Sonidegib (NVP-LDE225)

Name: Sonidegib (NVP-LDE225)
Brand: Selleck Chemicals
SKU: S2151
Rating: 5 (44 reviews)

For research use only.

Catalog No.S2151 Synonyms: Erismodegib

44 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 44 publications

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

PubMed: 24973920 ( 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	MVHDfZRwgGmlaYT5JIF{e2G7	NYnzc21GhjFyIN88US=>			M{O2S2lEPTB;MUKg{txO	MlXsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NUOzOVUoRjJ{NUWzN\|U2RC:jPh?=
A2780cp20	M2fITmN6fG:6aXPpeJkh[XO\|YYm=	NYnRTolVhjFyIN88US=>			MU\JR\|UxRTdwNTFOwG0>	M2HibVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUWzN\|U2Lz5{MkW1N\|M2PTxxYU6=
SKOV3ip1	NXyzO4szS3m2b4jpZ4l1gSCjc4PhfS=>	NEjuPWV,OTBizszN			M3HyZ2lEPTB;MkSg{txO	M2W1WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUWzN\|U2Lz5{MkW1N\|M2PTxxYU6=
SKOV3TRip2	MXjDfZRwgGmlaYT5JIF{e2G7	MnLMglExKM7:TR?=			MYrJR\|UxRTF{IN88US=>	NGq2T\|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N\|M2PSd-MkK1OVM{PTV:L3G+
HeyA8	M3TXZmN6fG:6aXPpeJkh[XO\|YYm=	MW\+NVAh\|ryP			MYrJR\|UxRTF6IN88US=>	NGrFTI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW1N\|M2PSd-MkK1OVM{PTV:L3G+
HeyA8MDR	MVHDfZRwgGmlaYT5JIF{e2G7	M4PXd54yOCEQvF2=			NXnaOXBwUUN3ME24JO69VQ>?	Mnn3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NUOzOVUoRjJ{NUWzN\|U2RC:jPh?=
OS5	NHSyS2FIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M4PrWJ42KM7:TR?=			MXvy[YR2[2W\|IITo[UBxem:uaX\ldoF1cW:w	MmXWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NEO1PVUoRjJ\|MkSzOVk2RC:jPh?=
OS18	NGfIemRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	NGHvNXJ,PSEQvF2=			NIjMT25z\WS3Y3XzJJRp\SCycn;sbYZmemG2aX;u	MoDxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NEO1PVUoRjJ\|MkSzOVk2RC:jPh?=
Glioblastoma initiating cells	NXztOZp2S3m2b4jpZ4l1gSCjc4PhfS=>	MWn+NVAh\|ryP			M37jOmlvcGmkaYTzJGNmdGxiVnnhZoltcXS7	NIHmW2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S4NlY4OSd-MkO0PFI3PzF:L3G+
Glioblastoma initiating cells	MlnnSpVv[3Srb36gZZN{[Xl?	NHTWWnd,OTBizszN			MUXpcohq[mm2czDu[ZVzd3OyaHXy[UBnd3KvYYTpc44>	M{nYPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|NEiyOlcyLz5{M{S4NlY4OTxxYU6=
Glioblastoma initiating cells	MYnDfZRwgGmlaYT5JIF{e2G7	MkTKglExKM7:TR?=			MYPpcoR2[2W\|IHHwc5B1d3Orcx?=	NUfC[41VRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0PFI3PzFpPkKzOFgzPjdzPD;hQi=>
Glioblastoma initiating cells	M2r4N2Z2dmO2aX;uJIF{e2G7	NX25NFJ{hjFyIN88US=>			M3;L[YRwf26{ZXf1cIF1\XNidHjlJHNJUCC\|aXfuZYxqdmdicHH0bJdigQ>?	NInISmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S4NlY4OSd-MkO0PFI3PzF:L3G+
Glioblastoma initiating cells	M4[3U2Z2dmO2aX;uJIF{e2G7	NYLMWWcxhjFyIN88US=>			MUfJcohq[mm2czD0bIUhTXiycnXzd4lwdiCxZjDH[Y5meyCLbo\vcJZm\CCrbjDNZYlvfGGrbnnu[{BRdHW{aYDveIVv[3l?	M1mzNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|NEiyOlcyLz5{M{S4NlY4OTxxYU6=
Glioblastoma initiating cells	M3PSPGZ2dmO2aX;uJIF{e2G7	MVX+NVAh\|ryP			M4jqSGlvcGmkaYTzJG1wfGmuaYT5MEBKdn[jc3nvckwh[W6mIF3p[5JifGmxbh?=	M{jsS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|NEiyOlcyLz5{M{S4NlY4OTxxYU6=
LOX IMVI	MYrGeY5kfGmxbjDhd5NigQ>?	Moq0NVAh\|ryP		MkHCSG1UVw>?	NVrLOJN4cW6qaXLpeJMhUGWmZ3Xoc4cuT0yLIIDheIh4[Xl?	NXq1[nB2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N\|U6OjVpPkKzPVM2QTJ3PD;hQi=>
