AMG176 (Tapotoclax) | Mcl-1 inhibitor | Probechem Biochemicals

Chemical Structure : AMG176

CAS No.: 1883727-34-1

AMG176 (Tapotoclax, AMG-176)

Catalog No.: PC-70089Not For Human Use, Lab Use Only.

AMG176 (Tapotoclax, AMG-176) is a novel, potent and selective Mcl-1 inhibitor that binds with high affinity (Ki=0.06 nM) and selectivity to the BH3-binding groove of Mcl-1.

Packing	Price	Stock
1 mg	$248	In stock
5 mg	$458	In stock
10 mg	$758	In stock
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Biological Activity

AMG176 (Tapotoclax, AMG-176) is a novel, potent and selective Mcl-1 inhibitor that binds with high affinity (Ki=0.06 nM) and selectivity to the BH3-binding groove of Mcl-1.
AMG-176 disrupts the interaction between Mcl-1 and Bak, leading to downstream activation of the intrinsic apoptosis pathway in a cell based split-luciferase complementation assay (IC50=43 nM).
AMG-176 shows robust anti-tumor activity in Mcl-1 dependent cancer models.
AMG-176 is orally bioavailable.

Physicochemical Properties

M.Wt	613.21
Formula	C33H41ClN2O5S
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Spiro[5,7-etheno-1H,11H-cyclobut[i][1,4]oxazepino[3,4-f][1,2,7]thiadiazacyclohexadecine-2(3H),1'(2'H)-naphthalen]-8(9H)-one, 6'-chloro-3',4',12,13,16,16a,17,18,18a,19-decahydro-16-methoxy-11,12-dimethyl-,10,10-dioxide, (1'S,11R,12S,14E,16S,16aR,18aR)-

References

1. Sean R. Caenepeel, et al. AACR Annual Meeting 2017; April 1-5, 2017.
2, Caenepeel S, et al. Cancer Discov. 2018 Dec;8(12):1582-1597.

AMG176 (Tapotoclax, AMG-176)

Biological Activity

Physicochemical Properties

References

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