HM43239 free base · Synonyms: Tuspetinib | 2569527-64-4

HM43239 is a Novel Potent Small Molecule FLT3 Inhibitor.

For research use only. Not for human or veterinary use.

Target FLT3 Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Data Sheet COA

HM43239 structure

CAS No.: 2294874-49-8

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 520.00	BP-01999-100mg	In stock	Get quote
250 mg	USD 832.00	BP-01999-250mg	In stock	Get quote
500 mg	USD 1,206.00	BP-01999-500mg	In stock	Get quote
1 g	USD 1,750.00	BP-01999-1g	In stock	Get quote
5 g	Inquire	BP-01999-5g	Inquire	Inquire

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Description

HM43239 is a Novel Potent Small Molecule FLT3 Inhibitor, in Acute Myeloid Leukemia (AML) with FMS-like Tyrosine Kinase 3 (FLT3) Mutations

Biological activity

In Vitro Tuspetinib 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). Tuspetinib also inhibits KG1a cells (CD34+/CD38- cells) proliferation. Tuspetinib induces the caspase 3/7-dependent apoptosis of leukemic stem cell (LSC) marker-expressing KG1a cells (CD34+/CD38- cells). Tuspetinib potently inhibits phosphorylation of SYK, STAT3, and STAT5 in KG1a cells. In Vivo Tuspetinib shows the excellent dose proportional antitumor activity in mouse models xenografted with both MV4-11 and MOLM-13 cell lines without any significant toxicity. Tuspetinib prolongs survival in FLT3 ITD/TKD double mutated xenograft mouse models.

Identifiers

SMILES: C[C@H]1CN(CC2=CC(=CC(NC3=NC=C(Cl)C(=N3)C3=CNC4=C3C=CC(C)=C4)=C2)C2CC2)C[C@@H](C)N1
InChIKey: FZLSDZZNPXXBBB-KDURUIRLSA-N

Specifications

MW (average): 501.0660
Formula: C₂₉H₃₃ClN₆
CAS No.: 2294874-49-8
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4°C, protect from light; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO 125 mg/mL

Documents

References

[1]. Miyoung Lee, et.al. Abstract 804: Antitumor activity of the potent and novel FLT3 inhibitor HM43239 in acute myeloid leukemia. Cancer Res July 1 2018 (78) (13 Supplement) 804.

[2]. Naval G. Daver, et.al. HM43239, a Novel Potent Small Molecule FLT3 Inhibitor, in Acute Myeloid Leukemia (AML) with FMS-like Tyrosine Kinase 3 (FLT3) Mutations: Phase 1 /2 Study. Blood 2019; 134 (Supplement_1): 1331.

[3]. JiSook Kim, et.al. Abstract 1293: HM43239, a novel FLT3 inhibitor in overcoming resistance for acute myeloid leukemia. Cancer Res July 1 2019 (79) (13 Supplement) 1293.

Same target

Search FLT3

Same research area

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