UACC 257	MnHKSpVv[3Srb36gZZN{[Xl?	NX;0UodTOTBizszN		NEHGe2NFVVOR	NVf4NXR4cW6qaXLpeJMhUGWmZ3Xoc4cuT0yLIIDheIh4[Xl?	M{jj[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|OUO1PVI2Lz5{M{mzOVkzPTxxYU6=
LOX IMVI	MXLGeY5kfGmxbjDhd5NigQ>?	MmOyNVAh\|ryP		MX;EUXNQ	M1LrcIlv\HWlZYOgS\|Eh[2WubDDjfYNt\SCjcoLld5Q>	NUO4SoVkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N\|U6OjVpPkKzPVM2QTJ3PD;hQi=>
UACC 257	M1W2d2Z2dmO2aX;uJIF{e2G7	MXmxNEDPxE1?		M3PLd2ROW09?	MVnpcoR2[2W\|IFexJINmdGxiY4njcIUh[XK{ZYP0	NFv1W3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mzOVkzPSd-MkO5N\|U6OjV:L3G+
LOX IMVI	MlzxR5l1d3irY3n0fUBie3OjeR?=	NWrJc\|RnOTBizszN		NWrHT\|gxTE2VTx?=	Mlrn[IVkemWjc3XzJJR2dW:{IHPlcIwhfmmjYnnsbZR6	MnXWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7M{W5NlUoRjJ\|OUO1PVI2RC:jPh?=
UACC 257	MmHmR5l1d3irY3n0fUBie3OjeR?=	MkHlNVAh\|ryP		MkfkSG1UVw>?	MlXn[IVkemWjc3XzJJR2dW:{IHPlcIwhfmmjYnnsbZR6	NIe5T2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{mzOVkzPSd-MkO5N\|U6OjV:L3G+
LOX IMVI	NUfRZ2JOSXCxcITvd4l{KGG\|c3H5	M1\NOVExKM7:TR?=		MoPXSG1UVw>?	Mo\vbY5lfWOnczDhdI9xfG:\|aYO=	NV;VXlVTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5N\|U6OjVpPkKzPVM2QTJ3PD;hQi=>
UACC 257	NUDCdGtKSXCxcITvd4l{KGG\|c3H5	NI\uTYQyOCEQvF2=		MmTXSG1UVw>?	MYHpcoR2[2W\|IHHwc5B1d3Orcx?=	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl\|NUmyOUc,OjN7M{W5NlU9N2F-
ACHN	NFXMV3lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=	M1nFOp42KM7:TR?=		MnLqSG1UVw>?	MlHjTWM2OD1{LURihKnPxE1?	M3;uSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEmzOFkyLz5{NUC5N\|Q6OTxxYU6=
769-P	NXS3SYFJT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	M3vEdZ42KM7:TR?=		MULEUXNQ	M3XPZ2lEPTB;Mj2z5qCK\|ryP	NHTPRmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC5N\|Q6OSd-MkWwPVM1QTF:L3G+
786-O	M4\RRWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7	NF36NFR,PSEQvF2=		NVTiVIpvTE2VTx?=	MXzJR\|UxRTJvM,MAje69VQ>?	MlTrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyOUO0PVEoRjJ3MEmzOFkyRC:jPh?=
786-O SuR	NVXz[5lqT3Kxd4ToJIlvcGmkaYTvdpkh[XO\|YYm=	MnOyglUh\|ryP		NVG2OHk5TE2VTx?=	NV7Oc4VEUUN3ME2yMVPjiIoQvF2=	M3vFTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEmzOFkyLz5{NUC5N\|Q6OTxxYU6=
SP53	MX7GeY5kfGmxbjDhd5NigQ>?	MmLuN\|Ah\|ryP		NFTkbGVFVVOR	NYfPeVRIcW6qaXLpeJMh[2WubDDh[Ihme2mxbjDhcoQhdWmpcnH0bY9v	NVLqZXdVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PFU3ODhpPkK2PFg2PjB6PD;hQi=>
SP53	M3jQfWZ2dmO2aX;uJIF{e2G7	NWHoUGJyOzBizszN		NVjPUWVjTE2VTx?=	NEDucnFqdmirYnn0d{B1cGViVlzBOE1u\WSrYYTl[EBHSUtic3nncoFtcW6pIIDheIh4[Xl?	NYDVPWY1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PFU3ODhpPkK2PFg2PjB6PD;hQi=>
HS5	MVXGeY5kfGmxbjDhd5NigQ>?	M3X0T\|MxKM7:TR?=		MV7EUXNQ	NWi1boxlcW6qaXLpeJMh[2WubDDh[Ihme2mxbjDhcoQhdWmpcnH0bY9v	M13jT\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEi1OlA5Lz5{Nki4OVYxQDxxYU6=
HS27a	NHjUZ4lHfW6ldHnvckBie3OjeR?=	NWHrVlJZOzBizszN		MoDRSG1UVw>?	M2L6SYlvcGmkaYTzJINmdGxiYXTo[ZNqd25iYX7kJI1q\3KjdHnvci=>	NVnMOlgyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PFU3ODhpPkK2PFg2PjB6PD;hQi=>
SP53	NF7GPHREgXSxeHnjbZR6KGG\|c3H5	NWD6cVZ2OzBizszN		Ml;ISG1UVw>?	NYXVT2t1cW6mdXPld{BifXSxcHjh[5k>	MknaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6OEW2NFgoRjJ4OEi1OlA5RC:jPh?=
