526529
PIM-Kinase Inhibitor X, CX-6258
The PIM-Kinase Inhibitor X, CX-6258 controls the biological activity of PIM-Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
동의어(들):
PIM-Kinase Inhibitor X, CX-6258, ( E)-5-Chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one, HCl
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모든 사진(2)
About This Item
추천 제품
Quality Level
분석
≥99% (HPLC)
양식
powder
제조업체/상표
Calbiochem®
저장 조건
OK to freeze
desiccated (hygroscopic)
protect from light
색상
orange
solubility
DMSO: 25 mg/mL
배송 상태
ambient
저장 온도
2-8°C
SMILES string
O=C(/C1=C/C2=CC=C(C3=CC=CC(C(N4CCCN(C)CC4)=O)=C3)O2)NC5=C1C=C(Cl)C=C5.[xHCl]
일반 설명
An orally bioavailable oxindolo-furanyl compound that acts as a potent, reversible and ATP-competitive inhibitor of pan PIM-kinases (IC50 = 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3, respectively; Ki = 5 nM for PIM-1) with excellent selectivity over 107 kinases (IC80 >500 nM). Shown to arrest the proliferation of several human cancer cells (IC50 = 20 and 452 nM for MV-4-11 and PC3 cells) and block phosphorylation of Bad-Ser112, 4E-BP1-Ser65 and Thr37/46 with an IC50 of ~ 1.0 µM. Displays favorable pharmacokinetic profile and efficacy in mice, and suppresses tumor growth in MV-4-11 and PC3 xenograft murine model (50 mg/kg, p.o.). Further, potentiates doxorubicin (Cat. No. 324380) and paclitaxel (Cat. No. 580555) toxicity in PC3 cells.
생화학적/생리학적 작용
Cell permeable: yes
Primary Target
PIM Kimases
PIM Kimases
Reversible: yes
Secondary Target
Flt3
Flt3
Target IC50: 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3
포장
Packaged under inert gas
경고
Toxicity: Standard Handling (A)
재구성
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
기타 정보
Haddach, M., et al. 2012. ACS Med. Chem. Lett.3, 135.
법적 정보
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
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