Sonidegib (NVP-LDE225)

Name: Sonidegib (NVP-LDE225)
Brand: Selleck Chemicals
SKU: S2151
Rating: 5 (47 reviews)

For research use only.

Catalog No.S2151 Synonyms: Erismodegib

47 publications

Sonidegib (NVP-LDE225) Chemical Structure

CAS No. 956697-53-3

Sonidegib (Erismodegib, NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.

Selleck's Sonidegib (NVP-LDE225) has been cited by 47 publications

Nat Med, 2014, 20(7):732-40

PubMed: 24973920 ( click the link to review the publication )

Blood, 2021, blood.2020010207

PubMed: 34424959 ( click the link to review the publication )

Sci Rep, 2021, 11(1):17665

PubMed: 34480080 ( click the link to review the publication )

Reprod Sci, 2021, 10.1007/s43032-021-00731-y

PubMed: 34642915 ( click the link to review the publication )

Genome Med, 2020, 18;12(1):17

PubMed: 32070411 ( click the link to review the publication )

Cell Rep, 2020, 30(3):771-782

PubMed: 31968252 ( click the link to review the publication )

Cells, 2020, 10(1)E53

PubMed: 33396427 ( click the link to review the publication )

Carcinogenesis, 2020, 41(7):993-1004

PubMed: 31740922 ( click the link to review the publication )

J Clin Invest, 2020, 130(8):4006-4018

PubMed: 32568216 ( click the link to review the publication )

Proc Natl Acad Sci U S A, 2019, 116(26):12986-12995

PubMed: 31182587 ( click the link to review the publication )

Neuro Oncol, 2019, 10.1093/neuonc/noz089

PubMed: 31111916 ( click the link to review the publication )

Cancers (Basel), 2019, 11(10)

PubMed: 31658643 ( click the link to review the publication )

Cancers (Basel), 2019, 11(12)

PubMed: 31835472 ( click the link to review the publication )

Stem Cell Res Ther, 2019, 10(1):289

PubMed: 31547878 ( click the link to review the publication )

Int J Biochem Cell Biol, 2019, 115:105578

PubMed: 31374250 ( click the link to review the publication )

PLoS One, 2019, 14(12):e0226570

PubMed: 31860685 ( click the link to review the publication )

Onco Targets Ther, 2019, 12:7477-7488

PubMed: 31686853 ( click the link to review the publication )

Med Sci Monit, 2019, 25:8579-8586

PubMed: 31724562 ( click the link to review the publication )

Front Pharmacol, 2019, 10:1576

PubMed: 32038250 ( click the link to review the publication )

Nat Commun, 2018, 9(1):4010

PubMed: 30275454 ( click the link to review the publication )

J Invest Dermatol, 2018, 138(4):893-902

PubMed: 29138054 ( click the link to review the publication )

Cell Death Dis, 2018, 9(10):944

PubMed: 30237504 ( click the link to review the publication )

Endocrinology, 2018, 159(2):579-596

PubMed: 29211850 ( click the link to review the publication )

PLoS One, 2018, 13(1):e0190070

PubMed: 29293549 ( click the link to review the publication )
Cell Death Dis, 2018, 9(2):142

PubMed: 29396391 ( click the link to review the publication )

J Med Chem, 2017, 60(17):7447-7458

PubMed: 28787156 ( click the link to review the publication )

Br J Cancer, 2017, 116(11):1425-1435

PubMed: 28441382 ( click the link to review the publication )

Cancer Discov, 2017,

PubMed: 28923910 ( click the link to review the publication )

BMC Cancer, 2017,

PubMed: 28806950 ( click the link to review the publication )

, 2017, 49(11):e396

PubMed: 29147013 ( click the link to review the publication )

Stem Cells Int, 2017, 2017:7507380

PubMed: 28243259 ( click the link to review the publication )

Blood, 2016, 127(10):1325-35

PubMed: 26668133 ( click the link to review the publication )

