Cyclosporin A

For research use only.

Catalog No.S2286 Synonyms: Cyclosporine A

30 publications

Cyclosporin A  Chemical Structure

Molecular Weight(MW): 1202.61

Cyclosporin A is an immunosuppressive agent, binds to the cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay, widely used in organ transplantation to prevent rejection.

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Selleck's Cyclosporin A has been cited by 30 publications

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Biological Activity

Description Cyclosporin A is an immunosuppressive agent, binds to the cyclophilin and then inhibits calcineurin with IC50 of 7 nM in a cell-free assay, widely used in organ transplantation to prevent rejection.
Targets
calcineurin [1]
(Cell-free assay)
7 nM
In vitro

Cyclosporin A binds to the cyclophilin (immunophilin) in T cells[1] , forms a Cyclophilin-Cyclosporin A complex which the binds to and inhibits calcineurin. [2] Cyclosporin A inhibits calcineurin with IC50 of 7 nM[3], then blocks the nuclear translocation of NF-AT. [4] Cyclosporin A also affects mitochondria by preventing the MTP (mitochondrial permeability transition pore) from opening with an IC50 of 39 nM. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HepG2 cells MVnGeY5kfGmxbjDhd5NigQ>? NIjjW5dKdmirYnn0bY9vKG:oIHzpeoVzKHO2YXflJHBt[XOvb3TpeY0h[mW{Z3jlbUBqdm[nY4Tpc44hcW5iSHXwS|Ih[2WubIOsJGlEPTB;MT62OUBvVQ>? NH61[3ozOjV6NkGyOC=>
Jurkat cells MWfGeY5kfGmxbjDhd5NigQ>? NH3YNHZKdW23bn;zeZBxemW|c3n2[UBi[3Srdnn0fUB4[XNibXXhd5Vz\WRiYomgbY5pcWKrdHnvckBw\iC2aHWgTWwuOiCycn;keYN1cW:wIHnuJGp2emujdDDj[YxteyxiSVO1NF0zKG6P MkiwNVQ3PDN|M{e=
human PBMC MoHsSpVv[3Srb36gZZN{[Xl? MUSxJIg> NGDjWoFCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIlvKGi3bXHuJHBDVUNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjboTpMWNFOy:FREK4JIFvfGmkb3T5MYlv\HWlZXSgTWwuOiCycn;keYN1cW:wIITy[YF1\WRiZn;yJFEhcHJiYnXmc5JmKGGwdHmtR2Q{N0OGMkigZY51cWKxZImgZ4hidGynbnflJI1m[XO3cnXkJIFnfGW{IE[gbJJ{KGK7IHntcZVvd3O3cIDy[ZN{cW:wIHHzd4F6NCCHQ{WwQVMvOSCwTR?= NVLpfHNTOTl7M{O3PVU>
human Jurkat cells MVPGeY5kfGmxbjDhd5NigQ>? NX;LRpFQOSCq MXXBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHnuJIh2dWGwIFr1dotifCClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIFvfGlvQ1SzM2NFOjhiYX70bYJw\HlvaX7keYNm\CCLTD2yJJBzd2S3Y4Tpc44hfHKnYYTl[EBnd3JiMTDodkBj\W[xcnWgZY51cS2FREOvR2QzQCCjboTpZo9lgSClaHHscIVv\2VibXXhd5Vz\WRiYX\0[ZIhPiCqcoOgZpkhcW2vdX7vd5VxeHKnc4Ppc44h[XO|YYmsJGVEPTB;NTDuUS=> MonENVk6OzN5OUW=
