UNC569 是一种有效的、可逆的、ATP 竞争性和口服活性的 Mer 激酶抑制剂，IC50 为 2.9 nM，Ki 为 4.3 nM。 UNC569 还抑制 Axl 和 Tyro3，IC50 分别为 37 nM 和 48 nM。 UNC569 可用于急性淋巴细胞白血病 (ALL) 和非典型畸胎瘤/横纹肌瘤研究
| Cas No. | 1350547-65-7 |
| 化学名 | 1-[(trans-4-aminocyclohexyl)methyl]-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine |
| Canonical SMILES | CCCCNC1=NC=C2C(N(C[C@H]3CC[C@H](N)CC3)N=C2C4=CC=C(F)C=C4)=N1 |
| 分子式 | C22H29FN6 |
| 分子量 | 396.5 |
| 溶解度 | DMF: 2.5 mg/ml,DMF:PBS (pH 7.2) (1:4): 0.2 mg/ml,DMSO: 0.2 mg/ml,Ethanol: 2 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
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描述 | UNC569 is a potent inhibitor of the TAM family receptor tyrosine kinases Mer, Axl, and Tyro3 (IC50s = 2.9, 37, and 48 nM, respectively). It has antiproliferative activity in vitro against acute lymphoblastic leukemia (ALL) cells (IC50s = 0.5 and 1.2 μM for 697 and Jurkat cell lines, respectively) and inhibits Mer phosphorylation (IC50s = 141 and 193 nM in 697 and Jurkat cell lines, respectively). UNC569 activates Akt and ERK1/2 phosphorylation, induces apoptosis, and sensitizes ALL cells to etoposide and methotrexate . In vivo, UNC569 (4 μM) decreases tumor burden by 47.8% relative to vehicle controls in human MYC transgenic zebrafish. UNC569 (10 mg/kg) delays leukemia onset, reduces CNS infiltration, and prolongs survival of mice implanted with patient-derived Mer-expressing ALL primary cells. |
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