Cancer Res, 2016, 76(23):7049-7058

PubMed: 27758883 ( click the link to review the publication )

Cell Death Dis, 2016, 7(9):e2376

PubMed: 27899820 ( click the link to review the publication )

PLoS Genet, 2016, 12(9):e1006279

PubMed: 27588951 ( click the link to review the publication )

Int J Oncol, 2016, 48(2):801-12

PubMed: 26676886 ( click the link to review the publication )

PLoS One, 2016, 11(3):e0150836

PubMed: 26938241 ( click the link to review the publication )

Clin Cancer Res, 2015, 21(20):4686-97

PubMed: 26124204 ( click the link to review the publication )

Mol Cancer, 2015, 10.1186/s12943-015-0345-x

PubMed: ( click the link to review the publication )

J Hematol Oncol, 2015, 8:63

PubMed: 26048374 ( click the link to review the publication )

Oncogene, 2015, 34(29):3770-9

PubMed: 25241898 ( click the link to review the publication )

Oncogene, 2015, 10.1038/onc.2015.267

PubMed: 26189795 ( click the link to review the publication )

Mol Cancer, 2015, 14:72

PubMed: 25889650 ( click the link to review the publication )

Br J Cancer, 2014, 111(6):1168-7

PubMed: 25093491 ( click the link to review the publication )

Mol Pharmacol, 2014, 83(5):1020-9

PubMed: 23448715 ( click the link to review the publication )

Oncotarget, 2014, 5(7):1926-41

PubMed: 24732172 ( click the link to review the publication )

Nat Chem Biol, 2013, 9(4):247-9

PubMed: 23416332 ( click the link to review the publication )

Purity & Quality Control

Choose Selective Hedgehog/Smoothened Inhibitors

Biological Activity

Description

Targets

Smo (mouse) ^[1] (Cell-free assay)	Smo (human) ^[1] (Cell-free assay)
1.3 nM	2.5 nM