human T-cell MVPGeY5kfGmxbjDhd5NigQ>? NYHDSFd{UW5idnn0do8hcW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJHQu[2WubDDwdo9lfWO2aX;uJI9nKGy7bYDoc4tqdmViSVytNkwhUUN3ME24MlEhdk1? M2faeFc2Ozd|M{G=
human splenocytes MnfGSpVv[3Srb36gZZN{[Xl? M1P4T|Qh\GG7cx?= MknhTY1ufW6xc4XwdJJme3OrdnWgZYN1cX[rdImgbY4hcHWvYX6gd5Bt\W6xY4n0[ZMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBcO0ifdHj5cYllcW6nIHnuZ49zeG:{YYTpc44h[W[2ZYKgOEBl[Xm|IHL5JIFtdG:pZX7pZ{BucXinZDDsfY1xcG:leYTlJJJm[WO2aX;uJIF{e2G7LDDJR|UxRTFyIH7N MYGxPVgzPzh|MR?=
mouse T cells NGPNRXNHfW6ldHnvckBie3OjeR?= NYjGO3ZZPCCmYYnz NX;oSlFwUW2vdX7vd5VxeHKnc4PpeoUh[WO2aY\peJkhcW5ibX;1d4UhXCClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJR4dyC5YYmgcYl5\WRibIntdIhw[3m2ZTDy[YFkfGmxbjDh[pRmeiB2IHThfZMh[nliTWTUJIF{e2G7LDDpZ|UxRTFzIH7N M3WzWFIzQTh2OUi3
human PBMC MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 M3:4WWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFLNR{whUUN3ME2xNkBvVQ>? Ml7DNVU3Pzl|MEm=
human MDA435/LCC6MDR cells MlzKSpVv[3Srb36gZZN{[Xl? NWfXTYpVPSCmYYnz MVjNc4R2dGG2aX;uJI9nKFBvZ4CgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCqdX3hckBOTEF2M{WvUGNEPk2GUjDj[YxteyCjc4Pld5Nm\CCjczDy[ZZmenOrbnegdIFkdGm2YYjlcEBz\XOrc4ThcoNmKG2nYYP1doVlKGG|IHPlcIwhe3W{dnn2ZYwh[W[2ZYKgOUBl[Xm|IHL5JG1VWyCjc4PhfUwhTUN3ME2wMlA{OiEQvF2u NF[1NpEzPTl6NUG5OS=>
HEK293 cells NVnRbVBITnWwY4Tpc44h[XO|YYm= MVLJcohq[mm2aX;uJI9nKE:DVGCxRlEhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJIF{e2W|c3XkJIF{KHC{b4TlbY4udWWmaXH0[YQheGm2YY\hd5RifGmwIIXweIFs\e,:jDDLbV0xNjJizszN MnS0NlI2QDd7OE[=
CK1 cells MlPBSpVv[3Srb36gZZN{[Xl? MUDBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIVHYuOzNiaX7m[YN1\WRiaX6gR2syKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geolz[WxicnXwcIlk[XSrb36gZYZ1\XJiNzDkZZl{NCCWQ{WwQVAvOyEQvF2= M4fiUlE5OjF{MUCw
mouse mammary carcinoma cell line EMT6/AR 1.0 NFrCR41HfW6ldHnvckBie3OjeR?= MXzS[ZZmenOjbDDl[oZm[3Rib36geIhmKGGlY4XteYxifGmxbjDv[kBcO0ifLTDkZZVvd3K3YnnjbY4hcW5ibX;1d4UhdWGvbXHyfUBk[XKlaX7vcYEh[2WubDDsbY5mKEWPVE[vRXIhOS5yLDDJR|UxRTBwNESg{txO M3PVN|ExODl6Nkex
KB cell M1r2XWZ2dmO2aX;uJIF{e2G7 NHLZe2ZKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhU0JiY3XscEBtcW6nIHHmeIVzKDd{IHigc4Yh\HK3ZzDlfJBwe3W{ZTygTWM2OD1yLk[g{txO NUPvO28xOTV2OEG5PVE>
