BTSA1.2 | BAX activator | Probechem Biochemicals

Chemical Structure : BTSA1.2

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BTSA1.2 (BAX activator BTSA1.2)

货号: PC-72943Not For Human Use, Lab Use Only.

BTSA1.2 is a potent, selective, orally bioavailable BAX activator, demonstrated increased binding to BAX (IC50=149 nM) compared to BTSA1 (IC50=247 nM).

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生物&药学活性

BTSA1.2 is a potent, selective, orally bioavailable BAX activator, demonstrated increased binding to BAX (IC50=149 nM) compared to BTSA1 (IC50=247 nM).
BTSA1.2 also showed more potent cellular activity in a set of lymphoma cell lines compared to BTSA1(SU-DHL-4 IC50 1.24 uM vs2.29 uM, SU-DHL-6 IC50 1.75 uM vs2.6 uM).
BTSA1.2 directly engaging with cellular BAX.
BTSA1.2 demonstrated favorable properties by oral administration such as substantial half-life (T1/2 ~14 h) in mouse plasma, favorable oral bioavailability (%F ~50%) and significant plasma exposure (AUC-100 uΜ h).
BTSA1.2 treatment showed significantly better cytotoxicity in leukemia and lymphoma cell lines (mean IC50<3 uM) than in most solid tumor cell lines (mean IC50>10 uM).
BTSA1.2 and Navitoclax synergize to inhibit cell viability and induce apoptosis in various tumor cell lines.
Combination of BTSA1.2 and Navitoclax is well tolerated and does not enhance Navitoclax driven toxicity in the hematopoietic system, shows potent efficacy in resistant colorectal tumor xenografts.
BTSA1.2, a rationalized BTSA1 analog, has improved binding to BAX, cellular cytotoxicity, and is better-tolerated in vivo.

物理化学性质&存储条件

分子量	458.558
分子式	C23H18N6OS2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	4-(2-(4,5-dimethylthiazol-2-yl)hydrazono)-5-phenyl-2-(4-phenylthiazol-2-yl)-2,4-dihydro-3H-pyrazol-3-one

参考文献

1. Andrea Lopez, et al. Nat Commun. 2022 Mar 7;13(1):1199.

BTSA1.2 (BAX activator BTSA1.2)

生物&药学活性

物理化学性质&存储条件

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BTSA1.2 (BAX activator BTSA1.2)

生物&药学活性

物理化学性质&存储条件

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