2. Protein Tyrosine Kinase/RTK
  3. FLT3 FGFR
  4. MAX-40279 hydrochloride

MAX-40279 hydrochloride 是一种口服有效的双重 FLT3 激酶和 FGFR 激酶抑制剂。MAX-40279 hydrochloride 对 FLT3 突变体 (例如 FLT3D835Y) 也有抑制作用，这表明它可以克服对 Quizartinib (HY-13001) 和 Sorafenib (HY-10201) 的耐药性。MAX-40279 hydrochloride 可抑制 NDRG1 蛋白 330 位点的磷酸化，并抑制内皮细胞-间质转化 (EndMT)。MAX-40279 hydrochloride 可用于急性髓系白血病 (AML) 的研究。

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MAX-40279 hydrochloride

MAX-40279 hydrochloride Chemical Structure

CAS No. : 2388506-51-0

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MAX-40279 hydrochloride 的其他形式现货产品:

Customer Review

Other Forms of MAX-40279 hydrochloride:

MAX-40279 hydrochloride 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MAX-40279 hydrochloride is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hydrochloride is also effective against the FLT3 mutants such as FLT3D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 hydrochloride inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hydrochloride can be used for the research of acute myelogenous leukemia (AML)[1][2][3].

IC50 & Target

FLT3 and FGFR[1]
体外研究
(In Vitro)

MAX-40279 (0.5-1 μM, 48 h) hydrochloride 通过抑制 HUVECs、MAECs 和 MPLECs 中 Ser-330 位点的 NDRG1 磷酸化来阻碍内皮细胞-间质转化[3]。

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

MAX-40279 hydrochloride 相关抗体:

Cell Migration Assay [3]

Cell Line: HUVECs
Concentration: 0.5 and 1 μM
Incubation Time: 48 h
Result: Attenuated migration of HUVEC induced by H2O2 and TGF-β.

Western Blot Analysis[3]

Cell Line: HUVECs, MAECs, and MPLECs
Concentration: 0.5 and 1 μM
Incubation Time: 48 h
Result: Significantly inhibited the phosphorylation of NDRG1 at Ser-330.
Reduced the total protein level of NDRG1.
Inhibited the expression of mesenchymal markers such as ZEB1, α-SMA, Slug, Snail, and TAGLN.
体内研究
(In Vivo)

MAX-40279 (12 mg/kg，口服，每日一次，连用 7 天) hydrochloride 在小鼠 Mini-PDX 试验中对 43% 的患者肿瘤样本有效[1]。
MAX-40279 (12 mg/kg，口服，每日两次，连用 21-28 天) hydrochloride 显著抑制 MV4-11 和 KG-1 细胞诱导的小鼠异种移植模型中的肿瘤生长[1]。
MAX-40279 (7-15 mg/kg，口服，每日两次，连用 2-3 周) hydrochloride 显著增强小鼠乳腺癌模型中的抗 PD-1 效果[1]。
MAX-40279 (口服，单剂量) hydrochloride 在 SD 大鼠骨髓中的药物浓度远高于血浆中的药物浓度[2]。

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

Animal Model: Micro patient-derived xenotransplantation model established in 5-week-old nu/nu mice[1]
Dosage: 12 mg/kg
Administration: Oral administration (p.o.), once daily for 7 days
Result: Reduced the vitality of tumor cells.
The growth rates of tumour volume and weight were smaller but that the combined inhibition was more remarkable.
Animal Model: MV4-11 and KG-1 cells induced xenograft model established in immunodeficient mice[1]
Dosage: 12 mg/kg
Administration: Oral administration (p.o.), once daily for 21-28 days
Result: Significantly inhibited tumor growth, with no significant weight loss or toxicity observed.
Animal Model: 4T1 induced breast cancer model combination with anti-PD-1 established in mice[1]
Dosage: 7, 10 and 15 mg/kg
Administration: Oral administration (p.o.), once daily for 2-3 weeks
Result: Significantly enhanced the efficacy of anti-PD-1 effect, and the combined treatment with anti-PD-1 antibodies yielded the best results.
Clinical Trial
分子量

474.98

Formula

C22H24ClFN6OS
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MAX-40279 hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MAX-402792388506-51-0MAX40279MAX 40279FLT3FGFRCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Fibroblast growth factor receptordualacute myelogenous leukemiaInhibitorinhibitorinhibit

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