Pseudolaric Acid A

N.º de catálogoE0249 Lote:E024901

Imprimir

Datos técnicos

Fórmula

C₂₂H₂₈O₆

Peso molecular

388.45

Número CAS

82508-32-5

Solubilidad (25°C)*

In vitro

DMSO

78 mg/mL (200.79 mM)

In vivo (Agregue los solventes al producto individualmente y en orden.)

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml significa ligeramente soluble o insoluble.
* Tenga en cuenta que Selleck prueba la solubilidad de todos los compuestos internamente, y la solubilidad real puede diferir ligeramente de los valores publicados. Esto es normal y se debe a ligeras variaciones entre lotes.
* Envío a temperatura ambiente (Las pruebas de estabilidad demuestran que este producto se puede enviar sin medidas de refrigeración.)

Preparación de soluciones madre

Actividad biológica

Descripción

Pseudolaric Acid A, un inhibidor de Hsp90 con una IC50 de 0,60 μM, 2,72 μM, 1,36 μM, 2,92 μM y 6,16 μM en células HL-60, A549, SMMC-7721, HeLa y SW480 respectivamente, es el principal ingrediente bioactivo en la corteza de Pseudolarix, e induce la detención del ciclo celular en la fase G2/M y promueve la muerte celular a través de la vía de la caspasa-8/caspasa-3, demostrando potentes actividades antiproliferativas y anticancerígenas.

Objetivos

Hsp90 (in HL-60 cells cytotoxicity assay)	Hsp90 (in SMMC-7721 cells cytotoxicity assay)	Hsp90 (in A549 cells cytotoxicity assay)	Hsp90 (in HeLa cells cytotoxicity assay)	Hsp90 (in SW480 cells cytotoxicity assay)
0.60 μM	1.36 μM	2.72 μM	2.92 μM	6.16 μM

In vitro

Pseudolaric Acid A es más sensible a la leucemia P-388 y al melanoma SK-MEL5, lo que sugiere que este compuesto merece un mayor desarrollo como agente antitumoral potencialmente útil.

Protocolo (de referencia)

Ensayo celular:^{^[2]}	Líneas celulares KB, A-549, HCT-8, P-388, and L-1210 tumor cells Concentraciones -- Tiempo de incubación -- Método KB screen: The KB cells are maintained on Roswell Park Memorial Institute (RMPI) 1640 media supplemented with 5 % fetal calf serum and 100 µg/ml kanamycin. The cells (5 x 10<sup>4</sup>cell/ml) are plated 24 hours before the addition of Pseudolaric Acid A. All counting of KB cells is done on a hemacytometer. Results are expressed as the dose that inhibits growth to 50 % of control growth by three days after drug addition. P-388 and L-1210 screens: The P-388 lymphocytic leukemia and L- 1210 lymphoid leukemia cells are maintained in minimum essential medium (MEM) plus 10% fetal calf serum and 100 µg/ml penicillin/ streptomycin. Cells (10<sup>4</sup>) are incubated with this compound prepared in 0.05 % tween-80 NaCI. Cells are counted in control and treated tubes on day 3 using a hemacytometer. A-549, HCT-8 screens: Media used for the propagation and growth of these cell lines are F-12 with 10% fetal calf serum (FCS) for A-549, RPMI-1640 with sodium pyruvate and 10 % horse serum for HCT- 8. All media are treated with 50 ng/ml of gentocin to prevent bacterial contamination. The cells are grown in a humidified atmosphere of 5% CO2 and 95% air at 37℃. 24-well tissue culture plates are seeded each well with approximately 1 x 10<sup>4</sup>cells per 2 ml of growth medium and incubated at 37℃ overnight. The starting cell numbers in quadruplicate wells are determined by dispersing the monolayer with trypsin-EDTA solution and the total number of cells per well is determined. This chemical in suitable concentration are added to quadruplicate wells in order to achieve a maximum treatment dosage of 10 µg/ml. After further incubation of the tissue culture plates at 37℃ for 72 h, the cell numbers in each well are determined.

Ensayo celular:^{^[2]}

Líneas celulares
KB, A-549, HCT-8, P-388, and L-1210 tumor cells
Concentraciones
--
Tiempo de incubación
--
Método
KB screen: The KB cells are maintained on Roswell Park Memorial Institute (RMPI) 1640 media supplemented with 5 % fetal calf serum and 100 µg/ml kanamycin. The cells (5 x 104cell/ml) are plated 24 hours before the addition of Pseudolaric Acid A. All counting of KB cells is done on a hemacytometer. Results are expressed as the dose that inhibits growth to 50 % of control growth by three days after drug addition. P-388 and L-1210 screens: The P-388 lymphocytic leukemia and L- 1210 lymphoid leukemia cells are maintained in minimum essential medium (MEM) plus 10% fetal calf serum and 100 µg/ml penicillin/ streptomycin. Cells (104) are incubated with this compound prepared in 0.05 % tween-80 NaCI. Cells are counted in control and treated tubes on day 3 using a hemacytometer. A-549, HCT-8 screens: Media used for the propagation and growth of these cell lines are F-12 with 10% fetal calf serum (FCS) for A-549, RPMI-1640 with sodium pyruvate and 10 % horse serum for HCT- 8. All media are treated with 50 ng/ml of gentocin to prevent bacterial contamination. The cells are grown in a humidified atmosphere of 5% CO2 and 95% air at 37℃. 24-well tissue culture plates are seeded each well with approximately 1 x 104cells per 2 ml of growth medium and incubated at 37℃ overnight. The starting cell numbers in quadruplicate wells are determined by dispersing the monolayer with trypsin-EDTA solution and the total number of cells per well is determined. This chemical in suitable concentration are added to quadruplicate wells in order to achieve a maximum treatment dosage of 10 µg/ml. After further incubation of the tissue culture plates at 37℃ for 72 h, the cell numbers in each well are determined.

Referencias

https://pubmed.ncbi.nlm.nih.gov/33991836/
https://pubmed.ncbi.nlm.nih.gov/2236294/

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