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1211441-98-3 (LEE011)

1

Identification

LEE011 LEE011
Name LEE011
Formula C23H30N8O
MW 434.54
CAS No. 1211441-98-3
EINECS
Smiles O=C(N(C)C)C(N1C2CCCC2)=CC(C1=N3)=CN=C3NC(N=C4)=CC=C4N5CCNCC5
Synonyms LEE 011;LEE-011; 7-cyclopentyl-N,N-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide
InChI InChI=1S/C23H30N8O/c1-29(2)22(32)19-13-16-14-26-23(28-21(16)31(19)17-5-3-4-6-17)27-20-8-7-18(15-25-20)30-11-9-24-10-12-30/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28)
2

Introduction

LEE011 is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity.

Background Information

An orally available, and highly specific CDK4 and 6 inhibitor ......by AOBIOUS INC
LEE011 is an orally available, small-molecule inhibitor of cyclin-dependent kinases (CDK) which targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. CDK4/6 inhibitor LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. LEE011 caused cell-cycle arrest and cellular senescence that was attributed to dose-dependent decreases in phosphorylated RB and FOXM1, respectively. In addition, responsiveness of neuroblastoma xenografts to LEE011 translated to the in vivo setting in that there was a direct correlation of in vitro IC50 values with degree of subcutaneous xenograft growth delay. Treatment with LEE011 significantly reduced proliferation in 12 of 17 human neuroblastoma-derived cell lines by inducing cytostasis at nanomolar concentrations (mean IC50 = 307 ± 68 nmol/L in sensitive lines). LEE011 is currently in Phase I development by Novartis. ......by AbMole BioScience
LEE011 is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
Ribociclib, also known as LEE011, is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. CDK4/6 inhibitor LEE011 specifically inhibits CDK4 and ......by BOC Sciences
Ribociclib is a potent cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. LEE011 has been shown to reduce proliferation in 12 of 17 human neuroblastoma-derived cell lines by inducing cytostasis (mean IC₅₀ = 306 nM in sensitive lines). ......by BioVision, Inc.,
LEE011 is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex. ......by MedChemexpress Co., Ltd.
Ribociclib Free Base, also known as LEE011, is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. CDK4/6 inhibitor LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation. ......by MedKoo Biosciences, Inc.
Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3. ......by Selleck Chemicals LLC
LEE011 is an orally available, and highly specific CDK4/6 inhibitor. Phase 3. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000013233

Storage condition

Storage condition:Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Stock solution storage:0 - 4 C for short term (days to weeks), or -20 C for long term (months). Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. by MedKoo Biosciences, Inc.

Solubility

DMSO by MedChemexpress Co., Ltd.
Soluble in DMSO, not in water by MedKoo Biosciences, Inc.
5

Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
LEE011 Novartis AG Breast tumor 2013/10/31 2014/4/30 Phase 2 Clinical
LEE011 Novartis AG Stage IV melanoma 2013/9/30 2016/10/31 Phase 2 Clinical
LEE011 Novartis AG Metastatic breast cancer 2013/10/31 2016/4/30 Phase 2 Clinical
LEE011 Novartis AG Metastatic breast cancer 2013/9/30 2016/6/30 Phase 2 Clinical
LEE011 Novartis AG Melanoma 2013/4/30 2015/4/30 Phase 2 Clinical
LEE011 - Launched
7

Safety Data of LEE011

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Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC 1mg/USD15() USA
AbMole BioScience 5mg/USD90(In stock) USA
Adipogen Corporation USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC 5mg/USD140(In stock) USA
Ark Pharm, Inc. USA
Axon Medchem BV 5mg/USD114(In Stock) Netherlands
BOC Sciences 200mg/USD228(In stock)
BioVision, Inc., 5mg/USD95() USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD72();10mg/USD96() USA
Cayman Chemical Company 500ug/USD25() USA
ChemieTek 10mg/USD130() USA
LC Laboratoies USA
Lancrix Chemicals. 50mg/USD315() China
MedChemexpress Co., Ltd. 5mg/USD72();10mg/USD96() USA
MedKoo Biosciences, Inc. 5mg/USD80() USA
Pure Chemistry Scientific Inc. 100mg/USD153(In stock) USA
Selleck Chemicals LLC 5mg/USD248(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD72();10mg/USD96() China
Target Molecule Corp. 2mg/USD45();5mg/USD90();10mg/USD165();25mg/USD268();50mg/USD448() USA
10

Related Products

Other Forms of 1211441-98-3

Name CAS No Formula MW
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

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
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
Trametinib 871700-17-3 C26H23FIN5O4 615.39
Ostarine 841205-47-8 C19H14F3N3O3 389.33
Toremifene 89778-26-7 C26H28ClNO 405.96
Toremifene (Citrate) 89778-27-8 C32H36ClNO8 598.08
MLN4924 905579-51-3 C21H25N5O4S 443.52
IDO5L 914471-09-3 C9H7ClFN5O2 271.6356
SB-590885 405554-55-4 C27H27N5O2 453.54
MK-0752 471905-41-6 C21H21ClF2O4S 442.9
Betulinic acid 472-15-1 C30H48O3 456.7
Cyclophosphamide 50-18-0 C7H15Cl2N2O2P 261.09
Fenretinide 65646-68-6 C26H33NO2 391.55
FK866 658084-64-1 C24H29N3O2 391.51
Retaspimycin 857402-23-4 C31H45N3O8 587.7
Retaspimycin (Hydrochloride) 857402-63-2 C31H46ClN3O8 624.17
Motesanib (Diphosphate) 857876-30-3 C22H29N5O9P2 569.44
Litronesib 910634-41-2 C23H37N5O4S2 511.701
Veliparib 912444-00-9 C13H16N4O 244.29
Veliparib (dihydrochloride) 912445-05-7 C13H18Cl2N4O 317.21
Ganetespib 888216-25-9 C20H20N4O3 364.4
Ixabepilone 219989-84-1 C27H42N2O5S 506.7
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Route of Synthesis

12

References

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More Information

LEE011

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