1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. FLT3
    Apoptosis
  3. HM43239

HM43239 

Cat. No.: HY-145015 Purity: 99.77%
Handling Instructions

HM43239 is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells.

For research use only. We do not sell to patients.

HM43239 Chemical Structure

HM43239 Chemical Structure

CAS No. : 2294874-49-8

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5 mg USD 480 In-stock
Estimated Time of Arrival: December 31
10 mg USD 800 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2400 In-stock
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100 mg USD 3600 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

HM43239 is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells[1][2].

IC50 & Target[1]

FLT3 WT

1.1 nM (IC50)

FLT3 ITD

1.8 nM (IC50)

FLT3 D835Y

1.0 nM (IC50)

In Vitro

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 KG1a cells (CD34+/CD38- cells)[1].
HM43239 potently inhibits phosphorylation of SYK, STAT3, and STAT5[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

501.07

Formula

C₂₉H₃₃ClN₆

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9957 mL 9.9786 mL 19.9573 mL
5 mM 0.3991 mL 1.9957 mL 3.9915 mL
10 mM 0.1996 mL 0.9979 mL 1.9957 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Product Name:
HM43239
Cat. No.:
HY-145015
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