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934660-94-3 (Cobimetinib (R-enantiomer))

1

Identification

Cobimetinib (R-enantiomer) Cobimetinib (R-enantiomer)
Name Cobimetinib (R-enantiomer)
Formula C21H21F3IN3O2
MW 531.31
CAS No. 934660-94-3
EINECS
Smiles FC1=C(F)C=CC(C(N2CC([[email protected]]3CCCCN3)(O)C2)=O)=C1NC4=CC=C(I)C=C4F
Synonyms GDC-0973 R-enantiomer;XL-518 R-enantiomer; (R)-(3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)phenyl)(3-hydroxy-3-(piperidin-2-yl)azetidin-1-yl)methanone
InChI InChI=1S/C21H21F3IN3O2/c22-14-6-5-13(19(18(14)24)27-16-7-4-12(25)9-15(16)23)20(29)28-10-21(30,11-28)17-3-1-2-8-26-17/h4-7,9,17,26-27,30H,1-3,8,10-11H2/t17-/m1/s1
2

Introduction

Cobimetinib R-enantiomer (GDC-0973; XL518) is the R-enantiomer of Cobimetinib, which is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase(MEK1/2). IC50 value: Target: MEK1/2 in vitro: The combination of GDC-0973 with the PI3K inhibitor GDC-0941 resulted in combination efficacy in vitro and in vivo via induction of biomarkers associated with apoptosis, including Bcl-2 family proapoptotic regulators [1]. in vivo: The population rate constants associated with tumor growth inhibition for GDC-0973 and GDC-0941 were 0.00102 and 0000651 μM(-1) h(-1), respectively.

Background Information

Cobimetinib (R-enantiomer) is a selective inhibitor of MEK. It is also known as mitogen activated protein kinase kinase (MAPKK) and is a key component of the RAS/RAF/MEK/ERK pathway, which is frequently activated in human tumors. ......by BOC Sciences
Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor. ......by MedChemexpress Co., Ltd.
Cobimetinib R-enantiomer (GDC-0973; XL518) is the R-enantiomer of Cobimetinib (GDC-0973; XL518), which is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase(MEK1/2). ......by ProbeChem
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance: EBNumber:EB000017801

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Cobimetinib (R-enantiomer) Roche Holding AG Stage IV melanoma 2013/1/31 2016/11/30 Phase 3 Clinical
Cobimetinib (R-enantiomer) Genentech Inc Advanced solid tumor 2013/10/1 2016/3/1 Phase 1 Clinical
Cobimetinib (R-enantiomer) Genentech Inc Advanced solid tumor 2012/4/30 2014/8/31 Phase 1 Clinical
Cobimetinib (R-enantiomer) Roche Holding AG Stage IV melanoma 2011/2/28 2014/10/31 Phase 1 Clinical
Cobimetinib (R-enantiomer) Genentech Inc Advanced solid tumor 2009/11/30 2014/3/31 Phase 1 Clinical
Cobimetinib (R-enantiomer) - No Development Reported
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Safety Data of Cobimetinib (R-enantiomer)

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AdooQ BioScience, LLC 5mg/USD165() USA
Apexbio Technology LLC 5mg/USD205(Ship Within 10-14 Days) USA
Ark Pharm, Inc. USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD1200() USA
Carbosynth Limited 1mg/USD88()
MedChemexpress Co., Ltd. 5mg/USD1200() USA
ProbeChem
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD1200() China
10

Related Products

Other Forms of 934660-94-3

Name CAS No Formula MW
Cobimetinib (racemate) 934662-91-6 C21H21F3IN3O2 531.31
Cobimetinib 934660-93-2 C21H21F3IN3O2 531.31

Recommended Compounds in MEK

Name CAS No Formula MW
Isorhamnetin 480-19-3 C16H12O7 316.26
GDC-0623 1168091-68-6 C16H14FIN4O3 456.21
Honokiol 35354-74-6 C18H18O2 266.33
TAK-733 1035555-63-5 C17H15F2IN4O4 504.23
Cobimetinib (racemate) 934662-91-6 C21H21F3IN3O2 531.31
SL327 305350-87-2 C16H12F3N3S 335.35
RO4987655 874101-00-5 C20H19F3IN3O5 565.28
Refametinib 923032-37-5 C19H20F3IN2O5S 572.34
MEK inhibitor 334951-92-7 C26H26N4O2 426.51
Refametinib (R enantiomer) 923032-38-6 C19H20F3IN2O5S 572.34
MEK162 606143-89-9 C17H15BrF2N4O3 441.23
Cobimetinib 934660-93-2 C21H21F3IN3O2 531.31
PD318088 391210-00-7 C16H13BrF3IN2O4 561.09
AZD8330 869357-68-6 C16H17FIN3O4 461.23
BIX02189 1265916-41-3 C27H28N4O2 440.54
BIX02188 334949-59-6 C25H24N4O2 412.48
AS703026 1236699-92-5 C15H15FIN3O3 431.2
U0126 1173097-76-1 C20H22N6OS2 426.56
PD98059 167869-21-8 C16H13NO3 267.28
PD0325901 391210-10-9 C16H14F3IN2O4 482.19

Recommended Compounds in Same Indication

Name CAS No Formula MW
OSI-930 728033-96-3 C22H16F3N3O2S 443.44
AT7867 857531-00-1 C20H20ClN3 337.85
Trametinib 871700-17-3 C26H23FIN5O4 615.39
NVP-BGJ398 872511-34-7 C26H31Cl2N7O3 560.48
BMS-599626 (Hydrochloride) 873837-23-1 C27H28ClFN8O3 567.01
RO4987655 874101-00-5 C20H19F3IN3O5 565.28
MGCD-265 analog 875337-44-3 C26H20FN5O2S2 517.5977
Regorafenib (Hydrochloride) 835621-07-3 C21H16Cl2F4N4O3 519.28
AT9283 896466-04-9 C19H23N7O2 381.43
KX2-391 897016-82-9 C26H29N3O3 431.53
MLN4924 905579-51-3 C21H25N5O4S 443.52
SNX-2112 908112-43-6 C23H27F3N4O3 464.48
IDO5L 914471-09-3 C9H7ClFN5O2 271.6356
ABC294640 915385-81-8 C23H25ClN2O 380.91
OTSSP167 1431697-89-0 C25H28Cl2N4O2 487.42
SB-590885 405554-55-4 C27H27N5O2 453.54
MK-0752 471905-41-6 C21H21ClF2O4S 442.9
ZSTK474 475110-96-4 C19H21F2N7O2 417.41
BMS-599626 714971-09-2 C27H27FN8O3 530.55
PHA-848125 802539-81-7 C25H32N8O 460.57
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Route of Synthesis

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References

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More Information

Cobimetinib (R-enantiomer)

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