| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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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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| Additional Infomation |
SNX-5422 is a synthetic, novel, small molecule Hsp90 Inhibitor. As an oral formulation that demonstrates strong efficacy and tolerability, SNX-5422 is positioned as a breakthrough therapy with broad applicability across a wide range of cancers.
Drug Indication Investigated for use/treatment in cancer/tumors (unspecified). Mechanism of Action SNX-5422 is a direct, potent inhibitor of Hsp90 across a broad range of human cancer cell lines and causes degradation of important Hsp90 client proteins including HER2, AKT and ERK. Pharmacodynamics SNX-5422 is under development by Serenex. It is orally administered (pill form). Once in the body, SNX-5422 is converted to SNX-2122; that is, SNX-5422 is a prodrug of SNX-2112, which is the active form. |
| Molecular Formula |
C25H30F3N5O4
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| Molecular Weight |
521.53
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| Exact Mass |
521.224
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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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| PubChem CID |
44195571
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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 |
646.5±55.0 °C at 760 mmHg
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| Melting Point |
298-299℃
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| Flash Point |
344.8±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.637
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| LogP |
3.38
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
37
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| Complexity |
877
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AVDSOVJPJZVBTC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H30F3N5O4/c1-24(2)10-18-21(19(34)11-24)22(25(26,27)28)32-33(18)14-5-8-16(23(30)36)17(9-14)31-13-3-6-15(7-4-13)37-20(35)12-29/h5,8-9,13,15,31H,3-4,6-7,10-12,29H2,1-2H3,(H2,30,36)
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| Chemical Name |
[4-[2-carbamoyl-5-[6,6-dimethyl-4-oxo-3-(trifluoromethyl)-5,7-dihydroindazol-1-yl]anilino]cyclohexyl] 2-aminoacetate
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| Synonyms |
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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: ≥ 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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