• Search chemicals, activators, Inhibitors, APIs, intermediates and raw materials.

1619903-54-6 (LY2857785)

1

Identification

LY2857785 LY2857785
Name LY2857785
Formula C26H36N6O
MW 448.6
CAS No. 1619903-54-6
EINECS
Smiles CC(C1=C2C=C(C3=NC(N[[email protected]]4CC[[email protected]](NC5CCOCC5)CC4)=NC=C3)C=CC2=NN1C)C
Synonyms LY 2857785;LY-2857785; (1r,4r)-N1-(4-(3-isopropyl-2-methyl-2H-indazol-5-yl)pyrimidin-2-yl)-N4-(tetrahydro-2H-pyran-4-yl)cyclohexane-1,4-diamine
InChI InChI=1S/C26H36N6O/c1-17(2)25-22-16-18(4-9-24(22)31-32(25)3)23-10-13-27-26(30-23)29-20-7-5-19(6-8-20)28-21-11-14-33-15-12-21/h4,9-10,13,16-17,19-21,28H,5-8,11-12,14-15H2,1-3H3,(H,27,29,30)/t19-,20-
2

Introduction

LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC50 11 nM) and other transcription kinases CDK8 (IC50 16 nM), and CDK7 (IC50 246 nM).

Background Information

LY2857785 is a potent and selective CDK9 inhibitor; significantly reduces RNAP II CTD phosphorylation and dramatically decreases MCL1 protein levels to result in apoptosis in a variety of leukemia and solid tumor cell lines. ......by AdooQ BioScience, LLC
LY2857785 is a potent and selective CDK9 inhibitor; significantly reduces RNAP II CTD phosphorylation and dramatically decreases MCL1 protein levels to result in apoptosis in a variety of leukemia and solid tumor cell lines. ......by BOC Sciences
LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC50 11 nM) and other transcription kinases CDK8 (IC50 16 nM), and CDK7 (IC50 246 nM). ......by MedChemexpress Co., Ltd.
LY2857785 is a potent CDK9 inhibitor with potential anticancer activity. LY2857785 significantly reduces RNAP II CTD phosphorylation and dramatically decreases MCL1 protein levels to result in apoptosis in a variety of leukemia and solid tumor cell lines. LY2857785 inhibits the growth of a broad panel of cancer cell lines, and is particularly efficacious in leukemia cells, including orthotopic leukemia preclinical models as well as in ex vivo acute myeloid leukemia and chronic lymphocytic leukemia patient tumor samples. The inhibition of CDK9 may represent a promising approach as a cancer therapeutic target, especially in hematologic malignancies. ......by MedKoo Biosciences, Inc.
LY2857785 is a potenrt, reversible and ATP-competitive CDK9 inhibitor with IC50 of 11 nM, also inhibits CDK8 (IC50=16 nM) and weakly inhibits CSK7 (IC50=246 nM); showes good selectivity against a panel of 114 protein kinases; inhibits RNAP II C-terminal domain (CTD) P-Ser2 and CTD P-Ser5 in U2OS cells with IC50 of 89 and 42 nM, dramatically decreases MCL1 protein levels to result in apoptosis in a variety of leukemia and solid tumor cell lines (MV-4-11 cell IC50=40 nM); inhibits RNAP II CTD P-Ser2 in vivo, demonstrates potent antitumor growth efficacy in tumor xenografts. ......by ProbeChem
LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9(IC50=0.011 μM) and also inhibits other transcription kinases CDK8(IC50=0.016 μM) and CDK7 (IC50=0.246 μM). ......by Selleck Chemicals LLC
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000010008

Storage condition

4°C by MedChemexpress Co., Ltd.

Solubility

10 mM in DMSO by CHEMSCENE, LLC
10 mM in DMSO by MedChemexpress Co., Ltd.
5

Mechanism and Indication

Signaling Pathways Cell Cycle/DNA Damage
Target CDK
Research Area Cancer
Indications
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
LY2857785 - Not Found
LY2857785 - No Development Reported
7

Safety Data of LY2857785

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AdooQ BioScience, LLC USA
Apexbio Technology LLC 5mg/USD350(Ship Within 10-14 Days) USA
Ark Pharm, Inc. USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 2mg/USD132();5mg/USD420() USA
MedChemexpress Co., Ltd. 2mg/USD132();5mg/USD264() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 2mg/USD132();5mg/USD264() China
Shanghai XingMo Biotechnology Co., Ltd. 1g/USD950(In stock) CHINA
10

Related Products

Other Forms of 1619903-54-6

Name CAS No Formula MW

Recommended Compounds in CDK

Name CAS No Formula MW
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
NU6102 444722-95-6 C18H22N6O3S 402.47

Recommended Compounds in Same Indication

Name CAS No Formula MW
11

Route of Synthesis

12

References

13

More Information

LY2857785

Tags: buy 1619903-54-6 IC50 | 1619903-54-6 price | 1619903-54-6 cost | 1619903-54-6 solubility | 1619903-54-6 purchase | 1619903-54-6 manufacturer | 1619903-54-6 research buy | 1619903-54-6 order | 1619903-54-6 MSDS | 1619903-54-6 chemical structure | 1619903-54-6 Storage condition | 1619903-54-6 molecular weight | 1619903-54-6 mw | 1619903-54-6 datasheet | 1619903-54-6 supplier | 1619903-54-6 cell line | 1619903-54-6 NMR | 1619903-54-6 MS | 1619903-54-6 IR | 1619903-54-6 solubility | 1619903-54-6 Safe information | 1619903-54-6 Qc and Spectral Information | 1619903-54-6 Clinical Information | 1619903-54-6 Clinical Trial | 1619903-54-6 Route of Synthesis | 1619903-54-6 storage condition | 1619903-54-6 diseases and conditions | 1619903-54-6 flash point | 1619903-54-6 boiling point | 1619903-54-6 melting point | 1619903-54-6 storage condition | 1619903-54-6 brand