In vitro

Sonidegib (Erismodegib, NVP-LDE225) inhibits TM3 luciferized cell line with 0.6 nM and 8 nM, at the presence of 1 nM and 25 nM Hh agonist Ag1.5, respectively. ^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
A2780ip2	NV70TmhGS3m2b4jpZ4l1gSCjc4PhfS=>	NV7FbHB4hjFyIN88US=>			MnjKTWM2OD1zMjFOwG0>	Ml\ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NUOzOVUoRjJ{NUWzN\|U2RC:jPh?=
A2780cp20	NHXqR\|dEgXSxeHnjbZR6KGG\|c3H5	MVH+NVAh\|ryP			MkThTWM2OD15LkWg{txO	NX3Pe\|N6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OVM{PTVpPkKyOVU{OzV3PD;hQi=>
SKOV3ip1	MUPDfZRwgGmlaYT5JIF{e2G7	MYP+NVAh\|ryP			Mo\KTWM2OD1{NDFOwG0>	NEjDdII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N\|M2PSd-MkK1OVM{PTV:L3G+
SKOV3TRip2	NESyVFBEgXSxeHnjbZR6KGG\|c3H5	NVnjcZhEhjFyIN88US=>			MWnJR\|UxRTF{IN88US=>	NWfRRnQ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OVM{PTVpPkKyOVU{OzV3PD;hQi=>
HeyA8	NFe1c\|VEgXSxeHnjbZR6KGG\|c3H5	MVz+NVAh\|ryP			NUi4blZnUUN3ME2xPEDPxE1?	NYf5fG0{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1OVM{PTVpPkKyOVU{OzV3PD;hQi=>
HeyA8MDR	MYPDfZRwgGmlaYT5JIF{e2G7	NXr5cXVthjFyIN88US=>			NVS0[4RWUUN3ME24JO69VQ>?	NEXKSlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N\|M2PSd-MkK1OVM{PTV:L3G+
OS5	M{j4bmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NYDtXZVZhjVizszN			MnnPdoVlfWOnczD0bIUheHKxbHnm[ZJifGmxbh?=	MmjZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NEO1PVUoRjJ\|MkSzOVk2RC:jPh?=
OS18	MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	M1LwPZ42KM7:TR?=			MnnMdoVlfWOnczD0bIUheHKxbHnm[ZJifGmxbh?=	MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ2M{W5OUc,OjN{NEO1PVU9N2F-
Glioblastoma initiating cells	M{j2SGN6fG:6aXPpeJkh[XO\|YYm=	MUP+NVAh\|ryP			Ml3ITY5pcWKrdIOgR4VtdCCYaXHibYxqfHl?	NF;5b\|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S4NlY4OSd-MkO0PFI3PzF:L3G+
Glioblastoma initiating cells	Ml;JSpVv[3Srb36gZZN{[Xl?	NVOxPWdyhjFyIN88US=>			MXzpcohq[mm2czDu[ZVzd3OyaHXy[UBnd3KvYYTpc44>	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR6Mk[3NUc,OjN2OEK2O\|E9N2F-
Glioblastoma initiating cells	M3y5bmN6fG:6aXPpeJkh[XO\|YYm=	MoLnglExKM7:TR?=			NWOzeXh{cW6mdXPld{BieG:ydH;zbZM>	NUfBbXlMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PFI3PzFpPkKzOFgzPjdzPD;hQi=>
Glioblastoma initiating cells	MXrGeY5kfGmxbjDhd5NigQ>?	MlrSglExKM7:TR?=			M{PHV4Rwf26{ZXf1cIF1\XNidHjlJHNJUCC\|aXfuZYxqdmdicHH0bJdigQ>?	MkKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2OEK2O\|EoRjJ\|NEiyOlcyRC:jPh?=
Glioblastoma initiating cells	NUWyVJU3TnWwY4Tpc44h[XO\|YYm=	M1SwbJ4yOCEQvF2=			NHy3PVNKdmirYnn0d{B1cGViRYjwdoV{e2mxbjDv[kBI\W6nczDJcpZwdH[nZDDpckBO[WmwdHHpcolv\yCSbIXybZBwfGWwY4m=	NG\qOZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S4NlY4OSd-MkO0PFI3PzF:L3G+
Glioblastoma initiating cells	MknoSpVv[3Srb36gZZN{[Xl?	M3HnV54yOCEQvF2=			MmX4TY5pcWKrdIOgUY91cWyrdImsJGlvfmG\|aX;uMEBidmRiTXnndoF1cW:w	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzR6Mk[3NUc,OjN2OEK2O\|E9N2F-
LOX IMVI	NGHMdnhHfW6ldHnvckBie3OjeR?=	M3zzTFExKM7:TR?=		NX;EWXJ{TE2VTx?=	NXnqUIN1cW6qaXLpeJMhUGWmZ3Xoc4cuT0yLIIDheIh4[Xl?	M3TpVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OUO1PVI2Lz5{M{mzOVkzPTxxYU6=
UACC 257	M1PkZ2Z2dmO2aX;uJIF{e2G7	NYL3PZNNOTBizszN		NHiwO2dFVVOR	M{W5UolvcGmkaYTzJGhm\GenaH;nMWdNUSCyYYToe4F6	NI\ZdIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mzOVkzPSd-MkO5N\|U6OjV:L3G+
