A-1155463

ChemicalBook > CAS DataBase List > A-1155463

Product Name: A-1155463
CAS No.: 1235034-55-5
Chemical Name: A-1155463
Synonyms: A-1155463;A-1155463, 10 mM in DMSO;Exenatide acetate (free base);A-1155463; A 1155463; A1155463.;Bcl-2 Family,Inhibitor,A-1155463,inhibit;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;2-(8-(Benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-5-(3-(4-(3-(dimethylamino)prop-1-yn-1-yl)-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
CBNumber: CB13066996
Molecular Formula: C35H32FN5O4S2
Formula Weight: 669.79
MOL File: 1235034-55-5.mol

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A-1155463 Property

Density: 1.45±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: ≥67 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
form: solid
pka: 1.11±0.36(Predicted)
color: Off-white to yellow

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML3162
Product name: A-1155463
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $123
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML3162
Product name: A-1155463
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $495
Updated: 2024/03/01

Cayman Chemical

Product number: 27369
Product name: A-1155463
Packaging: 1mg
Price: $36
Updated: 2024/03/01

Cayman Chemical

Product number: 27369
Product name: A-1155463
Packaging: 25mg
Price: $450
Updated: 2024/03/01

Cayman Chemical

Product number: 27369
Product name: A-1155463
Packaging: 5mg
Price: $117
Updated: 2024/03/01

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A-1155463 Chemical Properties,Usage,Production

Uses

A-1155463 Hydrochloride, is a potent and selective BCL-XL inhibitor with in vivo activity. A-1155463 is a proteolytically stable, cell-permeable and high affinity BH3 mimetic Ligand of BCL protein BCL-XL, binding to the target potently and selectively with a Ki value of <0.01nM (<10 pM), highly selective against closely related proteins of BCL-2 (Ki = 74nM, >7000-fold selectivity), BCL-W (Ki = 8 nM, >800-fold selectivity), and MCL-1 (Ki >444nM, >40000-fold selectivity). A-1155463, together with A-1331852 , represent the first-in-class small molecule BCL-XL selective inhibitors achieving clear-on-target in vivo activity with high potency and selectivity. In living cells, A-1155463, as anticipated, experts an effort to disrupt the tight-binding BCL-XL-BIM, but not BCL-2–BIM, complexes, killi

Biological Activity

ki=19 nma-1155463 is a potent and selective bcl-xl inhibitor.bcl-2 plays a key role in the survival of lymphoid malignancies, while bcl-xl overexpression has been associated with drug resistance and disease progression of various solid tumors and hematological malignancies.

in vitro

a-1155463 was identified via nuclear magnetic resonance fragment screening and structure-based design to be a highly potent and selective bcl-xl inhibitor. a-1155463 was found to be substantially more potent against bcl-xl-dependent cell lines relative to the previously reported inhibitor, wehi-539 [1].

in vivo

animal study showed that following a single ip dose of a-1155463 at 5 mg/kg in nontumor bearing scid-beige mice, platelet counts dramatically decreased at 6 h postdose and then rebounded to normal levels within 72 h. such platelet depletion and recovery kinetics were similar to those of the dual inhibitor navitoclax. moreover, in order to give additional evidence that a-1155463 was conferring on-target in-vivo activity, a-1155463 was then administered to scidbeige mice that had been inoculated with bcl-xl-dependent h146 tumor cells. results showed that the daily ip dosing of a-1155463 at 5 mg/kg for 14 days caused a statistically significant inhibition of tumor growth, which was alleviated upon cessation of dosing [1].

target

Target	Value
BCL-XL (Cell-free assay)	<0.01 nM(Ki)

References

[1] tao zf et al. discovery of a potent and selective bcl-xl inhibitor with in vivo activity. acs med chem lett. 2014 aug 26;5(10):1088-93.

A-1155463 Preparation Products And Raw materials

Raw materials

Preparation Products

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1235034-55-5, A-1155463Related Search:

A-1155463

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

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

A-1155463; A 1155463; A1155463.

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-(Benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)-5-(3-(4-(3-(dimethylamino)prop-1-yn-1-yl)-2-fluorophenoxy)propyl)thiazole-4-carboxylic acid

Bcl-2 Family,Inhibitor,A-1155463,inhibit

Exenatide acetate (free base)

A-1155463, 10 mM in DMSO

1235034-55-5

C35H32FN5O4S2