Jeko	NGW1S2tEgXSxeHnjbZR6KGG\|c3H5	NW\hVVFFOzBizszN		NUPaNoI2TE2VTx?=	M4r0PYlv\HWlZYOgZZV1d3CqYXf5	NUT6WVlPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[4PFU3ODhpPkK2PFg2PjB6PD;hQi=>
U2OS	MorrSpVv[3Srb36gZZN{[Xl?		Ml\CNkBpenN?		MnPKSIl{eGyjY3Xt[Y51KG:oIGuzTH1kgWOub4DhcYlv\SCocn;tJJdqdGRidInw[UBUdW9iZYjwdoV{e2WmIHnuJHUzV1NiY3XscJMh[W[2ZYKgNkBpenNiYomgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiS3mgQUAxNjByNjFOwG0v	NETlclY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{C2N\|UzOid-MkOwOlM2OjJ:L3G+
NIH/3T3	NHO0VWZHfW6ldHnvckBie3OjeR?=				MX3Jcohq[mm2aX;uJI9nKGinZHflbI9oKHOrZ37hcIlv\yCyYYToe4F6KGmwIH3veZNmKE6LSD:zWFMh[2WubIOg[ZhxemW\|c3nu[{B4cWymIIT5dIUhW22xIHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCJbHmgcXJPSSCneIDy[ZN{cW:wIHL5JHJVNVCFUjDt[ZRpd2RuIFnDOVAhRSByLkCwOFQh\|ryPLh?=	M1P4WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5OEGwOVkyLz5{N{ixNFU6OTxxYU6=
NIH/3T3	MXXGeY5kfGmxbjDhd5NigQ>?				MmfWTY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC\|aXfuZYxqdmdicHH0bJdigSCrbjDtc5V{\SCQSVivN3Q{KGOnbHzzJIhiemKxcnnu[{BUdW9iRES3O2ghdXW2YX70JIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjDHcIkhdVKQQTDlfJBz\XO\|aX;uJIJ6KFKWLWDDVkBu\XSqb3SsJGlEPTBiPTCwMlAzOjdizszNMi=>	NWPrUIRCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QTFpPkK3PFExPTlzPD;hQi=>
NIH/3T3	NYKzWWY{TnWwY4Tpc44h[XO\|YYm=		NHTjO5kzPCCqcoO=		MVLJcohq[mm2aX;uJI9nKGinZHflbI9oKHOrZ37hcIlv\yCyYYToe4F6KGmwIH3veZNmKE6LSD:zWFMh[2WubIOgcYVie3W{ZXSgZYZ1\XJiMkSgbJJ{KGK7IFfsbU1lfWGuIHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhUUN3MDC9JFAvODB4IN88UU4>	NYDQbXp4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QTFpPkK3PFExPTlzPD;hQi=>
TM3	NV\6ZotOTnWwY4Tpc44h[XO\|YYm=		M2fDOlQ5KGi{cx?=		MnPhTY5pcWKrdHnvckBw\iCKaDDzbYdv[WyrbnegdIF1cHejeTDpckBud3W\|ZTDUUVMh[2WubIOgZZN{\XO\|ZXSgZZMh\G:5boLl[5Vt[XSrb36gc4YhT2yrMTDn[Y5mKGW6cILld5Nqd25iYX\0[ZIhPDhiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OCB;IECuNFAyOiEQvF2u	NGPndpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nkm3OlIyPSd-Mk[5O\|YzOTV:L3G+
NIH3T3	NUTEclRITnWwY4Tpc44h[XO\|YYm=		NGezXGY1QCCqcoO=		MofDTY5pcWKrdHnvckBw\iCVSFigd4lodmGuaX7nJJBifGi5YYmgbY4hdW:3c3WgUmlJO1R\|IHPlcIx{KG2nYYP1doVlKGGodHXyJFQ5KGi{czDifUBIdGlvbIXjbYZmemG\|ZTDy[ZBwenSncjDhd5NigSxiSVO1NEA:KDBwMEC1OUDPxE1w	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF5NkO5Okc,OjRzN{[zPVY9N2F-
NIH3T3	MWTGeY5kfGmxbjDhd5NigQ>?		MXS0PEBpenN?		NFr0WWpKdmirYnn0bY9vKG:oIGPvcolkNWmwZIXj[YQhcGWmZ3Xoc4che2mpbnHscIlv\yCrbjDtc5V{\SCQSVizWFMh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFfsbU1tfWOrZnXyZZNmKHKncH;yeIVzKGG\|c3H5MEBKSzVyIE2gNE4xODV3IN88UU4>	M3fLbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OEKwOVU1Lz5{NkiyNFU2PDxxYU6=
NIH/3T3	MoToSpVv[3Srb36gZZN{[Xl?				NIPPeHBKdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHX4dJJme3OnZDDpckBud3W\|ZTDOTWgwO1R\|IHPlcIx{KGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gc4YhcGWmZ3Xoc4cucW6mdXPl[EBIdGlvMjDhZ4N2dXWuYYTpc44h[XRidHnwJI9nKHC{aX3hdpkh[2muaXGgZpkhTEGSSTDzeIFqdmmwZzDiZZNm\CClb37mc4NidCCvaXPyc5Nkd3CrYzDhcoFtgXOrcx?=	MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzhzMEW5NUc,Ojd6MUC1PVE9N2F-
