2. Protein Tyrosine Kinase/RTK
  3. FLT3
  4. TTT 3002

TTT 3002 是一种口服有效的 FLT3 抑制剂。TTT 3002 通过激活残基 D835 的突变来有效抑制 FLT3 磷酸化，其 IC50 为 0.2 nM。TTT 3002 可用于急性髓系白血病 (AML) 的研究。

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TTT 3002 Chemical Structure

TTT 3002 Chemical Structure

CAS No. : 871037-95-5

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TTT 3002 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TTT 3002 is a potent and orally active FLT3 inhibitor. TTT 3002 potently inhibits FLT3 phosphorylation by activating mutations at residue D835, with an IC50 of 0.2 nM. TTT 3002 can be used for AML (acute myeloid leukemia) research[1].

体外研究
(In Vitro)

TTT 3002 下调 Molm14 和 MV4-11 细胞中的 FLT3 磷酸化(pFLT3)[1]。
TTT 3002 诱导细胞周期停滞，随后显著诱导凋亡[1]。

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

TTT 3002 相关抗体:

Western Blot Analysis[1]

Cell Line: Molm14 and MV4-11 cells
Concentration: 0, 0.25, 0.5, 1, 2 nM
Incubation Time: 1 h
Result: Downregulated FLT3 phosphorylation (pFLT3) in Molm14 and MV4-11 cells in a dose-dependent manner. The IC50 for FLT3 phosphorylation in both cell lines was six- to seven fold lower for TTT 3002 compared with Quizartinib (HY-13001) at 0.2 vs 1.3 nM, respectively.

Cell Cycle Analysis[1]

Cell Line: Molm14 and MV4-11 cells
Concentration: 0, 1, 2, 5, 10 nM
Incubation Time: 24 h
Result: Showed cell cycle arrest followed by marked induction of apoptosis, along with concurrent activation of caspase 3 and poly ADP ribose polymerase cleavage.
体内研究
(In Vivo)

TTT 3002 (6 mg/kg，口服灌胃，每天两次，持续 2 至 4 周) 在体内对几种 FLT3/ITD 相关 AML 小鼠肿瘤模型有效，且毒性极小[1]。
TTT 3002 (6 mg/kg，口服灌胃，单次) 可被迅速吸收，具有双相最大血清浓度 (Cmax) 随后是单指数衰减[1]。

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

Animal Model: BALB/C mice (female, age 6 to 8 weeks, received Ba/F3-ITD Luc+ cells by tail vein injection on day 0)[1]
Dosage: 6 mg/kg
Administration: Oral gavage, twice per day, for 2 to 4 weeks
Result: Showed no significant changes in animal weight and was sufficient to eliminate the presence of Ba/F3-ITD Luc+ cells by day 17 (10 days of treatment).
Animal Model: Leukemic engrafted mice (female, age 6 to 8 weeks)[1]
Dosage: 6 mg/kg
Administration: Oral gavage, single (Pharmacokinetic Analysis)
Result: After oral administration, TTT 3002 was rapidly absorbed with a biphasic maximum serum concentration (Cmax) followed by a monoexponential decay. The Cmax and area under the concentration-time curve from time 0 to infinity (AUC0→∞) were 613 nM and 3127 nM⋅h, respectively. The half-life, apparent volume of distribution, and apparent clearance were 3.6 hours, 21 L/kg, and 4.1 L/h per kilogram, respectively.
分子量

465.50

Formula

C27H23N5O3
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

TTT 3002 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

TTT 3002871037-95-5TTT3002TTT-3002FLT3Cluster of differentiation antigen 135CD135Fms like tyrosine kinase 3internal tandem duplicationITDMolm14MV4-11 cellsFLT3/ITDFLT3/PMand FLT3/WT cellInhibitorinhibitorinhibit

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目录号：
HY-111249
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