SNX-2112 (PF-04928473)


SNX-2112 (PF-04928473)化学構造


SNX-2112 (PF-04928473) selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG.

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  • Mol Cell Biol 2013 33(12), 2375-87. SNX-2112 (PF-04928473) purchased from Selleck.


HSP (e.g. HSP90)阻害剤の選択性比較


製品説明 SNX-2112 (PF-04928473) selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG.
HSP90α [1]
(cell-free assay)
HSP90β [1]
(cell-free assay)
30 nM(Ka) 30 nM(Ka)

Treatment of BT-474 cells with 1 μM SNX-2112 results in down-regulation of HER2 expression within 3 to 6 hours of drug exposure with near-complete loss of HER2 expression by 10 hours. Treatment with SNX-2112 also results in a decline in total Akt expression. SNX-2112 inhibits cell proliferation with IC50 values ranging from 10 to 50 nM, in BT474, SKBR-3, SKOV-3, MDA-468, MCF-7 and H1650 cancer cells. And these antiproliferative effects are associated with hypophosphorylation of Rb, arrest of G1 and modest levels of apotosis. [1] SNX-2112 competitively binds to the N-terminal adenosine triphosphate binding site of Hsp90. SNX-2112 induces apoptosis via caspase-8, -9, -3, and poly (ADPribose) polymerase cleavage. SNX-2112 inhibits cytokine-inducedAkt and extracellular signal-related kinase (ERK) activation and also overcomes the growth advantages conferred by interleukin-6, insulin-like growth factor-1, and bone marrow stromal cells. SNX-2112 inhibits tube formation by human umbilical vein endothelial cells via abrogation of eNOS/Akt pathway and markedly inhibits osteoclast formation via down-regulation of ERK/c-fos and PU.1. [2] Cell lines (eight cell lines from osteosarcoma, neuroblastoma, hepatoblastoma, and ymphoma) studied demonstrates sensitivity to SNX-2112 with IC50 values ranging from 10-100 nM. A higher dose (70 nM) exhibits a more prolonged inhibition and larger sub-G1 accumulation. Observed levels of Akt1 and C-Raf are markedly reduced over time along with an increase in PARP cleavage. [3] A recent research indicates NX-2112 induces autophagy in a time- and dose-dependent manner via Akt/mTOR/p70S6K inhibition. SNX-2112 induces significant apoptosis and utophagy in human melanoma A-375 cells, and may be an effective targeted therapy agent. [4]

