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Purity: ≥98%
PF-04929113 (SNX-5422; PF04929113; PF-4929113) is a potent and selective inhibitor of heat shock protein 90 (HSP90) with potential antineoplastic activity. It inhibits HSP90 with a Kd of 41 nM. PF 04929113 exhibits excellent in vivo antitumor efficacy in fox chase SCID mice bearing MM.1S cells.
| ln Vitro |
Orally administered SNX-5422 inhibits Hsp90 with a Kd of 41 nM and causes Her-2 degradation with an IC50 of 37 nM. With IC50 values of 5 ± 1, 11 ± 3, and 61 ± 22 nM, respectively, SNX-5422 demonstrates strong effects on Her2 and p-ERK stability in AU565 cells and p -S6 in A375 cells. With an IC50 of 13 ± 3 nM, SNX-5422 also activates Hsp70 in A375 cells[1]. Cell viability is decreased in a concentration-dependent manner by SNX5422; 0.5, 1, 2, 5, and 10 μM. Furthermore, equal doses of HDAC inhibitors (PXD101, SAHA, and TSA) combined with SNX-5422 (1, 3, 5, 7 μM) synergistically cause cell death in ATC cells by suppressing PI3K/Akt/mTOR signaling[3].
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| ln Vivo |
SNX-5422 (50 mg/kg, po) administered three times a week for three weeks (qod×3/2×3) effectively suppresses the growth of tumors in the HT-29 human colon tumor xenograft model[1]. In mice, SNX-5422 (20–40 mg/kg, po) significantly reduces angiogenesis and the formation of multiple myeloma (MM) tumors[2].
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| References |
[1]. Huang KH, et al. Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents. J Med Chem. 2009 Jul 23;52(14):4288-305
[2]. Chandarlapaty S, et al. SNX2112, a synthetic heat shock protein 90 inhibitor, has potent antitumor activity against HER kinase-dependent cancers. Clin Cancer Res. 2008 Jan 1;14(1):240-8. [3]. Kim SH, et al. The heat shock protein 90 inhibitor SNX5422 has a synergistic activity with histone deacetylase inhibitors in induction of death of anaplastic thyroid carcinoma cells. Endocrine. 2016 Feb;51(2):274-82 |
| Molecular Formula |
C25H30F3N5O4
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| Molecular Weight |
521.53
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| CAS # |
908115-27-5
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| Related CAS # |
908115-27-5;1173111-67-5 (mesylate);
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| SMILES |
FC(C1C2C(C([H])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])C=2N(C2C([H])=C([H])C(C(N([H])[H])=O)=C(C=2[H])N([H])C2([H])C([H])([H])C([H])([H])C([H])(C([H])([H])C2([H])[H])OC(C([H])([H])N([H])[H])=O)N=1)=O)(F)F
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| Synonyms |
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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: ≥ 3.25 mg/mL (6.23 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 32.5 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 3.25 mg/mL (6.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 32.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 0.5% CMC+0.25% Tween 80: 25mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9174 mL | 9.5872 mL | 19.1744 mL | |
| 5 mM | 0.3835 mL | 1.9174 mL | 3.8349 mL | |
| 10 mM | 0.1917 mL | 0.9587 mL | 1.9174 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.
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