HM43239 is an orally active and selectiveFLT3inhibitor withIC₅₀s of 1.1 nM, 1.8 nM and 1.0 nM forFLT3WT,FLT3internal tandem duplication (ITD) andFLT3D835Y kinases, respectively. HM43239 inhibits the kinase activity ofFLT3as a reversible type I inhibitor and modulates p-STAT5, p-ERK,SYK, JAK1/2, and TAK1. HM43239 inhibits the proliferation and induces theapoptosisof leukemic cells^[1][2][3].

HM43239 potently inhibits the growth of acute myeloid leukemia cell lines harboring FLT3 ITD mutation, such as MV4-11 (IC₅₀: 1.3 nM), MOLM-13 (IC₅₀: 5.1 nM), and MOLM-14 (IC₅₀: 2.9 nM). HM43239 also inhibits KG1a cells (CD34+/CD38- cells) proliferation^[1].
HM43239 induces the caspase 3/7-dependent apoptosis of leukemic stem cell (LSC) marker-expressing KG1a cells (CD34+/CD38- cells)^[1].
HM43239 potently inhibits phosphorylation of SYK, STAT3, and STAT5 in KG1a cells^[3].

HM43239 shows the excellent dose proportional antitumor activity in mouse models xenografted with both MV4-11 and MOLM-13 cell lines without any significant toxicity^[1].
HM43239 prolongs survival in FLT3 ITD/TKD double mutated xenograft mouse models^[3].

501.07

Solid

C₂₉H₃₃ClN₆

2294874-49-8

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

DMSO : 125 mg/mL(249.47 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (4.15 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。