4-Thiazolecarboxylic acid, 2-[8-[(2-benzothiazolylamino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinyl]-5-[3-[4-[3-(dimethylamino)-1-propyn-1-yl]-2-fluorophenoxy]propyl]-

Name	A-1155463
Synonyms	A-1155463 A1155463. A 1155463 2-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-5-(3-(4-(3-(dimethylamino)prop-1-ynyl)-2-fluorophenoxy)propyl)thiazole-4-carboxylic acid 4-Thiazolecarboxylic acid, 2-[8-[(2-benzothiazolylamino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinyl]-5-[3-[4-[3-(dimethylamino)-1-propyn-1-yl]-2-fluorophenoxy]propyl]- 2-[8-(1,3-Benzothiazol-2-ylcarbamoyl)-3,4-dihydro-2(1H)-isoquinolinyl]-5-(3-{4-[3-(dimethylamino)-1-propyn-1-yl]-2-fluorophenoxy}propyl)-1,3-thiazole-4-carboxylic acid
CAS	1235034-55-5

Molecular Formula	C35H32FN5O4S2
Molar Mass	669.79
Density	1.45±0.1 g/cm3(Predicted)
Solubility	DMSO: ≥ 31 mg/mL
pKa	1.11±0.36(Predicted)
Storage Condition	-20℃
In vitro study	A- 1155463 disrupts the BCL-XL-BIM complex but not the BCL-2-BIM complex in the cell. A- 1155463 could kill BCL-XL-dependent Molt-4 cells (IC50=70 nM), but showed no significant cytotoxicity to RS4;11 cells (EC50>5 mM). A- 1155463 induced apoptosis markers in BCL-XL-dependent H146 cells, such as mitochondrial release of cytochrome c, caspase activation, and caspase-dependent sub-G0-G1-phase DNA content accumulation.
In vivo study	After A single intraperitoneal injection of 5 mg/kg A- 1155463 into SCID-Beige tumor-free mice, the number of platelets decreased significantly at 6 hours after injection and returned to normal levels within 72 hours after injection. SCID-Beige mice inoculated with BCL-XL-dependent H146 tumor cells were intraperitoneally injected with 5 mg/kg A- 1155463 every day. After 14 days, the A- 1155463 significantly inhibited the growth of tumors, the effect is reduced.

Last Update：2024-01-02 23:10:35

biological activity	A-1155463 is a highly potent and selective BCL-XL inhibitor. Its affinity for BCL-XL is of the picomolar order, and its binding for BCL-2, BCL-W(Ki = 19 nM), MCL-1(Ki>440 nM) is more than 1000 times weaker than BCL-XL.
Target	Value
BCL-XL (Cell-free assay)	<0.01 nM(Ki)

Last Update：2024-04-09 20:49:11

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CAS: 1235034-55-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

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4-Thiazolecarboxylic acid, 2-[8-[(2-benzothiazolylamino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinyl]-5-[3-[4-[3-(dimethylamino)-1-propyn-1-yl]-2-fluorophenoxy]propyl]- Request for Quotation