mouse L5178 cells MonQSpVv[3Srb36gZZN{[Xl? MlXiNlAhdWmwcx?= MVvJcohq[mm2aX;uJI9nKGi3bXHuJGFDS0JzLX3l[IlifGWmIILoc4RidWmwZTCxNlMh\W[obIX4JIlvKG2xdYPlJGw2OTd6IHPlcIx{KGW6cILld5NqdmdiaIXtZY4hVUSUMTDh[pRmeiB{MDDtbY5{KGK7IF\BR3Mh[W6jbInzbZMtKEmFNUC9NE43PSEQvF2= MYOyNVM1OTd2NR?=
LLC-PK1 epithelial cells MoPBSpVv[3Srb36gZZN{[Xl? MVfJcohq[mm2aX;uJI9nKFBvZ3z5Z49xem:2ZXnuMEBud3W|ZTDMMY1lejGkIHX4dJJme3OnZDDpckBNVENvUFuxJIVxcXSqZXzpZYwh[2WubIOgeZNqdmdiY3HsZ4Vqdi2DTTDwc4xiemm|YYTpc44h[XO|YYpvwKwhUUN3ME2wMlch|ryP MlHzNVI3QTl|OEm=
human K562/R7 cells MonsSpVv[3Srb36gZZN{[Xl? MX:xJO69VQ>? Mon2O|IhcA>? MYXQc5RmdnSrYYTpc44hd2ZiZH;4c5J2[mmlaX6tbY5lfWOnZDDjfZRwfG:6aXPpeJkh[WejaX7zeEBld3ixcoXibYNqdi2{ZYPpd5RidnRiaIXtZY4hUzV4Mj;SO{Bk\WyuczDhd5Nme3OnZDDhd{Bld3ixcoXibYNqdiCLQ{WwJIF1KDFidV2gZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkeg{txO Moq5NlU3OzRyNEG=
A2780/ADR cells NGrjZ3lHfW6ldHnvckBie3OjeR?= MmfMTY5pcWKrdHnvckBw\iCSLXfsfYNweHKxdHXpckBmgHC{ZYPz[YQhcW5iQUK3PFAwSUSUIHPlcIx{KGK7IHPhcINmcW5iQV2gZZN{[XoxvJygTWM2OD1zLkSxNlU1KM7:TR?= NFOwN4UyPzh7MEC5OC=>
KB/MDR cell MX7GeY5kfGmxbjDhd5NigQ>? MVO3NkBp NFzqNm1KdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhU0JxTVTSJINmdGxibHnu[UBi\nSncjC3NkBpeiCxZjDkdpVoKGW6cH;zeZJmNCCLQ{WwQVEvPSEQvF2= MkHoNVU1QDF7OUG=
guinea pig ventricular myocytes NFflfWRHfW6ldHnvckBie3OjeR?= NHvicXpKdmirYnn0bY9vKG:oIFyteJlx\SClYXzjbZVuKGOqYX7u[YwhdWWjc4Xy[YQhfXOrbnege4hwdGVvY3XscEBx[XSlaDDjcIFueCCrbjDneYlv\WFicHnnJJZmdnS{aXP1cIFzKG27b3P5eIV{NCCLQ{WwQVIh|ryP M4L4dFIzPzZzMECw
human MDA435/LCC6MDR cells NIX1Z2dEgXSxdH;4bYPDqGG|c3H5 NIL5XHc4Omh? M4iyS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSTR|NT;MR2M3VUSUIHPlcIx{KGW6cILld5NqdmdiTVTSJIFnfGW{IEeyJIhze+,:jDDJR|UxRTJwODFOwG0> NYGzRWNtOjJ|MkC0NFI>
human Caco2 cells NHrTR|NHfW6ldHnvckBie3OjeR?= MlTqcohq[mm2aX;uJI9nKFBvZ4CgbY4hcHWvYX6gR4FkdzJiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJIRq\2:6aX6g[YZndHW6LDDJR|UxRTJwOTFOwG0> NGrWV4QzOzN6MkS1PC=>
leukemia CEM cells NHXXNnFHfW6ldHnvckBie3OjeR?= M{D5XmlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBJfW2jbjDNSHIyKFBvR3z5Z49xem:2ZXnuJGFDSyCWcnHud5BwenSncjD1d4lv\yCuZYXr[Y1q[SCFRV2gZ4VtdHNuIFnDOVA:Oy52IN88US=> MnLuNVI{PjF|OEe=
human HeLa cells MnO5SpVv[3Srb36gZZN{[Xl? MXXBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDIVHYuOThiaX7m[YN1\WRiaX6gbJVu[W5iSHXMZUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oII\pdoFtKHKncHzpZ4F1cW:wIHHmeIVzKDdiZHH5d-+9lCCWQ{WwQVQvPiEQvF2= NYPoNnRrOTh{MUKxNFA>
human 2008 cells M2\NfWZ2dmO2aX;uJIF{e2G7 NI[2XGVKdmirYnn0bY9vKG:oIHj1cYFvKE2UUEGgbY4hcHWvYX6gNlAxQCClZXzsd{whUUN3ME20Mlc5KM7:TR?= NWjKUlNPOTh5MEe4PFQ>
human HuH7 cells NUPZ[nN{S3m2b4TvfIlkyqCjc4PhfS=> NGOyOJJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJfUh5IHPlcIx{KGG|c3Xzd4VlKGG|IILlcIVie2Vib3[gcIFkfGG2ZTDk[Yh6\HKxZ3XuZZNmNCCLQ{WwQVUvQDFizszN NWnwbmVPOjB7NEOzPVA>
human Huh5-2 cells MWnDfZRwfG:6aXRCpIF{e2G7 M2DvWVMh\GG7cx?= MlXlR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTJVpPS1{IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZkhNCCFQ{WwQVYh|ryP M{jGWlE5PjJ3N{[2
human HuH6 cells M4HpcGN6fG:2b4jpZ:Kh[XO|YYm= NULJdYJiOyCmYYnz NHzRfWVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJfUh4IHPlcIx{KGGodHXyJFMh\GG7czDifUBOXFRiYYPzZZktKEOFNUC9O{DPxE1? NVi1Soc1OTh4MkW3OlY>
human Huh-9-13 cells M3rDNGN6fG:2b4jpZ:Kh[XO|YYm= NXr5cIF1OyCmYYnz NESyUmtEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJfWhvOT2xN{Bk\WyuczDh[pRmeiB|IHThfZMh[nliTWTUJIF{e2G778{MJGNEPTB;NzFOwG0> NVXycWNSOTh4MkW3OlY>
african green monkey Vero cells MmjxSpVv[3Srb36gZZN{[Xl? M4TVSlI1KGh? MYHBcpRqfmm{YXygZYN1cX[rdImgZYdicW6|dDDX[ZN1KE6rbHWgeolzfXNiaX7m[YN1\WRiaX6gZYZzcWOjbjDndoVmdiCvb37r[ZkhXmW{bzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckB3cXKjbDDSUmEhe3mwdHjld4l{KGGodHXyJFI1KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFnDOVA:QCEQvF2= Ml[wNVk1PTF{OE[=
human HeLa cells MknoR5l1d3SxeHnjxsBie3OjeR?= NXvaU4NpS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWOYTDj[YxteyxiVFO1NF05NjNizszN M4fFdFE5OjF{MUCw
human LCC-6 cells M1HmNGN6fG:2b4jpZ:Kh[XO|YYm= M1vp[FczKGh? MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMR2MuPiClZXzsd{Bi\nSncjC3NkBpenNuIFnDOVA:QC5|IN88US=> NIPPTYszOjN{MESwNi=>
MDCK cells NHHRcW9EgXSxdH;4bYPDqGG|c3H5 MXLDfZRwfG:6aXPpeJkh[WejaX7zeEBOTEONIHPlcIx{NCCWQ{WwQVkvQSEQvF2= M2PORlE5OjF{MUCw
human Huh-Mono cells M3ewc2N6fG:2b4jpZ:Kh[XO|YYm= MV:zJIRigXN? NFnV[mhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJfWhvTX;uc{Bk\WyuczDh[pRmeiB|IHThfZMh[nliTWTUJIF{e2G778{MJGNEPTB;MkSg{txO MVexPFYzPTd4Nh?=
mouse L929 cells NH36Z2VEgXSxdH;4bYPDqGG|c3H5 MoPyN{Bl[Xm| MV7DfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDMPVI6KGOnbHzzJIFnfGW{IEOg[IF6eyCkeTDNWHMh[XO|YYmsJGlEPTB;M{Cg{txO M1\lNlI2QTh3MUm1
rat H42E cells MkP4R5l1d3SxeHnjxsBie3OjeR?= NFPHem1EgXSxdH;4bYNqfHliYXfhbY5{fCC{YYSgTFQzTSClZXzsd{Bie3Onc4Pl[EBieyCrboTyZYNmdGy3bHHyJGFVWCCuZY\lcEwhXEN3ME20NkDPxE1? MkL0NVk2ODJyNUi=

... Click to View More Cell Line Experimental Data

In vivo Cyclosporin A is an immunosuppressive agent that is effective following either parenteral or oral administration in mice, rat and guinea pigs. [6], is clinically used in organ transplantation to prevent rejection. [7]

Protocol

Kinase Assay:[3]
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Phosphatase Assay:

Purified bovine brain calcineurin and calmodulin are purchased. Reaction mixtures with purified enzyme contains 100 nM calcineurin, 100 nM calmodulin, and 5 μM 32P-labeled phosphopeptide, in 60 μl (total volume) of assay buffer containing 20 mM Tris (pH 8), 100 mM NaCI, 6 mM MgCl2, 0.5 mM dithiothreitol, 0.1 mg of bovine serum albumin per ml, and either 0.1 mM CaCl2 or 5 mM EGTA. Reaction mixtures with cell lysates contains 20 μl of undiluted lysate, 5 μM 32P-labeled phosphopeptide, and 40 μl of assay buffer. Where indicated, reaction mixtures contains 50 μM peptide 412 or 413 and/or 500 nM okadaic acid, a specific inhibitor of phosphatases 1 and 2A; 500 nM okadaic acid is sufficient for inhibition of Ca2+-independent phosphatases, whereas higher concentrations partially inhibit Ca2+-dependent activity as well. After 15 min at 30°C, reactions are terminated by the addition of 0.5 ml of 100 mM potassium phosphate buffer (pH 7.0) containing 5% trichloroacetic acid. Free inorganic phosphate is isolated by Dowex cation-exchange chromatography and quantitated by scintillation counting as described.
Cell Research:[3]
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  • Cell lines: Jurkat cells (clone J77)
  • Concentrations: ~100 nM
  • Incubation Time: 1 hr
  • Method: Immunosuppressive agents are dissolved in ethanol at concentrations 1000-fold more than the concentration desired for cell treatments. Cells (106) are suspended in 1 ml of complete medium in microcentrifuge tubes; 1 μl of ethanol or of the ethanolic solution of Cyclosporin A is added, and the cells are incubated at 37°C for 1 hr. Cells are washed twice with 1 ml of PBS on ice and lysed in 50μl of hypotonic buffer containing 50 mM Tris (pH 7.5); 0.1 mM EGTA; 1 mM EDTA; 0.5 mM dithiothreitol; and 50 μg of phenylmethylsulfonyl fluoride, 50 μg of soybean trypsin inhibitor, 5 μg of leupeptin, and 5 μg of aprotinin per ml. Lysates are subjected to three cycles of freezing in liquid nitrogen followed by thawing at 30°C and then are centrifuged at 4°C for 10 min at 12,000×g.
    (Only for Reference)
Animal Research:[6]
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  • Animal Models: Rat
  • Dosages: 45 mg/kg
  • Administration: orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (83.15 mM)
Ethanol 100 mg/mL warmed (83.15 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/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 1202.61
Formula

C62H111N11O12

CAS No. 59865-13-3
Storage powder
in solvent
Synonyms Cyclosporine A
Smiles CCC1NC(=O)C(C(O)C(C)C\C=C\C)N(C)C(=O)C(C(C)C)N(C)C(=O)C(CC(C)C)N(C)C(=O)C(CC(C)C)N(C)C(=O)C(C)NC(=O)C(C)NC(=O)C(CC(C)C)N(C)C(=O)C(NC(=O)C(CC(C)C)N(C)C(=O)CN(C)C1=O)C(C)C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04023760 Recruiting Drug: Apixaban Pharmacokinetics|Kidney Transplant|Lung Transplant University of Saskatchewan|Saskatchewan Health Research Foundation|Lung Association of Saskatchewan June 26 2019 Phase 4
NCT03865888 Completed Drug: Cyclosporins|Drug: Tacrolimus Dry Eye|Sjogren Syndrome Pavly Moawd|Cairo University October 30 2018 Phase 3

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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Frequently Asked Questions

  • Question 1:

    What is the difference between S2286 (cyclosporin A) and S1514 (cyclosporin)?

  • Answer:

    Cyclosporine is a mixture of Cyclosporine A, derivatives of Cyclosporine A, salts of Cyclosporine A. Cyclosporine A is an especially useful Cyclosporine component.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID