HM43239

产品编号 T9428Cas号 2294874-49-8

别名 Tuspetinib

HM43239 是一种具有口服活性和选择性 FLT3抑制剂，IC50值为 1.1 nM (FLT3 野生型)、1.8 nM (FLT3 ITD 突变型) 和 1.0 nM (FLT3 D835Y 突变型)。HM43239 作为可逆的 I 型抑制剂直接抑制 FLT3 的激酶活性，并调节 p-STAT5, p-ERK SYK, JAK1/2 和 TAK1。HM43239 抑制白血病细胞的增殖并诱导其凋亡 (apoptosis)。

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HM43239

产品编号 T9428别名 TuspetinibCas号 2294874-49-8

规格	价格	库存
1 mg	¥ 445	现货
5 mg	¥ 1,080	现货
10 mg	¥ 1,680	现货
25 mg	¥ 3,250	现货
50 mg	¥ 4,650	现货
100 mg	¥ 6,480	现货
1 mL x 10 mM (in DMSO)	¥ 1,370	现货

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产品介绍

生物活性

产品描述	HM43239 is an orally active and selective FLT3 inhibitor with IC 50 s 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 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1/2 and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells [1] [2] [3].
靶点活性	FLT3 (D835Y):1.0 nM, FLT3 (WT):1.1 nM, FLT3 (ITD):1.8 nM
体外活性	HM43239 potently inhibits the growth of acute myeloid leukemia cell lines harboring FLT3 ITD mutation like MV4-11 (IC 50 : 1.3 nM), MOLM-13 (IC 50 : 5.1 nM), and MOLM-14 (IC 50 : 2.9 nM). Besides, HM43239 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].
体内活性	HM43239 exhibits 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].
别名	Tuspetinib

化学信息

分子量	501.07
分子式	C₂₉H₃₃ClN₆
CAS No.	2294874-49-8

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 50 mg/mL (99.79 mM)

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9957 mL	9.9786 mL	19.9573 mL	99.7865 mL
5 mM	0.3991 mL	1.9957 mL	3.9915 mL	19.9573 mL
10 mM	0.1996 mL	0.9979 mL	1.9957 mL	9.9786 mL
20 mM	0.0998 mL	0.4989 mL	0.9979 mL	4.9893 mL
50 mM	0.0399 mL	0.1996 mL	0.3991 mL	1.9957 mL