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1414943-88-6 (BAY-1143572 Racemate)

1

Identification

BAY-1143572 Racemate BAY-1143572 Racemate
Name BAY-1143572 Racemate
Formula C18H18FN5O2S
MW 387.43
CAS No. 1414943-88-6
EINECS
Smiles N=S(CC1=CC(NC2=NC(C3=CC=C(F)C=C3OC)=NC=N2)=CC=C1)(C)=O
Synonyms BAY 1143572;BAY1143572
InChI InChI=1S/C18H18FN5O2S/c1-26-16-9-13(19)6-7-15(16)17-21-11-22-18(24-17)23-14-5-3-4-12(8-14)10-27(2,20)25/h3-9,11,20H,10H2,1-2H3,(H,21,22,23,24)
2

Introduction

BAY 1143572 is a highly selective, potent and orally available inhibitor of PTEFb/CDK9; inhibits the proliferation of AML cell lines with a median IC50 of 385 nM.

Background Information

BAY 1143572 is a highly selective, potent and orally available inhibitor of PTEFb/CDK9; inhibits the proliferation of AML cell lines with a median IC50 of 385 nM. ......by MedChemexpress Co., Ltd.
Atuveciclib, also known as BAY1143572, is a highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I. BAY1143572 inhibits MYC and shows convincing anti-tumor activity in multiple xenograft models by the induction of apoptosis. BAY 1143572 had potent and highly selective PTEFb-kinase inhibitory activity in the low nanomolar range against PTEFb/CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY 1143572 also showed single agent in vivo efficacy at tolerated doses in various xenograft tumor models in mice and rats upon once daily oral administration. ......by MedKoo Biosciences, Inc.
Atuveciclib (BAY-1143572) is a potent, highly selective, orally bioavailable CDK9/P-TEFb inhibitor with IC50 of 6 nM for CDK9/CyclinT1; displays >150-fold selectivity over CDK1/2/3/5/6/7 (IC50>800 nM), also shows submicromolar inhibitory activity against GSK3α (IC50=45 nM), GSK3β (IC50=87 nM); demonstrates antiproliferative activity against HeLa cells (IC50=920 nM) and MOLM‐13 cells (IC50=310 nM); exhibits anticancer activity in human AML models.Blood CancerPhase 1 Clinical ......by ProbeChem
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance: EBNumber:EB000070804

Storage condition

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 Cell Cycle/DNA Damage
Target CDK
Research Area Cancer
Indications Leukemia Neoplasms
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
BAY-1143572 Racemate Bayer Leukemia 2015/2/19 Phase 1
BAY-1143572 Racemate Bayer Neoplasms 2013/9/1 Phase 1
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Safety Data of BAY-1143572 Racemate

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
CHEMSCENE, LLC 1mg/USD180();5mg/USD420() USA
MedChemexpress Co., Ltd. 1mg/USD180();5mg/USD420() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Shanghai Haoyuan Chemexpress Co., Ltd. 1mg/USD180();5mg/USD420() China
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Related Products

Other Forms of 1414943-88-6

Name CAS No Formula MW

Recommended Compounds in CDK

Name CAS No Formula MW
LY2857785 1619903-54-6 C26H36N6O 448.6
THZ2 1604810-84-5 C31H28ClN7O2 566.0527
Palbociclib (isethionate) 827022-33-3 C26H35N7O6S 573.66
CDK9-IN-6 1391855-95-0 C27H37ClN6O2 513.07468
ML167 1285702-20-6 C19H17N3O3 335.36
AMG 925 1401033-86-0 C26H29N7O2 471.55
LDC000067 1073485-20-7 C18H18N4O3S 370.43
LEE011 (succinate hydrate) 1374639-79-8 C27H38N8O6X 570.64
LEE011 (succinate) 1374639-75-4 C27H36N8O5 552.63
LEE011 (hydrochloride) 1211443-80-9 C23H31ClN8O 471.0
LEE011 1211441-98-3 C23H30N8O 434.54
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
Wogonin 632-85-9 C16H12O5 284.26
1-NM-PP1 221244-14-0 C20H21N5 331.41
WHI-P180 211555-08-7 C16H15N3O3 297.31
THZ1 1604810-83-4 C31H28ClN7O2 566.05
Senexin A 1366002-50-7 C17H14N4 274.32
CDK4-IN-1 1256963-02-6 C22H29ClN8 440.97
Palbociclib (hydrochloride) 827022-32-2 C24H30ClN7O2 483.99
Purvalanol B 212844-54-7 C20H25ClN6O3 432.9

Recommended Compounds in Same Indication

Name CAS No Formula MW
ADH1 229971-81-7 C22H34N8O6S2 570.69
5-Azacytidine 320-67-2 C8H12N4O5 244.2
Triciribine 35943-35-2 C13H16N6O4 320.3
Dexrazoxane (Hydrochloride) 149003-01-0 C11H17ClN4O4 304.73
Zosuquidar 167354-41-8 C32H31F2N3O2 527.6
Perifosine 157716-52-4 C25H52NO4P 461.66
LY3009120 1454682-72-4 C23H29FN6O 424.51
ADH-1 trifluoroacetate 1135237-88-5 C24H35F3N8O8S2 684.71
SGI-110 929901-49-5 C18H24N9O10P 557.41
Ruxolitinib 941678-49-5 C17H18N6 306.37
AMG 900 945595-80-2 C28H21N7OS 503.58
Ro 5126766 946128-88-7 C21H18FN5O5S 471.46
LY2510924 1088715-84-7 C62H88N14O10 1189.45
VITAMIN K1 12001-79-5 C31H46O2 450.7
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Route of Synthesis

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References

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More Information

BAY-1143572 Racemate

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