NIH/3T3	MVLGeY5kfGmxbjDhd5NigQ>?				NFHMZlRKdmirYnn0bY9vKG:oIHjl[IdmcG:pIIPp[45idGmwZzDwZZRpf2G7IHnuJI1wfXOnIF7JTE8{XDNiY3XscJMh[XO\|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBp\WSpZXjv[{1qdmS3Y3XkJHNudy2HR1\QJINqdGmjcomgeJJidnOub3PheIlwdiCkeTDERXBKKHO2YXnubY5oKGKjc3XkJINwdm[xY3HsJI1q[3Kxc3PvdIlkKGGwYXz5d4l{	NYrxVYh1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke4NVA2QTFpPkK3PFExPTlzPD;hQi=>
MG 63 (6-TG R)	MmHhdWhVWyCjc4PhfS=>				MmjVdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUWchPjNiKE[tWGchWiliY3XscJM>	NXrrSY5pRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41	NHvs[2lyUFSVIHHzd4F6				M4faRpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpPDFiY3XscJM>	MoX5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
U-2 OS	NWniN5dEeUiWUzDhd5NigQ>?				NWHrdWVMeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXS1{IF;TJINmdGy\|	NH\Lc\|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
A673	MWHxTHRUKGG\|c3H5				MXjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>?	NXfrbXE2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12	NITUcFdyUFSVIHHzd4F6				M3Pjb5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?=	MnS0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R)	NUDkcmlGeUiWUzDhd5NigQ>?				MVTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN?	NEPzOHU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
NB-EBc1	NETpcVdyUFSVIHHzd4F6				MU\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?=	NILBcmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
OHS-50	M2\TfpFJXFNiYYPzZZk>				NHfW[2xyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz	NFK5c4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Saos-2	MlztdWhVWyCjc4PhfS=>				MnHudWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?=	NX7SW\|Z[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2	MnrOdWhVWyCjc4PhfS=>				NX3UdFd6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM>	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-MC	MojkdWhVWyCjc4PhfS=>				M4jBWJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz	M1PaNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH	NVzkW4lzeUiWUzDhd5NigQ>?				M1PCOJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz	MWS8ZUB1[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)

Dosage

mg/kg

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% 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.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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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 )

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The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

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 2021-01-06)

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

Selective Smoothened inhibitor

PF-5274857 : Smoothened-selective, IC50=5.8 nM.
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.
SANT-1

SANT-1 directly binds to Smoothened (Smo) receptor with K_d of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.

Features:Attenuates SAG stimulation of Shh-LIGHT2 cells to a greater extent relative to other antagonists.

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Sonidegib (NVP-LDE225)