdHnvckBw\iCqdX3hckBJSUxvMEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlMxOTd3IN88US=> NHTuT|RUSU6JRWK=
human 786-0 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUjJcohq[mm2aX;uJI9nKGi3bXHuJFc5Pi1yIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6zNVI5OyEQvF2= MlexV2FPT0WU
human GI-1 cell M4H3OWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2DhOGlvcGmkaYTpc44hd2ZiaIXtZY4hT0lvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|E5ODhizszN M3LWXXNCVkeHUh?=
human Becker cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MULJcohq[mm2aX;uJI9nKGi3bXHuJGJm[2uncjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuN|Y{OTVizszN M{DORXNCVkeHUh?=
human CCF-STTG1 cell NFX0NmpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2\SU2lvcGmkaYTpc44hd2ZiaIXtZY4hS0OILWPUWGcyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS52MkWyOUDPxE1? NGK1OZhUSU6JRWK=
human MC116 cell M33Zbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGDBNVZKdmirYnn0bY9vKG:oIHj1cYFvKE2FMUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU41PjF{MjFOwG0> NVLtUlBwW0GQR1XS
human MDA-MB-468 cell M4fD[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1zxUWlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVQ3QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNUO3N|Yh|ryP NXTGPJVHW0GQR1XS
human NB12 cell M1jZemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXHJcohq[mm2aX;uJI9nKGi3bXHuJG5DOTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkW0PFQzKM7:TR?= MUXTRW5ITVJ?
human LXF-289 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml36TY5pcWKrdHnvckBw\iCqdX3hckBNYEZvMki5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42PTFyNDFOwG0> MWDTRW5ITVJ?
human MFE-296 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmjxTY5pcWKrdHnvckBw\iCqdX3hckBOTkVvMkm2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU42Pjh|NjFOwG0> Moj0V2FPT0WU
human SNU-423 cell NGqyeplIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFzI[XRKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT20NlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjV5MUmyJO69VQ>? MmLOV2FPT0WU
human NCI-H2291 cell NVHRT|FNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn70TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKyPVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjV5NkGg{txO MknwV2FPT0WU
human OCUB-M cell NVv4cmZwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWTJcohq[mm2aX;uJI9nKGi3bXHuJG9EXUJvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOVg{OTRizszN Mom5V2FPT0WU
human KU812 cell NUn2NnlYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M37nN2lvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlU6PjJ6IN88US=> M1HPfHNCVkeHUh?=
human HuO9 cell M{\S[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVezO4o2UW6qaXLpeIlwdiCxZjDoeY1idiCKdV:5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU43OTJ6IN88US=> M3ntbnNCVkeHUh?=
human 639-V cell M2[xfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3rtWmlvcGmkaYTpc44hd2ZiaIXtZY4hPjN7LW[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlY{OTR2IN88US=> NGf0UlRUSU6JRWK=
human HCC70 cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGhESzdyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT62OlE1PiEQvF2= NGTUbFRUSU6JRWK=
human SNB75 cell M4DRPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mkn6TY5pcWKrdHnvckBw\iCqdX3hckBUVkJ5NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuOlY2ODhizszN MXnTRW5ITVJ?
human D-336MG cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1rlZWlvcGmkaYTpc44hd2ZiaIXtZY4hTC1|M{\NS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPjZ6ODFOwG0> NYDaUG86W0GQR1XS
human LoVo cell NUn4dnZLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWL1RpRDUW6qaXLpeIlwdiCxZjDoeY1idiCOb2\vJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44Ozh{NTFOwG0> MoHDV2FPT0WU
human EB2 cell M3\veGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3y3[GlvcGmkaYTpc44hd2ZiaIXtZY4hTUJ{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT63OVAyQSEQvF2= NGTuTYhUSU6JRWK=
human HSC-2 cell M3\Zd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIe3XVdKdmirYnn0bY9vKG:oIHj1cYFvKEiVQz2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU44PTd{NzFOwG0> NHTyb4dUSU6JRWK=
human D-542MG cell NH:5T5dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NW\FcmNmUW6qaXLpeIlwdiCxZjDoeY1idiCGLUW0Nm1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS56NUC3O{DPxE1? NVXzbpVPW0GQR1XS
human COLO-684 cell NHO3cWxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2O0PWlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22PFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjJyMEOyJO69VQ>? M4PlNnNCVkeHUh?=
human GDM-1 cell NGjKOnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWPJcohq[mm2aX;uJI9nKGi3bXHuJGdFVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj6yOFIxPiEQvF2= NH7uZnRUSU6JRWK=
human SW1088 cell NYLqPXBJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYHyfI1LUW6qaXLpeIlwdiCxZjDoeY1idiCVV{GwPFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjR6MUSzJO69VQ>? MXfTRW5ITVJ?
human SF295 cell M{\FSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3\CNGlvcGmkaYTpc44hd2ZiaIXtZY4hW0Z{OUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlc3QTV3IN88US=> NFPhfFRUSU6JRWK=
human NCI-H2030 cell MnPqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYLJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkCzNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvQTB{OEig{txO Mlf4V2FPT0WU
human NCI-H1755 cell MlzWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHu1OHVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVc2PSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwMkewOlMh|ryP Mom3V2FPT0WU
human MDA-MB-361 cell MkTHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1Tod2lvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVM3OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwNUK3NFkh|ryP MV\TRW5ITVJ?

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.
  • (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 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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