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A375 cells MXHGeY5kfGmxbjDhd5NigQ>? M1TlNlI1KGh? MknSTY5pcWKrdHnvckBw\iCKc4C5NEBqdiCqdX3hckBCOzd3IHPlcIx{KGG|c3Xzd4VlKGG|IIDTOkBl\We{YXTheIlwdiCjZoTldkAzPCCqcoOgZpkhcGmpaDDjc451\W62IIPjdoVmdmmwZzygTWM2OD1yLkCwNUDPxE1? NELhZY8yQTV3MkSzNy=>
LNCAP cells NGnXc4xRem:uaX\ldoF1cW:wIHHzd4F6 NGXSW2w4Oi1zNESgbC=> M2jU[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DRXAh[2WubIOgZYZ1\XJiN{KgeI8hOTR2IHjyd{BjgSCleYH1ZY51KESQQTDkfYUhdWW2aH;kMEBKSzVyPUCuNFA{KM7:TR?= MmPzNVk2PTJ2M{O=
human SW620 cells MW\Qdo9tcW[ncnH0bY9vKGG|c3H5 NFPv[o44Oi1zNESgbC=> Mn7vRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVV{[yNEBk\WyuczDh[pRmeiB5MjD0c{AyPDRiaILzJIJ6KGO7cYXhcpQhTE6DIHT5[UBu\XSqb3SsJGlEPTB;MD6wNFMh|ryP NUXPUmdlOTl3NUK0N|M>
HT-29 cells MUPQdo9tcW[ncnH0bY9vKGG|c3H5 NYTVWohNPzJvMUS0JIg> MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHHmeIVzKDd{IITvJFE1PCCqcoOgZpkh[3mzdXHueEBFVkFiZInlJI1mfGixZDygTWM2OD1yLkCwN{DPxE1? NUDDOJZEOTl3NUK0N|M>
human SK-MEL-5 cells M4rBR3Bzd2yrZnXyZZRqd25iYYPzZZk> M4HaO|czNTF2NDDo MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV3FUE02KGOnbHzzJIFnfGW{IEeyJJRwKDF2NDDodpMh[nliY4nxeYFvfCCGTlGg[JlmKG2ndHjv[EwhUUN3ME2wMlAxPiEQvF2= NIHHU5QyQTV3MkSzNy=>
sf9 cells MknSSpVv[3Srb36gZZN{[Xl? NES0UmY{KGh? MXrCbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIF6teIVzdWmwYXygdI9tgUircz30ZYdo\WRiSGPQPVBj\XSjIDjEPUB1dyCHMkO2LUBmgHC{ZYPz[YQhcW5iaX7z[YN1KHOoOTDj[YxteyCjZoTldkA{KGi{czDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7LDDLbV0xNjByNjFOwG0> Mn;5NlQ{OzJ2OEi=
K562 cells MlHzVJJwdGmoZYLheIlwdiCjc4PhfS=> NFnOVIs4Oi1zNESgbC=> Mn7rRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHHmeIVzKDd{IITvJFE1PCCqcoOgZpkh[3mzdXHueEBFVkFiZInlJI1mfGixZDygTWM2OD1yLkCwOkDPxE1? MnPvNVk2PTJ2M{O=
MDA-MB-231 cells Mn7wVJJwdGmoZYLheIlwdiCjc4PhfS=> MlPyO|IuOTR2IHi= MlrXRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGGodHXyJFczKHSxIEG0OEBpenNiYomgZ5lyfWGwdDDEUmEh\HmnIH3leIhw\CxiSVO1NF0xNjByNjFOwG0> MX2xPVU2OjR|Mx?=
PC3 cells NEHFOlNRem:uaX\ldoF1cW:wIHHzd4F6 MVK3Nk0yPDRiaB?= NYPrfmdCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiN{KgeI8hOTR2IHjyd{BjgSCleYH1ZY51KESQQTDkfYUhdWW2aH;kMEBKSzVyPUCuNFE4KM7:TR?= M3m5bVE6PTV{NEOz
NCI-H460 cells MkKwVJJwdGmoZYLheIlwdiCjc4PhfS=> M4DsSVczNTF2NDDo M{DRTGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg1PjBiY3XscJMh[W[2ZYKgO|IhfG9iMUS0JIhzeyCkeTDjfZF2[W62IFTORUBlgWVibXX0bI9lNCCLQ{WwQVAvODF6IN88US=> M4DXdlE6PTV{NEOz
MCF7 cells MXLGeY5kfGmxbjDhd5NigQ>? NFLPbGlKdmirYnn0bY9vKG:oIFjTVFkx[WyyaHGgbY4hcHWvYX6gUWNHPyClZXzsd{Bie3Onc4Pl[EBieyCmZXfyZYRifGmxbjDv[kBJ\XJvMjygSWM2OD1yLkCxPUDPxE1? NITDbm0zOjl|OECzNC=>
AU565 cells MYjGeY5kfGmxbjDhd5NigQ>? NIDONGIzPCCq MXPJcohq[mm2aX;uJI9nKEi|cEmwJIlvKGi3bXHuJGFWPTZ3IHPlcIx{KGG|c3Xzd4VlKGG|IIDFVmsh\GWpcnHkZZRqd25iYX\0[ZIhOjRiaILzJIJ6KGirZ3igZ49vfGWwdDDzZ5Jm\W6rbnesJGlEPTB;MD6wOFEh|ryP M4PSNlE6PTV{NEOz
HCT15 cells MXXQdo9tcW[ncnH0bY9vKGG|c3H5 NWTjSYt[PzJvMUS0JIg> MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEG1JINmdGy|IHHmeIVzKDd{IITvJFE1PCCqcoOgZpkh[3mzdXHueEBFVkFiZInlJI1mfGixZDygTWM2OD1yLkC1NkDPxE1? M3XSRVE6PTV{NEOz
MRC5 cells NYD5R|FOS3m2b4TvfIlkcXS7IHHzd4F6 MVK0PEBp MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNVmM2KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGNEPTB;MkGuN|Qh|ryP MYGyNlcxPDh7MB?=


