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1668553-26-1 (A-1210477)

1

Identification

A-1210477 A-1210477
Name A-1210477
Formula C46H55N7O7S
MW 850.04
CAS No. 1668553-26-1
EINECS
Smiles O=C(C(N1CCN2CCOCC2)=C(CCCOC3=C4C=CC=CC4=CC=C3)C5=C1C(C6=C(COC7=CC=C(N8CCN(S(=O)(N(C)C)=O)CC8)C=C7)N(C)N=C6C)=CC=C5)O
Synonyms 7-(5-((4-(4-(N,N-dimethylsulfamoyl)piperazin-1-yl)phenoxy)methyl)-1,3-dimethyl-1H-pyrazol-4-yl)-1-(2-morpholinoethyl)-3-(3-(naphthalen-1-yloxy)propyl)-1H-indole-2-carboxylic acid
InChI InChI=1S/C46H55N7O7S/c1-33-43(41(49(4)47-33)32-60-36-19-17-35(18-20-36)51-22-24-52(25-23-51)61(56,57)48(2)3)40-14-8-13-38-39(15-9-29-59-42-16-7-11-34-10-5-6-12-37(34)42)45(46(54)55)53(44(38)40)26-21-50-27-30-58-31-28-50/h5-8,10-14,16-20H,9,15,21-32H2,1-4H3,(H,54,55)
2

Introduction

A-1210477 is an inhibitor of MCL-1 (Ki=0.45 nM in TR-FRET-binding assays), is a much weaker binder of BCL-2 (Ki=0.132 μM) and BCL-XL(Ki>0.660 μM).

Background Information

A-1210477 is an inhibitor of MCL-1 (Ki=0.45 nM in TR-FRET-binding assays), is a much weaker binder of BCL-2 (Ki=0.132 μM) and BCL-XL(Ki>0.660 μM). IC50 value: 0.45 nM (Ki) Target: MCL-1 in vitro: A-1210477 causes a dose-dependent reduction in the amount of BIM co-immunoprecipitated with MCL-1, with an IC50 in the low-μM range. A-1210477 inhibits MCL-1-NOXA interactions with an IC50 of approximately 1 μM, while having no effect on BCL-2-BIM or BCL-XL-BCL-XS interactions measured in the same cell background. A-1210477 binds to MCL-1 selectively and with sufficient affinity to disrupt MCL-1-BIM complexes in living cells. A-1210477 induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines demonstrated to be MCL-1 dependent by BH3 profiling or siRNA rescue experiments. ......by MedChemexpress Co., Ltd.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000072258

Storage condition

4°C by MedChemexpress Co., Ltd.

Solubility

10 mM in DMSO by CHEMSCENE, LLC
10 mM in DMSO 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-1210477 - Not Found
A-1210477 - No Development Reported
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Safety Data of A-1210477

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Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
CHEMSCENE, LLC USA
MedChemexpress Co., Ltd. 5mg/USD100(In stock);10mg/USD170(In stock);50mg/USD460(In stock);100mg/USD740(In stock) USA
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. China
10

Related Products

Other Forms of 1668553-26-1

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
A-1155463 1235034-55-5 C35H32FN5O4S2 669.79

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

12

References

13

More Information

A-1210477

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