2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt MAPK/ERK Pathway PI3K/Akt/mTOR JAK/STAT Signaling Apoptosis
  3. FLT3 ERK Akt STAT Apoptosis
  4. UNC1666

UNC1666 是一种具有 ATP 竞争性的双靶点 Mer/Flt3 酪氨酸激酶抑制剂，IC50 分别为 0.55 nM、0.69 nM，Ki 分别为 0.16 nM、0.67 nM。UNC1666 可抑制 Mer 和 Flt3 的激酶活性，降低 Mer 和 Flt3 的磷酸化水平，抑制下游促存活信号通路 (Erk1/2、Akt 及 Stat)，诱导细胞凋亡 (apoptosis)，并减少急性髓系白血病细胞的集落形成。UNC1666 可用于急性髓系白血病的相关研究[1][2]。

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UNC1666

UNC1666 Chemical Structure

CAS No. : 1429882-12-1

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UNC1666 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

UNC1666 is an ATP-competitive dual-target Mer/Flt3 tyrosine kinase inhibitor with IC50 values of 0.55 nM and 0.69 nM, and Ki values of 0.16 nM and 0.67 nM, respectively. UNC1666 inhibits the kinase activities of Mer and Flt3, reduces their phosphorylation levels, suppresses downstream pro-survival signaling pathways (Erk1/2, Akt and Stat), induces cell apoptosis, and decreases colony formation of acute myeloid leukemia cells. UNC1666 is applicable to research related to acute myeloid leukemia[1][2].

体外研究
(In Vitro)

UNC1666 (Analogue 2) 对 Mer、Flt3、Axl (29 nM) 和 Tyro3 (37 nM) 激酶表现出亚纳摩尔至低纳摩尔水平的体外抑制活性，其中对 Flt3 (0.69 nM) 和 Mer (0.93 nM) 的活性最强[1]。
UNC1666 (10-300 nM) 可浓度依赖性地抑制 Kasumi-1 AML 细胞中 Mer 的磷酸化，在 MV4;11 Flt3-ITD AML 细胞中强效抑制 Flt3 磷酸化[2]。
UNC1666 (50-300 nM) 可呈剂量依赖性抑制 Mer 阳性 Kasumi-1 细胞和 Flt3-ITD MV4;11 AML 细胞经 2 小时处理后的下游促存活信号通路 (Erk1/2、Akt 及 Stat)，且在 Flt3-ITD 细胞中的活性更强[2]。
UNC1666 (10-300 nM; 72 h) 可在处理 72 小时后以剂量依赖方式诱导 Mer 阳性和 Flt3-ITD AML 细胞系发生细胞凋亡[2]。
UNC1666 (50-300 nM; 72 h) 可在处理结束后仍抑制 Kasumi-1 和 MV4;11 急性髓系白血病 (AML) 细胞的长期反弹生长[2]。
UNC1666 (10-300 nM; 72 h)可显著降低软琼脂培养的 Mer 阳性和 Flt3-ITD AML 细胞系的集落形成能力[2]。
UNC1666 (50-300 nM; 2 h) 可剂量依赖性地抑制共表达 Mer 和 Flt3ITD 的原发性 AML 原始细胞中 Mer 与 Flt3 的磷酸化，抑制细胞中下游促存活信号通路 (Erk1/2、Akt、Stat5)，诱导细胞凋亡，降低集落形成能力[2]。

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

UNC1666 相关抗体:

Apoptosis Analysis[2]

Cell Line: Mer-positive (Kasumi-1, NOMO-1) and Flt3-ITD (MV4;11, MOLM-13) AML cell lines
Concentration: 10, 25, 50, 100, 300nM
Incubation Time: 72 h
Result: Induced apoptosis in 50-67% of Mer-positive cells at 100 nM, and 68-76% of Mer-positive cells at 300 nM, with Kasumi-1 cells showing 76% apoptotic/dead cells at 300 nM.
Induced apoptosis in 54-67% of Flt3-ITD cells at 50 nM, and 90-98% of Flt3-ITD cells at 300 nM, with MV4;11 cells showing 90% apoptotic/dead cells at 300 nM and MOLM-13 cells showing 98% apoptotic/dead cells at 300 nM.
Confirmed increased cleavage of PARP and Caspase-3 in a dose-dependent manner via immunoblot.

Cell Proliferation Assay[2]

Cell Line: Mer-positive (Kasumi-1) and Flt3-ITD (MV4;11) AML cell lines
Concentration: 50, 100, 300nM
Incubation Time: 72 h (initial treatment)
Result: Resulted in only a 2.5-fold increase in viable cell number over 6 days in Kasumi-1 cells at 100 nM, compared to a 14-fold increase with vehicle.
Resulted in only a 13-fold increase in viable cell number over 6 days in MV4;11 cells at 50 nM, compared to a 67-fold increase with vehicle.
Caused more striking proliferation defects at higher concentrations, with minimal viable cells at Day 6.

Cell Proliferation Assay[2]

Cell Line: Mer-positive (Kasumi-1, NOMO-1) and Flt3-ITD (MV4;11, MOLM-13) AML cell lines
Concentration: 10, 25, 50, 100, 300nM
Incubation Time: Continuous treatment, medium renewed twice weekly (14-21 days total)
Result: Reduced Kasumi-1 cell colony formation by 90% at 100 nM.
Reduced NOMO-1 cell colony formation by 71% at 100 nM.
Reduced MV4;11 cell colony formation by 61% at 50 nM.
Reduced MOLM-13 cell colony formation by 93% at 50 nM.
分子量

513.66

Formula

C26H35N5O4S
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

UNC1666 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

UNC16661429882-12-1UNC 1666UNC-1666FLT3ERKAktSTATApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Extracellular signal regulated kinasesPKBProtein kinase Bdual-target Mer/Flt3 tyrosine kinase inhibitorprimary AMLKasumi-1 AML cellsMV4;11 Flt3-ITD AML cellsacute myeloid leukemiaInhibitorinhibitorinhibit

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