体内試験 SNX-2112, delivered by its prodrug SNX-5422, inhibits MM cell growth and prolongs survival in a xenograft murine model and blockade of Hsp90 by SNX-2112 not only inhibits MM cell growth but also acts in the bone marrow microenvironment to block angiogenesis and osteoclastogenesis. [2]


+ 展開

ATP Displacement Assay:

For the protein affinity-displacement assay, a purine-based affinity resin is generated by incubating ATP-linked Sepharose with Jurkat cell lysate (flash frozen and homogenized in saline) at 4 °C. This is then incubated with SNX-2112 for 90 minutes. Proteins eluted by drug are then resolved by SDS-PAGE, visualized with silver staining, and excised from the gel for MS-based identification. Briefly, after destaining and trypsin digestion, peptides are extracted with μC18 ZipTips and then eluted and spotted directly to a conventional stainless steel matrix-assisted laser desorption/ionization target with a saturated solution of α-cyano-4- hydroxycinnamic acid in 50% acetonitrile, 0.15% formic acid. Mass spectra are then acquired using a MALDI-TOF/TOF 4700 Proteomics Analyzer. MS spectra are acquired (1,000 shots per spectrum), and the three peaks from each with the greatest signal-to-noise ratio are automatically submitted for tandem MS analysis (3000 shots per spectrum). The collision energy is 1keV. Air is used as the collision gas. Protein identification is done from the MS and tandem MS data using GPS Explorer software with the integrated Mascot database search engine.
細胞試験: [1]
+ 展開
  • 細胞株: BT474, SKBR-3, SKOV-3, MDA-468, MCF-7 and H1650 cancer cells
  • 濃度: 0-500 nM
  • 反応時間: 24 hours
  • 実験の流れ: Cell viability is determined by seeding 2-5 × 103 cells per well in 96- well plates and treating with SNX-2112 24 hours after plating in complete medium (200 μL). Each drug concentration is tested in eight wells. Cells are assayed using the Alamar blue viability test after a 96-h incubation. Flow cytometry is done using nuclei stained with ethidium bromide and isolated via the Nusse protocol
+ 展開
  • 動物モデル: 5 × 106 MM.1S cells are inoculated subcutaneously in the Fox Chase SCID mice (6-7 weeks old).
  • 製剤: SNX-5422 is dissolved in 1% carboxy methylcellulose/0.5% Tween 80 at 10 mg/mL and stored at 4 °C for in vivo stud
  • 投薬量: 20 or 40 mg/kg
  • 投与方法: SNX-5422 is administered orally 3 times per week, total 3 weeks.

溶解度 (25°C)

体外 DMSO 93 mg/mL (200.22 mM)
Ethanol 1 mg/mL (2.15 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
0.5% CMC+0.25% Tween 80
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。


分子量 464.48


CAS No. 908112-43-6
in solvent
別名 N/A





質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)


  • 質量





開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1



  • 連続希釈剤

  • 計算結果

  • 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):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


質量 濃度 体積 分子量



Handling Instructions


  • * 必須

HSP (e.g. HSP90)シグナル伝達経路

HSP (e.g. HSP90) Inhibitors with Unique Features

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID