Basic information Safety Supplier Related

GS5829,alobresib

Basic information Safety Supplier Related

GS5829,alobresib Basic information

Product Name:
GS5829,alobresib
Synonyms:
  • GS5829,alobresib
  • Alobresib (GS-5829)
  • GS5829
  • 1H-Benzimidazole-7-methanol, 2-cyclopropyl-5-(3,5-dimethyl-4-isoxazolyl)-α,α-di-2-pyridinyl-
  • Inhibitor,GS5829,Alobresib,GS 5829,Epigenetic Reader Domain,inhibit
  • Alobresib, 10 mM in DMSO
CAS:
1637771-14-2
MF:
C26H23N5O2
MW:
437.5
Mol File:
1637771-14-2.mol
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GS5829,alobresib Chemical Properties

Boiling point:
718.9±60.0 °C(Predicted)
Density 
1.349±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:83.33(Max Conc. mg/mL);190.47(Max Conc. mM)
form 
A solid
pka
10.43±0.30(Predicted)
color 
Off-white to light yellow
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GS5829,alobresib Usage And Synthesis

Uses

Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research[1][2].

in vivo

Alobresib (10 and 20 mg/kg; oral; twice-daily; for 28 days) impaires USC-ARK2 xenograft tumor growth in female CB17/lcrHsd-Prkd/scid mice. Alobresib exhibits a significantly slower rate of tumor growth in mice, compared with vehicle control and to mice undergoing daily treatment with JQ1 (50 mg/kg/day i.p.)[1].
Alobresib (10 and 20 mg/kg; oral; twice-daily; for 28 days) is well tolerated with no clear impact on body weight compared with vehicle control[1].

Animal Model:Female CB17/lcrHsd-Prkd/scid mice (15-19 g) bearing USC-ARK2 tumors[1]
Dosage:10 and 20 mg/kg
Administration:Oral; twice-daily; 28 days
Result:Exhibited a significantly slower rate of tumor growth, compared with vehicle control and to mice undergoing daily treatment with JQ1 (50 mg/kg/day i.p.).

References

[1] Bonazzoli E, et al. Inhibition of BET Bromodomain Proteins with GS-5829 and GS-626510 in Uterine Serous Carcinoma, a Biologically Aggressive Variant of Endometrial Cancer. Clin Cancer Res. 2018 Oct 1;24(19):4845-4853. DOI:10.1158/1078-0432.CCR-18-0864
[2] Rahul Aggarwal, et al. Phase Ib Study of the BET Inhibitor GS-5829 as Monotherapy and Combined with Enzalutamide in Patients with Metastatic Castration-Resistant Prostate Cancer. Clin Cancer Res. 2022 Sep 15;28(18):3979-3989. DOI:10.1158/1078-0432.CCR-22-0175

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