产品号 #72162_C
酪氨酸激酶抑制剂；抑制 FGFR
总览
PD173074 是一种选择性、强效的 ATP 竞争性 FGFR 抑制剂。它同时作用于 FGFR3 和 FGFR1（IC50 分别为 5 和 21.5 nM），同时抑制 FGFR2、FGFR4 和 KDR。其效力比另一种常见的 FGFR 抑制剂 SU5402 强约 1000 倍。（Koziczak et al., Mohammadi et al., Trudel et al.）
重编程
·阻止使用 piggyBac 转座子产生的小鼠诱导多能干细胞的切除介导分化（Kaji et al.）。
·与 Oct4、Klf4、Klf2、LIF、CHIR99021 和 PD0325901 联合使用，可促进人胚胎干细胞 (ES) 重编程为 naïve 细胞，或使其维持在 naïve 状态。（Hanna et al.）
维护和自我更新
·抑制小鼠 ES 细胞分化并维持未分化状态（Kunath et al., Ying et al.）。
分化
·阻止小鼠 ES 细胞的神经分化（Stavridis et al.）。
·促进人 ES 细胞分化，但不会在 naïve 或“ground state”时起作用（Hanna et al.）。
别名
Not applicable
细胞类型
多能干细胞
种属
人，小鼠，非人灵长类，其它细胞系，大鼠
应用
分化，培养，重编程
研究领域
干细胞生物学
CAS 编号
219580-11-7
化学式
C₂₈H₄₁N₇O₃
分子量
523.7 克/摩尔
纯度
≥ 95 %
通路
酪氨酸激酶
靶点
FGFR
Protocols and Documentation
Find supporting information and directions for use in the Product Information Sheet or explore additional protocols below.
Applications
This product is designed for use in the following research area(s) as part of the highlighted workflow stage(s). Explore these workflows to learn more about the other products we offer to support each research area.
Resources and Publications
Educational Materials (3)
Publications (8)
Human embryonic stem cells with biological and epigenetic characteristics similar to those of mouse ESCs. Proceedings of the National Academy of Sciences of the United States of America 2010 MAY
Abstract
Human and mouse embryonic stem cells (ESCs) are derived from blastocyst-stage embryos but have very different biological properties, and molecular analyses suggest that the pluripotent state of human ESCs isolated so far corresponds to that of mouse-derived epiblast stem cells (EpiSCs). Here we rewire the identity of conventional human ESCs into a more immature state that extensively shares defining features with pluripotent mouse ESCs. This was achieved by ectopic induction of Oct4, Klf4, and Klf2 factors combined with LIF and inhibitors of glycogen synthase kinase 3beta (GSK3beta) and mitogen-activated protein kinase (ERK1/2) pathway. Forskolin, a protein kinase A pathway agonist which can induce Klf4 and Klf2 expression, transiently substitutes for the requirement for ectopic transgene expression. In contrast to conventional human ESCs, these epigenetically converted cells have growth properties, an X-chromosome activation state (XaXa), a gene expression profile, and a signaling pathway dependence that are highly similar to those of mouse ESCs. Finally, the same growth conditions allow the derivation of human induced pluripotent stem (iPS) cells with similar properties as mouse iPS cells. The generation of validated naïve" human ESCs will allow the molecular dissection of a previously undefined pluripotent state in humans and may open up new opportunities for patient-specific�
Virus-free induction of pluripotency and subsequent excision of reprogramming factors Nature 2009
Abstract
Reprogramming of somatic cells to pluripotency, thereby creating induced pluripotent stem (iPS) cells, promises to transform regenerative medicine. Most instances of direct reprogramming have been achieved by forced expression of defined factors using multiple viral vectors. However, such iPS cells contain a large number of viral vector integrations, any one of which could cause unpredictable genetic dysfunction. Whereas c-Myc is dispensable for reprogramming, complete elimination of the other exogenous factors is also desired because ectopic expression of either Oct4 (also known as Pou5f1) or Klf4 can induce dysplasia. Two transient transfection-reprogramming methods have been published to address this issue. However, the efficiency of both approaches is extremely low, and neither has been applied successfully to human cells so far. Here we show that non-viral transfection of a single multiprotein expression vector, which comprises the coding sequences of c-Myc, Klf4, Oct4 and Sox2 linked with 2A peptides, can reprogram both mouse and human fibroblasts. Moreover, the transgene can be removed once reprogramming has been achieved. iPS cells produced with this non-viral vector show robust expression of pluripotency markers, indicating a reprogrammed state confirmed functionally by in vitro differentiation assays and formation of adult chimaeric mice. When the single-vector reprogramming system was combined with a piggyBac transposon, we succeeded in establishing reprogrammed human cell lines from embryonic fibroblasts with robust expression of pluripotency markers. This system minimizes genome modification in iPS cells and enables complete elimination of exogenous reprogramming factors, efficiently providing iPS cells that are applicable to regenerative medicine, drug screening and the establishment of disease models.
The ground state of embryonic stem cell self-renewal. Nature 2008 MAY
Abstract
In the three decades since pluripotent mouse embryonic stem (ES) cells were first described they have been derived and maintained by using various empirical combinations of feeder cells, conditioned media, cytokines, growth factors, hormones, fetal calf serum, and serum extracts. Consequently ES-cell self-renewal is generally considered to be dependent on multifactorial stimulation of dedicated transcriptional circuitries, pre-eminent among which is the activation of STAT3 by cytokines (ref. 8). Here we show, however, that extrinsic stimuli are dispensable for the derivation, propagation and pluripotency of ES cells. Self-renewal is enabled by the elimination of differentiation-inducing signalling from mitogen-activated protein kinase. Additional inhibition of glycogen synthase kinase 3 consolidates biosynthetic capacity and suppresses residual differentiation. Complete bypass of cytokine signalling is confirmed by isolating ES cells genetically devoid of STAT3. These findings reveal that ES cells have an innate programme for self-replication that does not require extrinsic instruction. This property may account for their latent tumorigenicity. The delineation of minimal requirements for self-renewal now provides a defined platform for the precise description and dissection of the pluripotent state.
更多信息
| Molecular Weight | 523.7 g/mol |
|---|---|
| Species | Human, Mouse, Non-Human Primate, Other, Rat |
| Alternative Names | Not applicable |
| Cas Number | 219580-11-7 |
| Chemical Formula | C₂₈H₄₁N₇O₃ |
| Purity | ≥ 95% |
| Target | FGFR |
| Pathway | Tyrosine Kinase |
PRODUCTS ARE FOR RESEARCH USE ONLY AND NOT INTENDED FOR HUMAN OR ANIMAL DIAGNOSTIC OR THERAPEUTIC USES UNLESS OTHERWISE STATED. FOR ADDITIONAL INFORMATION ON QUALITY AT STEMCELL, REFER TO WWW.STEMCELL.COM/COMPLIANCE.