LOX IMVI	MVfGeY5kfGmxbjDhd5NigQ>?	MlHnNVAh\|ryP		M{XaZ2ROW09?	NX3CNpRYcW6mdXPld{BIOSClZXzsJIN6[2ynIHHydoV{fA>?	NXTsbld[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N\|U6OjVpPkKzPVM2QTJ3PD;hQi=>
UACC 257	MYXGeY5kfGmxbjDhd5NigQ>?	MkmyNVAh\|ryP		Mo\2SG1UVw>?	NVTCfYtIcW6mdXPld{BIOSClZXzsJIN6[2ynIHHydoV{fA>?	NYPUZnR{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N\|U6OjVpPkKzPVM2QTJ3PD;hQi=>
LOX IMVI	M2rpVmN6fG:6aXPpeJkh[XO\|YYm=	MXqxNEDPxE1?		MoXtSG1UVw>?	M1zDSYRm[3KnYYPld{B1fW2xcjDj[YxtKH[rYXLpcIl1gQ>?	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl\|NUmyOUc,OjN7M{W5NlU9N2F-
UACC 257	MlrwR5l1d3irY3n0fUBie3OjeR?=	NH3B[4oyOCEQvF2=		NFS4clZFVVOR	NFT5bVll\WO{ZXHz[ZMhfHWvb4KgZ4VtdCC4aXHibYxqfHl?	M4\2fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OUO1PVI2Lz5{M{mzOVkzPTxxYU6=
LOX IMVI	MWTBdI9xfG:\|aYOgZZN{[Xl?	M{i1[VExKM7:TR?=		NHXI[ZBFVVOR	NIjFTHRqdmS3Y3XzJIFxd3C2b4Ppdy=>	MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl\|NUmyOUc,OjN7M{W5NlU9N2F-
UACC 257	MWrBdI9xfG:\|aYOgZZN{[Xl?	NWDBSnU4OTBizszN		NXXobJk1TE2VTx?=	NX3ae\|lNcW6mdXPld{BieG:ydH;zbZM>	Mm\XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ\|OUO1PVI2RC:jPh?=
ACHN	MVrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?	NWT5Z25vhjVizszN		NWiwTmV2TE2VTx?=	NGPiRlBKSzVyPUKtN-KBkc7:TR?=	MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB7M{S5NUc,OjVyOUO0PVE9N2F-
769-P	MlnFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl?	MXL+OUDPxE1?		MmDPSG1UVw>?	MlXXTWM2OD1{LURihKnPxE1?	M2P2e\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEmzOFkyLz5{NUC5N\|Q6OTxxYU6=
786-O	NGrm[IVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NVriSYpGhjVizszN		M3nwSGROW09?	M4jzR2lEPTB;Mj2z5qCK\|ryP	MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB7M{S5NUc,OjVyOUO0PVE9N2F-
786-O SuR	NYfqc2xxT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	NFntWZZ,PSEQvF2=		NG\pVYtFVVOR	M1PjbGlEPTB;Mj2z5qCK\|ryP	MnK2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOUO0PVEoRjJ3MEmzOFkyRC:jPh?=
SP53	NVzPT\|lrTnWwY4Tpc44h[XO\|YYm=	MlP0N\|Ah\|ryP		NHy4SVFFVVOR	NXTTfJFycW6qaXLpeJMh[2WubDDh[Ihme2mxbjDhcoQhdWmpcnH0bY9v	NWnONo8zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PFU3ODhpPkK2PFg2PjB6PD;hQi=>
SP53	M4Gwb2Z2dmO2aX;uJIF{e2G7	NH7W[\|k{OCEQvF2=		NHXzTINFVVOR	Mn;kbY5pcWKrdIOgeIhmKF[OQUStcYVlcWG2ZXSgSmFMKHOrZ37hcIlv\yCyYYToe4F6	NELHVoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nki4OVYxQCd-Mk[4PFU3ODh:L3G+
HS5	M{L3fWZ2dmO2aX;uJIF{e2G7	MYCzNEDPxE1?		MlW2SG1UVw>?	MlXnbY5pcWKrdIOgZ4VtdCCjZHjld4lwdiCjbnSgcYloemG2aX;u	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh6NU[wPEc,OjZ6OEW2NFg9N2F-
HS27a	MkntSpVv[3Srb36gZZN{[Xl?	M3fld\|MxKM7:TR?=		Mo[2SG1UVw>?	NWnOOIV1cW6qaXLpeJMh[2WubDDh[Ihme2mxbjDhcoQhdWmpcnH0bY9v	MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh6NU[wPEc,OjZ6OEW2NFg9N2F-
SP53	NYjKZXpFS3m2b4jpZ4l1gSCjc4PhfS=>	NV\wcYU5OzBizszN		Mn\3SG1UVw>?	MmTkbY5lfWOnczDheZRweGijZ4m=	NVKybWNpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PFU3ODhpPkK2PFg2PjB6PD;hQi=>
Jeko	NGTNN21EgXSxeHnjbZR6KGG\|c3H5	MkjTN\|Ah\|ryP		Mn\hSG1UVw>?	NXrBXYpvcW6mdXPld{BifXSxcHjh[5k>	M1z3V\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEi1OlA5Lz5{Nki4OVYxQDxxYU6=
U2OS	MXnGeY5kfGmxbjDhd5NigQ>?		MkfBNkBpenN?		NYf6c3FbTGm\|cHzhZ4Vu\W62IH;mJHs{UF2leXPsc5BidWmwZTDmdo9uKHerbHSgeJlx\SCVbX:g[ZhxemW\|c3XkJIlvKFV{T2OgZ4VtdHNiYX\0[ZIhOiCqcoOgZpkhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygT4khRSByLkCwOkDPxE1w	Mnm4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyNkO1NlIoRjJ\|ME[zOVIzRC:jPh?=
