CHMFL-FLT3-122_product_DataBase

Bioactivity	CHMFL-FLT3-122 is a potent, selective and orally active FLT3 kinase with an IC50 of 40 nM. CHMFL-FLT3-122 shows selectivity for FLT3 over BTK (IC50 of 421 nM) and c-KIT (IC50 of 559 nM) kinases. CHMFL-FLT3-122 induces apoptosis by arresting the cell cycle into the G0/G1 phase[1].
Target	IC50: 40 nM (FLT3 kinase), 421 nM (BTK), 559 nM (c-KIT)
Invitro	CHMFL-FLT3-122（化合物18）显着抑制FLT3-ITD阳性急性髓性白血病（AML）癌细胞系MV4-11（GI50 = 22 nM）、MOLM13/14（GI50 = 21 nM/42 nM）的增殖[1]。 CHMFL-FLT3-122（0.03-1 μM；24 小时）可以阻止这些细胞系的细胞周期进展至 G0/G1 期并诱导细胞凋亡[1]。CHMFL-FLT3-122 (0.03-1 μM; 24 h) 显着抑制 FLT3 Tyr589/591 位点的自磷酸化，并抑制 Stat5 ERK、AKT 的磷酸化和 cMYC[1] . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> CHMFL-FLT3-122 相关抗体: Cell Cycle Analysis[1] Cell Line:
In Vivo	CHMFL-FLT3-122（12.5-50 mg/kg；口服灌胃；每天一次；持续 22 天）几乎可以完全抑制肿瘤进展，并且不显着影响小鼠体重[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
CAS	1839150-56-9
Formula	C26H29N7O2
Molar Mass	471.55
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Xixiang Li, et al. Discovery of (R)-1-(3-(4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)-2-(dimethylamino)ethanone (CHMFL-FLT3-122) as a Potent and Orally Available FLT3 Kinase Inhibitor for FLT3-ITD Positive Acute Myeloid Leukemia. J Med Chem. 2015 Dec 24;58(24):9625-38.

PeptideDB

CHMFL-FLT3-122

CAS: 1839150-56-9 F: C26H29N7O2 W: 471.55