Abemaciclib mesylate (LY2835219)
Mechanism of action Current clinical trials Study in vivo References- Product Name
- Abemaciclib mesylate (LY2835219)
- CAS No.
- 1231930-82-7
- Chemical Name
- Abemaciclib mesylate (LY2835219)
- Synonyms
- Bemaciclib;Abemaciclib Mesylate;CS-806;LY2835219;Bemaciclib(salt);LY2835219 mesylate;Bamaciclib Mesylate;LY2835219 USP/EP/BP;LY2835219/LY-2835219;ABEMACICLIB LY2835219 100MG
- CBNumber
- CB02628066
- Molecular Formula
- C28H36F2N8O3S
- Formula Weight
- 602.71
- MOL File
- 1231930-82-7.mol
Abemaciclib mesylate (LY2835219) Property
- storage temp.
- -20°
- solubility
- Soluble in DMSO (up to at least 25 mg/ml) or in Water (up to at least 25 mg/ml).
- form
- solid
- color
- Off-white
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 1 month.
- CAS DataBase Reference
- 1231930-82-7
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P321Specific treatment (see … on this label).
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 17740
- Product name
- LY2835219 (methanesulfonate)
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 17740
- Product name
- LY2835219 (methanesulfonate)
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $63
- Updated
- 2024/03/01
- Product number
- 17740
- Product name
- LY2835219 (methanesulfonate)
- Purity
- ≥95%
- Packaging
- 10mg
- Price
- $93
- Updated
- 2024/03/01
- Product number
- E925710
- Product name
- N-[5-[(4-Ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyrimidinamineMethanesulfonate
- Packaging
- 2.5mg
- Price
- $185
- Updated
- 2021/12/16
- Product number
- CS-1229
- Product name
- Abemaciclib(methanesulfonate)
- Purity
- 99.95%
- Packaging
- 200mg
- Price
- $190
- Updated
- 2021/12/16
Abemaciclib mesylate (LY2835219) Chemical Properties,Usage,Production
Mechanism of action
Many human tumors acquire alterations, which can lead to the activation of cyclin-dependent kinases (CDKs)—CDK4 and CDK6. These alterations include mutations that directly activate CDK4 and CDK6, gene amplifications, which increase expression of various protein activators such as cyclin D, as well as genetic losses, which reduce expression of protein inhibitors such as p16.
Abemaciclib(previously known as LY2835219) specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. 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 the serine/threonine kinases CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation.
Current clinical trials
Abemaciclib(LY2835219) is being investigated in clinical trials in patients with breast cancer, non-small cell lung cancer, and pancreatic cancer, including a combination clinical trial in immuno-oncology.
As of early 2016 Abemaciclib is involved in 3 Phase III clinical trials:
The JUNIPER Study is comparing Abemaciclib against Erlotinib in patients with stage IV Non-small-cell lung carcinoma.
The MONARCH 2 study is investigating the effectiveness of Abemaciclib in combination with Fulvestrant for women with breast cancer. It is due to end in Feb 2017.
The MONARCH 3 study is investigating the effectiveness of Abemaciclib, plus either anastrozole or letrozole, as a first-line treatment for women with breast cancer. The trail is expected to end in June 2017.
Study in vivo
The dose percentage of LY2835219-MsOH treating brain was 0.5-3.9%. LY2835219-MsOH could treat subcutaneous and intracranial glioma models (U87MG), inhibiting tumor growth, and the effect is dose-dependent, whether alone or in combination with mozolomide.
References
http://www.lillyoncologypipeline.com/molecule/cdk-4-and-cdk-6-inhibitor/overview
https://en.wikipedia.org/wiki/Abemaciclib
https://www.cancer.gov/publications/dictionaries/cancer-drug?cdrid=706364
Description
Abemaciclib (1231930-82-7) is a potent and selective CDK4/6 inhibitor (IC50?= 2 nM and 10 nM respectively).1?It caused G1 cell cycle arrest in colo-205 colorectal cells, MDA-MB-361 breast cancer cells, and MV4-11 AML cells. Abemaciclib was also active in several human tumor xenograft models. It displayed efficacy in patients with various solid tumors including breast cancer, non-small cell lung cancer. Glioblastoma, melanoma, colorectal cancer, and hormone receptor-positive breast cancer.2?Abemaciclib induced a T cell inflamed tumor microenvironment and enhanced the efficacy of PD-L1 checkpoint blockade in MCF-7 breast cancer cells.3?FDA approved for the treatment of advanced breast cancers.
Uses
LY2835219 is an orally-bioavailable dual inhibitor of cyclin-dependent kinase 4 (CDK4) and CDK6 (IC50s = 2 and 10 nM, respectively). Through this mechanism, it blocks phosphorylation of retinoblastoma protein, resulting in arrest of cell cycling in the G1 phase. LY2835219 has antitumor action against xenografts when used alone or in combination with other chemotherapeutic compounds.[Cayman Chemical]
Uses
N-[5-[(4-Ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5-fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2-pyrimidinamine is an CDK4/6 protein kinase inhibitor with potential antitumor effects.
