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1235034-55-5 (A-1155463)

1

Identification

A-1155463 A-1155463
Name A-1155463
Formula C35H32FN5O4S2
MW 669.79
CAS No. 1235034-55-5
EINECS
Smiles O=C(C1=C(CCCOC2=CC=C(C#CCN(C)C)C=C2F)SC(N3CC4=C(C=CC=C4C(NC5=NC6=CC=CC=C6S5)=O)CC3)=N1)O
Synonyms A1155463;A 1155463; 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
InChI InChI=1S/C35H32FN5O4S2/c1-40(2)17-6-8-22-14-15-28(26(36)20-22)45-19-7-13-30-31(33(43)44)38-35(47-30)41-18-16-23-9-5-10-24(25(23)21-41)32(42)39-34-37-27-11-3-4-12-29(27)46-34/h3-5,9-12,14-15,20H,7,13,16-19,21H2,1-2H3,(H,43,44)(H,37,39,42)
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Introduction

A-1155463 is a highly potent and selective BCL-XL inhibitor, A-1155463 shows picomolar binding affinity to BCL-XL (Ki <0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki = 80 nM) and related proteins BCL-W (Ki = 19 nM) and MCL-1 (Ki > 440 nM). IC50 value: <0.01 nM (Ki) [1] Target: BCL-XL in vitro: A-1155463 represents an excellent tool molecule for studying BCL-XL biology as well as a productive lead structure for further optimization.

Background Information

A-1155463 is a highly potent and selective BCL-XL inhibitor, A-1155463 shows picomolar binding affinity to BCL-XL (Ki <0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki = 80 nM) and related proteins BCL-W (Ki = 19 nM) and MCL-1 (Ki > 440 nM). IC50 value: <0.01 nM (Ki) [1] Target: BCL-XL in vitro: A-1155463 represents an excellent tool molecule for studying BCL-XL biology as well as a productive lead structure for further optimization. [1] A-1155463 demonstratsstrong growth inhibition of over half of the colorectal cell lines as defined by EC50 values ≤0.5 μM in the presence of 10 % FBS. [2] in vivo: A-1155463 causes a mechanism-based and reversible thrombocytopenia in mice and inhibits H146 small cell lung cancer xenograft tumor growth in vivo following multiple doses. he ability of A-1155463 to exert in vivo on-target activity was demonstrated through a rapid and reversible reduction in platelets in SCID-Beige mice following a single IP dose. Additionally, administration of A-1155463 to tumor bearing SCID-Beige mice afforded modest but statistically significant tumor growth inhibition. Detailed mechanistic studies of A-1155463 and combination activity with relevant chemotherapy across multiple tumor types will be reported in an accompanying manuscript. [1] ......by MedChemexpress Co., Ltd.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:light yellow to khaki Solid EBNumber:EB000067588

Storage condition

Store in a tightly closed container, in a cool and dry place. by MedChemexpress Co., Ltd.

Solubility

DMSO: 31mg/ml by CHEMSCENE, LLC
DMSO: 31mg/ml by MedChemexpress Co., Ltd.
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Mechanism and Indication

Signaling Pathways Apoptosis
Target Bcl-2 Family
Research Area Cancer
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
A-1155463 - No Development Reported
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Safety Data of A-1155463

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
CHEMSCENE, LLC USA
MedChemexpress Co., Ltd. 5mg/USD140(In stock);10mg/USD210(In stock);50mg/USD700(In stock);100mg/USD1150(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. China
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Related Products

Other Forms of 1235034-55-5

Name CAS No Formula MW

Recommended Compounds in Bcl-2 Family

Name CAS No Formula MW
MIM1 509102-00-5 C17H21N3O3S 347.43
713492-66-1
Gossypol-acetic acid 12542-36-8 C32H34O10 578.61
Marinopyrrole A 1227962-62-0 C22H12Cl4N2O4 510.15
WEHI-539 1431866-33-9 C31H29N5O3S2 583.72
Gambogic Acid 2752-65-0 C38H44O8 628.75
ABT-199 1257044-40-8 C45H50ClN7O7S 868.44
Apogossypol 66389-74-0 C28H30O6 462.53
Gossypol 303-45-7 C30H30O8 518.55
AT-101 90141-22-3 C30H30O8 518.55
BAM7 331244-89-4 C21H19N5O2S 405.47
SZ4TA2 406231-90-1 C28H32N4O5S2 568.71
TW-37 877877-35-5 C33H35NO6S 573.7
HA14-1 65673-63-4 C17H17BrN2O5 409.23
Obatoclax 803712-79-0 C21H23N3O4S 413.49
ABT-737 852808-04-9 C42H45ClN6O5S2 813.43
Navitoclax 923564-51-6 C47H55ClF3N5O6S3 974.61
Bax inhibitor peptide V5 579492-81-2 C27H50N6O6S 586.79
A-1331852 1430844-80-6 C38H38N6O3S 658.81
Bz 423 216691-95-1 C27H21ClN2O2 440.92

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

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More Information

A-1155463

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