NIH/3T3	MVzGeY5kfGmxbjDhd5NigQ>?				NYnCcGJlUW6qaXLpeIlwdiCxZjDo[YRo\WixZzDzbYdv[WyrbnegdIF1cHejeTDpckBud3W\|ZTDOTWgwO1R\|IHPlcIx{KGW6cILld5Nqdmdid3ns[EB1gXCnIGPtc{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gS4xqKG2UTlGg[ZhxemW\|c3nvckBjgSCUVD3QR3IhdWW2aH;kMEBKSzVyIE2gNE4xODR2IN88UU4>	NFK2TJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU6OSd-Mke4NVA2QTF:L3G+
NIH/3T3	NWnR[HZwTnWwY4Tpc44h[XO\|YYm=				NFK3dXlKdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHnuJI1wfXOnIF7JTE8{XDNiY3XscJMhcGG{Yn;ybY5oKFOvbzDEOFc4UCCvdYThcpQh[XO\|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJGdtcSCvUl7BJIV5eHKnc4Ppc44h[nliUmStVGNTKG2ndHjv[EwhUUN3MDC9JFAvODJ{NzFOwG0v	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW5NUc,Ojd6MUC1PVE9N2F-
NIH/3T3	NX:3[mJJTnWwY4Tpc44h[XO\|YYm=		NX62WYJoOjRiaILz		M2m4d2lvcGmkaYTpc44hd2ZiaHXk[4Vpd2dic3nncoFtcW6pIIDheIh4[XliaX6gcY92e2ViTlnIM\|NVOyClZXzsd{Bu\WG\|dYLl[EBi\nSncjCyOEBpenNiYomgS4xqNWS3YXygcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCLQ{WwJF0hOC5yME[g{txONg>?	NVnQZ2lxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QTFpPkK3PFExPTlzPD;hQi=>
TM3	NWj3T\|hoTnWwY4Tpc44h[XO\|YYm=		Mk\3OFghcHK\|		MoXNTY5pcWKrdHnvckBw\iCKaDDzbYdv[WyrbnegdIF1cHejeTDpckBud3W\|ZTDUUVMh[2WubIOgZZN{\XO\|ZXSgZZMh\G:5boLl[5Vt[XSrb36gc4YhT2yrMTDn[Y5mKGW6cILld5Nqd25iYX\0[ZIhPDhiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OCB;IECuNFAyOiEQvF2u	M2XxT\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUe2NlE2Lz5{Nkm3OlIyPTxxYU6=
NIH3T3	NWryU5V3TnWwY4Tpc44h[XO\|YYm=		MnLXOFghcHK\|		MVfJcohq[mm2aX;uJI9nKFOKSDDzbYdv[WyrbnegdIF1cHejeTDpckBud3W\|ZTDOTWg{XDNiY3XscJMhdWWjc4Xy[YQh[W[2ZYKgOFghcHK\|IHL5JGdtcS2udXPp[oVz[XOnIILldI9zfGW{IHHzd4F6NCCLQ{WwJF0hOC5yMEW1JO69VS5?	M2PqWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUe2N\|k3Lz5{NEG3OlM6PjxxYU6=
NIH3T3	MWTGeY5kfGmxbjDhd5NigQ>?		NEXyeZc1QCCqcoO=		NIiwR2RKdmirYnn0bY9vKG:oIGPvcolkNWmwZIXj[YQhcGWmZ3Xoc4che2mpbnHscIlv\yCrbjDtc5V{\SCQSVizWFMh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFfsbU1tfWOrZnXyZZNmKHKncH;yeIVzKGG\|c3H5MEBKSzVyIE2gNE4xODV3IN88UU4>	M3:0Z\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEKwOVU1Lz5{NkiyNFU2PDxxYU6=
NIH/3T3	MlXUSpVv[3Srb36gZZN{[Xl?				Mn62TY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC\|aXfuZYxqdmdicHH0bJdigSCneIDy[ZN{\WRiaX6gcY92e2ViTlnIM\|NVOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIhm\GenaH;nMYlv\HWlZXSgS4xqNTJiYXPjeY12dGG2aX;uJIF1KHSrcDDv[kBxemmvYYL5JINqdGmjIHL5JGRCWElic4ThbY5qdmdiYnHz[YQh[2:wZn;jZYwhdWmlcn;zZ49xcWNiYX7hcJl{cXN?	NG\yVWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{ixNFU6OSd-Mke4NVA2QTF:L3G+
NIH/3T3	NWi2e2NjTnWwY4Tpc44h[XO\|YYm=				M1S1V2lvcGmkaYTpc44hd2ZiaHXk[4Vpd2dic3nncoFtcW6pIIDheIh4[XliaX6gcY92e2ViTlnIM\|NVOyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIhm\GenaH;nMYlv\HWlZXSgV41wNUWJRmCgZ4ltcWG{eTD0doFve2yxY3H0bY9vKGK7IFTBVGkhe3SjaX7pcoch[mG\|ZXSgZ49v\m:lYXygcYlkem:\|Y3;wbYMh[W6jbInzbZM>	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW5NUc,Ojd6MUC1PVE9N2F-
MG 63 (6-TG R)	NVzFTFZOeUiWUzDhd5NigQ>?				NU\M[4hneUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN?	MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Rh41	M2\oVZFJXFNiYYPzZZk>				NHvtZ5lyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDRzIHPlcIx{	M2PIVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS	NGHiVoZyUFSVIHHzd4F6				M13lN5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHUuOiCRUzDj[Yxtew>?	MkLIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
