Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H3B-6545 Hydrochloride is a selective, oral estrogen receptor covalent antagonist (SERCA).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 8-10 weeks | $ 1,140.00 | |
50 mg | 8-10 weeks | $ 1,490.00 | |
100 mg | 8-10 weeks | $ 2,530.00 |
Description | H3B-6545 Hydrochloride is a selective, oral estrogen receptor covalent antagonist (SERCA). |
In vitro | H3B-6545 inhibits ERαWT activity and growth of ERαWT -positive breast cancer lines. H3B-6545 potently inhibits ERαWT activity and suppresses proliferation of ERαWT -positive breast cancer lines. With GI50s of 0.3-0.4, 1.0, 0.5, 5.2, and 0.2 nM for MCF7, HCC1428, BT483, T47D and CAMA-1 cell lines.H3B-6545 is a highly selective small molecule that potently antagonizes wild-type and mutant ERα in biochemical and cell based assays.?In vitro comparisons with standard of care and other experimental agents confirm increased cell potency of H3B-6545 under continuous as well as washout treatment conditions.?H3B-6545, a member of a novel class of ERα antagonists refer to as selective ER covalent antagonist (SERCA), which inactivates both wild-type and mutant ERα by targeting C530 and enforcing a unique antagonist conformation.?H3B-6545 is a first-in-class selective ER covalent antagonist (SERCA). |
In vivo | Administered orally once daily, H3B-6545 demonstrates potent and superior anti-tumor efficacy compared to fulvestrant in the MCF-7 xenograft model, achieving maximal effectiveness at doses notably lower than the maximum tolerated dose in mice. Furthermore, H3B-6545 exhibits enhanced anti-tumor effects over Tamoxifen and Fulvestrant in patient-derived xenograft models of estrogen receptor-positive breast cancer, including those with ERα mutations, across various species including rats and monkeys. Notably, H3B-6545 is well-tolerated across a wide dosage range, maintaining significant efficacy at exposures well above those necessary in mouse xenograft models. |
Molecular Weight | 604.04 |
Formula | C30H30ClF4N5O2 |
CAS No. | 2052132-51-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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H3B-6545 Hydrochloride 2052132-51-9 Others H3B6545 Hydrochloride H3B 6545 Hydrochloride H-3B-6545 Hydrochloride inhibitor inhibit