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Cat. No.: HY-123827

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GPA512

Name: GPA512
Brand: MedChemExpress
SKU: HY-123827
Availability: PreOrder

GPA512 is an orally active STAT3 inhibitor and a prodrug of Galiellalactone (HY-125170). GPA512 inhibits the binding of STAT3 to DNA, downregulates STAT3-activated genes, and suppresses tumor growth in prostate cancer xenograft models. GPA512 is rapidly converted to Galiellalactone in plasma. GPA512 can be used in research related to castration-resistant prostate cancer.

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CAS No.: 1808115-35-6
화학식: C₁₇H₂₅NO₆S
분자량:371.45

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

GPA512 Chemical Structure

CAS No.: 1808115-35-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

STAT3

All STAT Isoforms :

In Vitro

OthersAnti-cancer

Others

GPA512 is rapidly converted into its active metabolite Galiellalactone (HY-125170) in plasma across species at 37°C^[1]^[2].
GPA512 (5 μM; monitored over 0-120 min) exhibits moderate symmetric permeability across Caco-2 cell monolayers, with no directional preference between absorptive and secretive transport^[2].
GPA512 (10 μM; 2 h) is completely metabolized by mouse hepatocytes within 2 h, primarily via ester hydrolysis to form carboxylic acid (compound 3), which then spontaneously converts to Galiellalactone^[2].

Anti-cancer

GPA512 (compound 6) inhibits the proliferation of human prostate cancer cell line DU145 after 72 h, with an IC₅₀ value of 4.81 μM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2
Mice^[2]	10 mg/kg	p.o.	1893 ng/mL	15 min	92 min
Mice^[2]	40 mg/kg	p.o.	3733 ng/mL	15 min	180 min
Mice^[2]	100 mg/kg	p.o.	7478 ng/mL	15 min	180 min

In Vivo

Anti-cancerApoptosisCell Cycle RegulationOthers

Anti-cancer

Apoptosis

Cell Cycle Regulation

GPA512 (compound 6) (40 mg/kg; p.o.; daily five times per week; 28 days) significantly inhibits DU145 prostate cancer xenograft growth in NMRI-nude mice by reducing tumor cell proliferation and increasing apoptosis via STAT3 pathway inhibition, with no observed toxicity^[1]^[2].

Others

GPA512 (40-400 mg/kg; p.o.; single dose) is well tolerated in male CD1 mice, with no observed toxicity^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NMRI-nude (male)^[2]
Dosage:

40 mg/kg
Administration:

p.o.; daily five times per week; 28 days
Result:

Significantly reduced tumor growth rate at day 26 and day 29.
Significantly decreased Ki67-positive cell ratio.
Significantly increased number of cleaved caspase-3-positive cells.
Significantly reduced mRNA expression of STAT3-regulated anti-apoptotic gene MCL1.
Showed non-significant decrease in BCL2 mRNA expression.
Left pSTAT3 expression unchanged in treated tumors.
Caused no weight loss, behavioral alterations, or other side effects, and all mice survived the treatment.

Animal Model:

CD1 (male, 7 weeks old, body weight 27.0-38.5 g)^[2]
Dosage:

40 mg/kg; 200 mg/kg; 400 mg/kg
Administration:

p.o.; single dose
Result:

Exhibited no toxic signs, body weight shifts or pathological abnormalities across all tested doses.

Related Protocols :

Chemical Information

CAS No. 1808115-35-6
분자량 371.45
화학식 C₁₇H₂₅NO₆S
SMILES

O[C@]12[C@@]3([C@H](SC[C@@H](C(OC)=O)NC(C)=O)[C@@H](C)C[C@]1(CC[C@]2(OC3=O)[H])[H])[H]
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Hellsten R, et al. Abstract C179: Preclinical characterization of GPA512: A prodrug of a direct STAT3 inhibitor for the treatment of prostate cancer. Mol Cancer Ther. 2015;14(12_Suppl_2):C179.

[2]. Escobar Z, et al. Preclinical Characterization of 3β-(N-Acetyl l-cysteine methyl ester)-2aβ,3-dihydrogaliellalactone (GPA512), a Prodrug of a Direct STAT3 Inhibitor for the Treatment of Prostate Cancer. Journal of medicinal chemistry. 2016 May 26;59(10):4551-62. [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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