A673	NFS3R3pyUFSVIHHzd4F6				NXjUWYNFeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFG2O\|Mh[2WubIO=	NIHuWno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
BT-12	M3vtNpFJXFNiYYPzZZk>				MmewdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy\|	NGDHSGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
MG 63 (6-TG R)	NEHCTpRyUFSVIHHzd4F6				MUHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN?	MmCxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1	NXr0VWlXeUiWUzDhd5NigQ>?				M1HKPJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz	NFfKW2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
OHS-50	NIXneHJyUFSVIHHzd4F6				NVL3U3c6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=>	NGDqemU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Saos-2	NVG1RW55eUiWUzDhd5NigQ>?				M4fadZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO=	M{DnWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2	MVTxTHRUKGG\|c3H5				M2\TNpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz	NES2VW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
SK-N-MC	NHP1Z\|lyUFSVIHHzd4F6				MXzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?=	NF7iTXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
SK-N-SH	MkO2dWhVWyCjc4PhfS=>				NF3QdZVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=>	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	Bcl2 / c-myc / Cyclin D1 / pERK / ERK / pJNK / JNK / Caspase 3 / Cleaved caspase 3 ; PubMed: 22821765 Blood Immunoblot experiment of protein lysate from OPM1 cells treated with NVP-LDE225 (5μM) for 12, 24, and 36 hours and fractionated by electrophoresis and stained with different Abs as shown in figure (left). Cells were treated with different concentrations o䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸 Gli-1 / Gli-2 / p-Akt / Akt; PubMed: 25093491 Br J Cancer Western blot analysis on total cell lysates from renal cancer cell lines treated with NVP-LDE225 at different concentrations. Densitometric measurements were normalised to β-actin and reported under western blot images. pp70S6K / P70s6k; PubMed: 25093491 Br J Cancer Percentage of survival of 786-O, 786-O SuR, and 769-P renal cancer cell lines treated with NVP-LDE225 and everolimus or their combination, as measured by the MTT assay. Data represent the mean (±s.d.) of three independent experiments, each performed in tr䲧疝Ỵ疞㧀疜膉痘 瘿뙠ෆᾰƌෆĀ 㺣痖帉痖Ѐ瑖堘𢡄빢᎒ෆĀ鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ�෋䐺痖暼瘿�෋ᾰƌ �෋Ð㺣痖�෋𢡄�෋䀷痗�෋౴�෋㵶痗�෋뺖᎒泌Itemｾ᎒Count﫨呂�෋猴፲� p-p130CAS / p130CAS / p-FAK / FAK / p-Paxillin / Paxillin; PubMed: 25093491 Br J Cancer Western blot analysis of total cell lysates from 786-O, 786-O SuR, and 769-P human renal cancer cell lines treated with NVP-LDE225 (2.5 μm), everolimus (1 μm), and their combination. Densitometric measurements were normalised to β-actin and reported under䲧疝Ỵ疞㧀疜膉痘 	22821765 25093491
Immunofluorescence	GLI1; PubMed: 22821765 Blood U266 were cultured in the presence of control medium or NVP-LDE225 (5μM) for 24 hours. Immunocytochemical analysis was assessed using anti-Gli1 Ab, and 4,6-diamidino-2-phenylindole was used to stain nuclei. The cells were analyzed using an epifluorescence䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ뙠ෆ䐺痖暼瘿뙠ෆᾰƌ 뙠ෆÐ㺣痖뙠ෆ𢡄뙤ෆ	22821765

