| Company Name: |
Shanghai Weijiahe Biotechnology Co., Ltd Gold
|
| Tel: |
17502176150; 17502176150 |
| Email: |
861873257@qq.com |
| Products Intro: |
Product Name:MK-1084
CAS:2641216-67-1
Purity:98% HPLC Package:1g；5g；10g；20g
|
| Company Name: |
Taizhou Zhongzhi Biotechnology Co., Ltd Gold
|
| Tel: |
zhongzhipharma@126.c 15066129350 |
| Email: |
zhongzhipharma@126.com |
| Products Intro: |
Product Name:MK-1084
CAS:2641216-67-1
Purity:HPLC99% Package:100g;1kg;10kg;100kg
|
| Company Name: |
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
|
| Tel: |
17702719238 |
| Email: |
sales@sun-shinechem.com |
| Products Intro: |
Product Name:Calderasib ; MK-1084 ; MK1084 ; MK 1084
CAS:2641216-67-1
Purity:98% HPLC Package:5mg; 10mg;20mg;50mg;100mg
|
| Company Name: |
TaiChem Taizhou Limited
|
| Tel: |
052386810091 |
| Email: |
zcwy9518@yeah.net |
| Products Intro: |
Product Name:MK-1084
CAS:2641216-67-1
Package:5g;10g;100g
|
|
| | MK-1084 Basic information |
| Product Name: | MK-1084 | | Synonyms: | MK-1084;1,18-Etheno-4H-pyrido[4,3-e]pyrimido[1,6-g][1,4,7,9]benzodioxadiazacyclododecin-4-one, 20-chloro-2-[(2S,5R)-2,5-dimethyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-14,17-difluoro-11,12-dihydro-6-(1-methylethyl)-, (5S,17aR)-;(5S,17aR)-20-Chloro-2-[(2S,5R)-2,5-dimethyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-14,17-difluoro-11,12-dihydro-6-(1-methylethyl)-1,18-etheno-4H-pyrido[4,3-e]pyrimido[1,6-g][1,4,7,9]benzodioxadiazacyclododecin-4-one;Calderasib (MK-1084);Calderasib | | CAS: | 2641216-67-1 | | MF: | C32H31ClF2N6O4 | | MW: | 637.08 | | EINECS: | | | Product Categories: | | | Mol File: | 2641216-67-1.mol |  |
| | MK-1084 Chemical Properties |
| Boiling point | 788.913±70.00 °C(Press: 760.00 Torr)(predicted) | | density | 1.447±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | pka | 5.345±0.40(predicted) | | form | Solid | | color | White to off-white |
| | MK-1084 Usage And Synthesis |
| Uses | MK-1084 is a selective KRAS G12C inhibitor that is currently in Phase I clinical trial (NCT05067283). MK-1084 exhibits anticancer activity and can be used either alone or in combination with pembrolizumab (HY-P9902) for cancer research[1]. | | in vivo | MK-1084 (10-30 mg/kg, po for 14 days) exhibits antitumor efficacy in mouse MiaPaCa-2 xenograft models[2].
MK-1084 exhibits a good pharmacokinetic characteristics with a plasma clearance of 22 mL/min/kg, a mean residence time MRT of 1.1 h and an oral bioavailability of 61%[2]. | Animal Model: | Mouse MiaPaCa-2 xenograft models[2] | | Dosage: | 10-30 mg/kg | | Administration: | po for 14 days | | Result: | Inhibited tumor growth. |
| | References | [1] Rojas C, et al. 663P Safety and preliminary efficacy of the KRAS G12C inhibitor MK-1084 in solid tumors and in combination with pembrolizumab in NSCLC[J]. Annals of Oncology, 2023, 34: S466-S467.
[2] Ma X, et al., Discovery of MK-1084: An Orally Bioavailable and Low-Dose KRASG12C Inhibitor. J Med Chem. 2024 Jul 11;67(13):11024-11052. DOI:10.1021/acs.jmedchem.4c00572 |
| | MK-1084 Preparation Products And Raw materials |
|