Enzyme inhibitor
This oral cell cycle inhibitor (FWfree-base = 506.61 g/mol; FWmesylate-salt = 602.70 g/mol; CAS 1231930-82-7 (mesylate salt)), also known as LY2835219 and N-[5-[(4-ethyl-1-piperazinyl)methyl]-2-pyridinyl]-5- fluoro-4-[4-fluoro-2-methyl-1-(1-methylethyl)-1H-benzimidazol-6-yl]-2- pyrimidinamine, targets the cyclin-dependent kinase CDK4, or cyclin D1 (IC50 = 2 nM) and CDK6, or cyclin D3 (IC50 = 6 nM), inhibiting retinoblastoma (Rb) protein phosphorylation in early G1, thereby arresting the cell cycle in the G1, suppressing DNA synthesis, and inhibiting cancer cell growth. LY2835219 inhibits activation of AKT and ERK, but not mTOR.
References
1) Gelbert?et al.?(2014),?Preclinical characterization of the CDK4/6 inhibitor LY2835219: In-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine; Invest. New Drugs,?32?825 2) Patnail?et al.?(2016),?Efficacy and Safety of Abemaciclib, an Inhibitor of CDK4 and CDK6, for Patients with Breast Cancer, Non-small Cell Lung Cancer, and Other Solid Tumors; Cancer Discov.,?6?740 3) Schaer?et al. (2018),?The CDK4/6 Inhibitor Abemaciclib Induces a T Cell Inflamed Tumor Microenvironment and Enhances the Efficacy of PD-L1 Checkpoint Blockade; Cell Rep.,?22?2978
Abemaciclib mesylate (LY2835219) Preparation Products And Raw materials
Raw materials
Preparation Products
Abemaciclib mesylate (LY2835219) Suppliers
- Tel
- Fax
- 86-21-57758967
- sales@boylechem.com
- Country
- China
- ProdList
- 2922
- Advantage
- 55
- Tel
- 010-82848833 400-666-7788
- Fax
- 86-10-82849933
- jkinfo@jkchemical.com
- Country
- China
- ProdList
- 96815
- Advantage
- 76
- Tel
- +86-21-20908456
- Fax
- 021-58180499
- sales@BioChemBest.com
- Country
- China
- ProdList
- 6005
- Advantage
- 61
- Tel
- 021-54306202 13764082696
- info@hanhongsci.com
- Country
- China
- ProdList
- 42958
- Advantage
- 64
- Tel
- +86 (531) 88811783
- Fax
- +86 (531) 55696010 QQ 1762738062
- sales@trio-pharmatech.com (International market)
- Country
- China
- ProdList
- 1856
- Advantage
- 62
- Tel
- 0411-62910999 13889544652
- meilunui@163.com
- Country
- China
- ProdList
- 4727
- Advantage
- 58
- Tel
- 027-88320699
- Fax
- 027-88320962
- tycshyy@126.com
- Country
- China
- ProdList
- 297
- Advantage
- 66
- Tel
- 021-58170097
- info@topbiochem.com
- Country
- China
- ProdList
- 9458
- Advantage
- 58
- Tel
- 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
- Fax
- +86-27-87599188
- Country
- China
- ProdList
- 1493
- Advantage
- 55
- Tel
- 021-58950125
- Fax
- (86) 21-58955996
- info@chemexpress.com
- Country
- China
- ProdList
- 7552
- Advantage
- 61
- Tel
- 400-400-6206333 18521732826
- Fax
- 021-50323701
- market@aladdin-e.com
- Country
- China
- ProdList
- 25003
- Advantage
- 65
- Tel
- 0551-66399836 18955197623
- sales@enlipharma.com
- Country
- China
- ProdList
- 1874
- Advantage
- 55
- Tel
- 021-021-33632979 15002134094
- Fax
- 021-33632979
- marketing@targetmol.com
- Country
- China
- ProdList
- 7783
- Advantage
- 58
- Tel
- 0531-85828981
- Fax
- +86-531-85806006
- 864598798@qq.com
- Country
- China
- ProdList
- 588
- Advantage
- 58
- Tel
- Mobile:13665161512
- Fax
- +86-510-68873513
- Country
- China
- ProdList
- 1785
- Advantage
- 58
- Tel
- 0523-18601685-898 18652728585
- sales@allyrise.com
- Country
- China
- ProdList
- 2782
- Advantage
- 60
- Tel
- 023-89130144 18523560356
- Fax
- 023-67534737
- zhyong1011@163.com
- Country
- China
- ProdList
- 299
- Advantage
- 58
- Tel
- 18112588827
- sales4@sepharm.com.cn
- Country
- China
- ProdList
- 299
- Advantage
- 60
- Tel
- 0512-87182056 18013166090
- Fax
- 0512-87182056
- lingling.qi@yacoo.com.cn
- Country
- China
- ProdList
- 7295
- Advantage
- 60
- Tel
- 0571-82693216
- Fax
- 0571-82880190
- info@yuhaochemical.com
- Country
- China
- ProdList
- 2028
- Advantage
- 58
- Tel
- 021-61478794
- Fax
- 021-61478794
- sales@hcshhai.com
- Country
- China
- ProdList
- 9793
- Advantage
- 50
- Tel
- 025-58849295 18951903616;
- Fax
- 025-68650336
- info@adooq.cn
- Country
- China
- ProdList
- 2990
- Advantage
- 60
- Tel
- +86-21-5821 5861
- Fax
- +86-21-5106 2861
- sales@letopharm.com
- Country
- China
- ProdList
- 2384
- Advantage
- 58
- Tel
- 021-52996696，15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4566
- Advantage
- 55
- Tel
- 86(21)68097365
- Fax
- 86(21)33321566
- sales@anpharma.net
- Country
- China
- ProdList
- 4891
- Advantage
- 55
- Tel
- 0571-89081561; 10006559855
- Fax
- 0571 89081561
- info@cheminspire.com
- Country
- China
- ProdList
- 412
- Advantage
- 58
- Tel
- 021-57898186
- Fax
- 021-37699262
- Country
- China
- ProdList
- 449
- Advantage
- 55
- Tel
- 18607101326 15172504745
- Fax
- +86-27-84254680
- aileen@chemfaces.com
- Country
- China
- ProdList
- 7057
- Advantage
- 55
- Tel
- Fax
- -
- eric_feng1954@126.com
- Country
- China
- ProdList
- 9248
- Advantage
- 55
- Tel
- 13656237714 13656237714
- Fax
- 0512-65852853
- xiaokunfu@kyyykj.com
- Country
- China
- ProdList
- 295
- Advantage
- 55
- Tel
- 021-58088081 Q3382968513
- Fax
- QQ3382968513
- hailey@shsendpharm.com
- Country
- China
- ProdList
- 3129
- Advantage
- 55
- Tel
- 0576-89085261 15867635987
- Fax
- 0576-89085262
- jasonhu09@163.com
- Country
- China
- ProdList
- 442
- Advantage
- 50
- Tel
- 021-021-58111628 15800915896
- Fax
- QQ 3285589261
- sales@twochem.com
- Country
- China
- ProdList
- 304
- Advantage
- 55
- Tel
- 021-38751876 15000076078
- Fax
- 021-50275764
- Info@rochipharma.com
- Country
- China
- ProdList
- 568
- Advantage
- 55
- Tel
- 027-65388397 18164111589
- Fax
- 027-65388397
- 3321478047@qq.com
- Country
- China
- ProdList
- 1996
- Advantage
- 55
- Tel
- 18620099427
- Fax
- +86-20-62619665
- amy@howeipharm.com
- Country
- China
- ProdList
- 17687
- Advantage
- 55
- Tel
- 021-51619050 13301662590
- Fax
- +86-21-51619052
- mandy@atkchemical.com
- Country
- China
- ProdList
- 10200
- Advantage
- 55
- Tel
- 027-87614241 3310618156
- Fax
- -
- 3310618156@qq.com
- Country
- China
- ProdList
- 62
- Advantage
- 50
- Tel
- 020-61288194 61288195
- Fax
- 020-61288700
- 505721671@qq.com
- Country
- China
- ProdList
- 3866
- Advantage
- 58
- Tel
- 02781293128
- orders@biochemsafebuy.com
- Country
- China
- ProdList
- 9923
- Advantage
- 55
- Tel
- 0317-5296180 15533709196
- Fax
- 0317-5106596
- sale@enkepharma.com
- Country
- China
- ProdList
- 1934
- Advantage
- 55
- Tel
- 400-1166-196 18502815961
- Fax
- QQ：800101999
- cdhxsj@163.com
- Country
- China
- ProdList
- 14603
- Advantage
- 60
- Tel
- 177-54423994 17754423994
- Fax
- QQ:2853530913
- 2853530910@QQ.com
- Country
- China
- ProdList
- 8012
- Advantage
- 62
- Tel
- 18221735425
- sales@xinpingchem.com
- Country
- China
- ProdList
- 9942
- Advantage
- 58
- Tel
- 021-2022843681 15618226720
- Fax
- +86-21-51601218
- lucy@atkchemical.com
- Country
- China
- ProdList
- 9952
- Advantage
- 58
- Tel
- 010-50973130 4009686088
- 3193328036@qq.com
- Country
- China
- ProdList
- 29785
- Advantage
- 68
- Tel
- 18601958187
- Fax
- 18601958187
- 247340078@qq.com
- Country
- China
- ProdList
- 144
- Advantage
- 58
- Tel
- 571-89925085
- Fax
- 0086-571-89925065
- sales@amadischem.com
- Country
- China
- ProdList
- 131957
- Advantage
- 58
- Tel
- +86-13168912896
- Country
- China
- ProdList
- 253
- Advantage
- 58
- Tel
- 0519-83246372 13585352506
- Fax
- 0519-83246372
- Country
- China
- ProdList
- 1844
- Advantage
- 58
View Lastest Price from Abemaciclib mesylate (LY2835219) manufacturers
- Product
- LY2835219 1231930-82-7
- Price
- US $7.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 100KG
- Release date
- 2019-12-30