In vivo

Sonidegib (Erismodegib, NVP-LDE225) is highly bound to mouse, rat, and human plasma proteins (>99%) and moderately bound to dog and monkey plasma proteins (77 and 85%, respectively). LDE225 has high permeability (90.8% in man) in the PAMPA assay. LDE225 shows good oral bioavailability ranging from 69 to 102% in preclinical species when dosed in solution. LDE225 is a weak base with a measured pK_a of 4.20 and exhibits relatively poor aqueous solubility. LDE225 demonstrates dose-related antitumor activity. At a dose of 5 mg/kg/day qd, LDE225 significantly inhibits tumor growth, corresponding to a T/C value of 33%. When dosed at 10 and 20 mg/kg/day qd, LDE225 gives rise to 51 and 83% regression, respectively. Gli1 mRNA inhibition correlates with tumor and plasma exposure of LDE225. LDE225 successfully penetrates the blood−brain barrier in tumor-bearing animals and results in tumor growth inhibition after 4 days of treatment. ^[1] LDE225 significantly reduces the tumor volume by 95.7% in Rip1-Tag2 mice. LDE225 prolongs survival in Rip1Tag2 mice. LDE225 decreases expression of stromal markers in the LDE225-treated mice. ^[2]

Protocol

Cell Research:

^[1]

