| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
PF-04929113 mesylate (also known as SNX-5422 mesylate) is a potent and selective inhibitor of heat shock protein 90 (HSP90) with Kd of 41 nM, it induces Her-2 degradation with IC50 of 37 nM. PF-04929113 is a synthetic prodrug of SNX-2112 with potential antineoplastic activity. PF-04929113 is rapidly converted to SNX-2112, which accumulates in tumors relative to normal tissues. SNX-2112 inhibits Hsp90, which may result in the proteasomal degradation of oncogenic client proteins, including HER2/ERBB2, and the inhibition of tumor cell proliferation.
| ln Vitro |
|
||
|---|---|---|---|
| ln Vivo |
|
||
| Animal Protocol |
|
||
| References | |||
| Additional Infomation |
Hsp90 Inhibitor SNX-5422 Mesylate is the orally bioavailable mesylate salt of a synthetic prodrug targeting the human heat-shock protein 90 (Hsp90) with potential antineoplastic activity. Although the mechanism of action remains to be fully elucidated, Hsp90 inhibitor SNX-5422 is rapidly converted to SNX-2112, which accumulates more readily in tumors relative to normal tissues. SNX-2112 inhibits Hsp90, which may result in the proteasomal degradation of oncogenic client proteins, including HER2/ERBB2, and the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as HER2/ERBB2, AKT, RAF1, BCR-ABL, and mutated p53, as well as many other molecules that are important in cell cycle regulation or immune responses.
|
| Molecular Formula |
C26H34F3N5O7S
|
|
|---|---|---|
| Molecular Weight |
617.64
|
|
| Exact Mass |
617.213
|
|
| CAS # |
1173111-67-5
|
|
| Related CAS # |
908115-27-5;1173111-67-5 (mesylate);
|
|
| PubChem CID |
44195570
|
|
| Appearance |
Typically exists as solid at room temperature
|
|
| LogP |
5.612
|
|
| Hydrogen Bond Donor Count |
4
|
|
| Hydrogen Bond Acceptor Count |
13
|
|
| Rotatable Bond Count |
7
|
|
| Heavy Atom Count |
42
|
|
| Complexity |
969
|
|
| Defined Atom Stereocenter Count |
0
|
|
| SMILES |
S(C([H])([H])[H])(=O)(=O)O[H].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
|
|
| InChi Key |
NVGFSTMGRRADRG-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C25H30F3N5O4.CH4O3S/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;1-5(2,3)4/h5,8-9,13,15,31H,3-4,6-7,10-12,29H2,1-2H3,(H2,30,36);1H3,(H,2,3,4)
|
|
| Chemical Name |
[4-[2-carbamoyl-5-[6,6-dimethyl-4-oxo-3-(trifluoromethyl)-5,7-dihydroindazol-1-yl]anilino]cyclohexyl] 2-aminoacetate;methanesulfonic acid
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6191 mL | 8.0953 mL | 16.1907 mL | |
| 5 mM | 0.3238 mL | 1.6191 mL | 3.2381 mL | |
| 10 mM | 0.1619 mL | 0.8095 mL | 1.6191 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.
|
|---|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
