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Purity: ≥98%
SNX-2112 (SNX2112; SNX 2112; PF-04928473; PF04928473) is a novel and potent HSP90 (Heat Shock Protein 90) with potential antitumor activity and was in phase 1 clinical trials. It selectively inhibits HSP90α and HSP90β with Ka values of 30 nM and 30 nM. It exhibits excellent in vivo antitumor efficacy in in a xenograft murine model.
| ln Vitro |
SNX-2112 is an oral active Hsp90 inhibitor that has an IC50 of 10 nM and a Kd of 16 nM for Her-2 degradation[3]. SNX-2112 binds to Hsp90; its IC50 values for Hsp90 α and β, Grp94, and Trap-1 are 30 nM, 30 nM, 4.275 μM, and 0.862 μM, respectively [1]. IC50 values for SNX-2112 range from 3 nM to 53 nM, indicating strong antiproliferative action against several types of cancer cells. With IC50 values of 11 ± 5, 41 ± 12, and 1 ± 0.6 nM, respectively, SNX-2112 exhibited strong impacts on Her2 and p-ERK stability in AU565 cells and p-S6 in A375 cells. With an IC50 of 2 ± 0.9 nM, SNX-2112 also activates Hsp70 in A375 cells[3]. Furthermore, Hsp90 client signaling, including the Akt, ERK, and NF-κB pathways, can be efficiently blocked in many cell types by SNX-2112. With IC50 values of 52, 55, 19, 186, 89, 67, 93, and 53 nM at 48 hours, SNX-2112 suppresses the proliferation of multiple myeloma (MM) cell lines, including MM.1S, U266, INA-6, RPMI8226, OPM1, OPM2, MM.1R, and Dox40 MM cell lines. Along with downregulating ERK/c-fos and PU.1, SNX-2112 (2.5–10 nM) also prevents the development of osteoclasts [4].
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| Additional Infomation |
SNX-2112 is a heat shock protein 90 (Hsp90) inhibitor.
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| Molecular Formula |
C23H27F3N4O3
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| Molecular Weight |
464.48
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| Exact Mass |
464.203
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| CAS # |
908112-43-6
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| Related CAS # |
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| PubChem CID |
24772860
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
619.8±55.0 °C at 760 mmHg
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| Melting Point |
265-266℃
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| Flash Point |
328.6±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.638
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| LogP |
3.49
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
33
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| Complexity |
754
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZFVRYNYOPQZKDG-MQMHXKEQSA-N
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| InChi Code |
InChI=1S/C23H27F3N4O3/c1-22(2)10-17-19(18(32)11-22)20(23(24,25)26)29-30(17)13-5-8-15(21(27)33)16(9-13)28-12-3-6-14(31)7-4-12/h5,8-9,12,14,28,31H,3-4,6-7,10-11H2,1-2H3,(H2,27,33)/t12-,14-
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| Chemical Name |
4-(6,6-dimethyl-4-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)-2-(((1r,4r)-4-hydroxycyclohexyl)amino)benzamide
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| Synonyms |
PF 04928473; SNX2112; SNX-2112;PF-04928473; PF04928473; SNX 2112
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% CMC+0.25% Tween 80: 30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1529 mL | 10.7647 mL | 21.5295 mL | |
| 5 mM | 0.4306 mL | 2.1529 mL | 4.3059 mL | |
| 10 mM | 0.2153 mL | 1.0765 mL | 2.1529 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02612285 | Terminated Has Results | Drug: SNX-5422 | Cancer | Esanex Inc. | March 2016 | Phase 2 |
| NCT02914327 | Withdrawn | Drug: SNX-5422 plus ibrutinib | Cancer | Esanex Inc. | February 2, 2017 | Phase 1 |
| NCT02973399 | Terminated | Drug: SNX-5422 plus ibrutinib | Cancer | Esanex Inc. | February 7, 2017 | Phase 1 |
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