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Cell lines: TM3Hh12 cells
Concentrations: ~10 μM
Incubation Time: 30 minutes
Method:
LDE225 is prepared for assay by serial dilution in DMSO and then added to empty assay plates. TM3Hh12 cells (TM3 cells containing Hh-responsive reporter gene construct pTA-8xGli-Luc) are cultured in F12 Ham's/DMEM (1:1) containing 5% horse serum, 2.5% fetal bovine serum (FBS), and 15 mM HEPES, pH 7.3. Cells are harvested by trypsin treatment, resuspended in F12 Ham's/DMEM (1:1) containing 5% horse serum and 15 mM HEPES, pH 7.3, added to assay plates, and incubated with LDE225 for approximately 30 min at 37 °C in 5% CO₂. Then 1 nM or 25 nM Ag1.5 is added to assay plates and incubated at 37 °C in the presence of 5% CO₂. After 48 hours, either Bright-Glo or MTS reagent is added to the assay plates and luminescence or absorbance at 492 nm is determined. IC50 values, defined as the inflection point of the logistic curve, are determined by nonlinear regression of the Gli-driven luciferase luminescence or absorbance signal from MTS assay vs log10 (concentration) of LDE225 using the R statistical software pack

(Only for Reference)

Animal Research:

^[1]

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Animal Models: Orthotopic Ptch^+/-p53^-/- medulloblastoma allograft model in athymic nude mice
Dosages: 40 mg/kg/day
Administration: Administered via p.o. or b.i.d
(Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	97 mg/mL (199.79 mM)
	Ethanol	97 mg/mL warmed (199.79 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+corn oil For best results, use promptly after mixing.	10mg/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 Download Sonidegib (NVP-LDE225) SDF

Molecular Weight	485.5
Formula	C₂₆H₂₆F₃N₃O₃
CAS No.	956697-53-3
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	Erismodegib
Smiles	CC1CN(CC(O1)C)C2=NC=C(C=C2)NC(=O)C3=CC=CC(=C3C)C4=CC=C(C=C4)OC(F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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

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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.

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.

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
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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

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-09-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02358161	Completed	Drug: gemcitabine and nab paclitaxel	Pancreatic Cancer	Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)\|Novartis\|Celgene Corporation	September 2015	Phase 1\|Phase 2
NCT02254551	Terminated	Drug: LDE225\|Drug: Bortezomib	Multiple Myeloma	SCRI Development Innovations LLC\|Novartis	January 2015	Phase 2
NCT02138929	Completed	Drug: Everolimus\|Drug: LDE 225	Esophageal Cancer	M.D. Anderson Cancer Center\|Novartis\|National Cancer Institute (NCI)	November 10 2014	Phase 1
NCT02195973	Completed	Drug: LDE225	Recurrent Ovarian Cancer	University of Alabama at Birmingham\|Novartis Pharmaceuticals	September 2014	Phase 1
NCT02027376	Completed	Drug: LDE225\|Drug: Docetaxel	Advanced Breast Cancer	Spanish Breast Cancer Research Group\|Novartis	May 2014	Phase 1
NCT02111187	Completed	Drug: LDE225	Prostate Cancer	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins	April 2014	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.

Hedgehog/Smoothened Signaling Pathway Map

Hedgehog/Smoothened Inhibitors with Unique Features

Smoothened Inhibitor in Clinical Trial

LDE225 (NVP-LDE225,Erismodegib) : Phase III for Hh-pathway activated relapsed Medulloblastoma (MB).
Newest Smoothened Inhibitor

GANT61 : Inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.
Smoothened Activator

Purmorphamine : Directly binds and activates Smoothened, and blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM.

Related Hedgehog/Smoothened Products

Smoothened Agonist (SAG) HCl ^New

Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.
SB225002 ^New

SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.
SB-334867 ^New

SB-334867 is a selective orexin-1 (OX1) receptor antagonist.
Vismodegib (GDC-0449)

Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay.
Cyclopamine

Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.
GANT61

GANT61 (NSC 136476) is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.
Purmorphamine

Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.
Taladegib (LY2940680)

Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.
Glasdegib (PF-04449913)

Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.

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Sonidegib (NVP-LDE225)