PF-562271 HCl是PF-562271的盐酸盐形式，是一种强效的ATP竞争性的可逆的抑制剂，作用于FAK其IC50为1.5 nM。相比较FAK，对Pyk2的效果少了大约十倍，除了CDKs类的蛋白酶，PF-562271 HCl的选择性相比其他蛋白酶大大约100倍。 Information PF-562271 HCl is the hydrochloride salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor ofFAKwithIC50of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs. Phase 1. Targets FAK ; PYK2 ; CDK2/CyclinE ; CDK3/CyclinE ; CDK1/CyclinB 15161,1.5 nM; 13 nM; 30 nM; 47 nM; 58 nM In vitro PF-562271 binds in the ATP-binding cleft of FAK, forming two of the three “canonical” H-bonds between the inhibitor and main-chain atoms in the kinase hinge region. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with IC50 of 5 nM. PF-562271 (3.3 μM) results in G1 arrest of PC3-M cells. PF-562271 (1 nM) blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays. PF-262271 potently blocks blood vessel sprouting without detectable changes in vascular leakage. PF-562271 (250 nM) results in complete inhibition of collective A431 cell invasion into collagen gels. In vivo PF-562271 (
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PF-562271 HCl
Dangerous GoodsCAS number：939791-41-0 molecular formula：C21H21ClF3N7O3S
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | N-Methyl-N-{3-[({2-[(2-oxo-2,3-dihydro-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl}amino)methyl]-2-pyridinyl}methanesulfonamide hydrochloride (1:1) | ||
| CAS number | 939791-41-0 | molecular formula | C21H21ClF3N7O3S |
| molecular weight | 543.95 g/mol | Exact mass | 10mM in DMSO |
| PSA | 138.000 Ų | logp | 2.873 |
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P501: 将内容物/容器处理到。。。 P312: 打电话给毒物中心或医生。。。如果你觉得不舒服 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P362: 脱下污染的衣服并洗净后再使用。 P270:
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MSDS
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