| CHMFL-ABL-053BCR-ABL inhibitor |

Sample solution is provided at 25 µL, 10mM.
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Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure


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| Cas No. | 1808287-83-3 | SDF | Download SDF |
| Chemical Name | 2-((3-amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide | ||
| Canonical SMILES | CC1=CC=C(NC2=NC(NC)=C(C(NC3=CC(NC(C4=CC=CC(C(F)(F)F)=C4)=O)=CC=C3C)=O)C=N2)C=C1N | ||
| Formula | C28H26F3N7O2 | M.Wt | 549.55 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
CHMFL-ABL-053 (compound 18a) is a BCR-ABL inhibitor with ABL1: IC50 of 70 nM. CHMFL-ABL-053 is derived from a dihydropyrimidopyrimidine core scaffold based compound 27 (GNF 7). [1]
CHMFL-ABL-053 inhibited the proliferation of CML cell lines K562 (GI50 = 14 nM), KU812 (GI50 = 25 nM) and MEG 01 (GI50 = 16 nM), through significant suppression of the BCR-ABL auto phosphorylation (EC50 = 100 nM) and downstream mediators such as STAT5, Crkl and ERK’s phosphorylation. In the TEL fused isogenic BaF3 cells, CHMFL-ABL-053 exhibited strong binding ability against BLK, DDR1, DDR2, EPHA8, EphB6, HCK, LCK, p38α and SRC kinases. CHMFL-ABL-053 exhibited an IC50 of 70 nM against ABL1 kinase, inhibited p38α (IC50: 62 nM) and SRC kinase (IC50: 90 nM) by Invitrogen Select Screen biochemical assay. CHMFL-ABL-053 showed less potent to DDR1 (IC50: 292 nM) and DDR2 (IC50: 457 nM). CHMFL-ABL-053 did not exhibit apparent potency against c-KIT kinase (IC50: over 10000 nM). [1]
Pharmacokinetic study showed that CHMFL-ABL-053 had over 4 hours half-life and 24% bioavailability in rats. 50mg/kg/day dosage treatment could almost completely suppress the tumor progression in the K562 cells inoculated xenograft mouse model. As a potential useful drug candidate for CML, 18a is under extensive preclinical safety evaluation now. [1]
Reference:
1.Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl) benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia.J Med Chem. 2016 Feb 5. [Epub ahead of print]
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IgM是免疫球蛋白M(Immunoglobulin M,IgM)的缩写。根据结构的不同将免疫球蛋白分为五种,IgM是人的免疫球蛋白之一,其他还有lgA、lgG、IgD和lgE。
HSV1型导致的一般都是腰部以上的感染,典型症状是水泡有可能引起脑炎,而且有非活化状态的潜伏。所以我觉得你根本就不用担心这个抗体IgG阳性的化验单。
2-IgM也是一种特异性感染指标,但在人体内持续时间不长(有时是30天更短),往往是传染病的近期感染指标。呈阴性是指:你近期没有感染过结核杆菌。
文章原文链接http://www.jbc.org/content/282/23/16776.long

