SAH-SOS1A TFA
目录号: PL10845 纯度: ≥99%
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中文名称
SAH-SOS1A TFA
英文名称
SAH-SOS1A TFA
包装储存
Sealed storage, away from moisture and light, under nitrogenPowder -80°C 2 years;-20°C 1 ye
产品详情
SAH-SOS1A TFA 是一种基于肽的 SOS1/KRAS 蛋白相互作用抑制剂。SAH-SOS1A TFA 以纳摩尔亲和力 (EC50=106-175 nM) 与野生型和突变型 KRAS (G12D, G12V, G12C, G12S, Q61H) 结合,直接和独立地阻断核苷酸结合。SAH-SOS1A TFA 损害 KRAS 驱动的癌细胞活力,并通过阻断 KRAS 下游 ERK-MAPK 磷酸化信号级联的机制发挥作用。
生物活性
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC 50 =106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS.
性状
Solid
IC50 & Target[1][2]
KRAS-SOS1 KRas G12C 140 nM (EC50)
体外研究(In Vitro)
SAH-SOS1A TFA (0.625-40 μM; 24 hours) dose-responsively impairs the viability of cancer cells bearing G12D, G12C, G12V, G12S, G13D, and Q61H mutations with IC50 values in the 5- to 15-μM range. Cancer cells expressing wild-type KRAS, such as HeLa and Colo320-HSR cells, are similarly affected.
SAH-SOS1A TFA (5-40 μM; 4 hours) dose-responsively inhibits MEK1/2, ERK1/2, and AKT phosphorylation. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
SAH-SOS1A (0.2 μL of 10 mM solution; injection; 48 hours; abdomens of D. melanogaster Ras85D/ActinGS) treatment notably decreases the phosphorylation state of ERK1/2. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisture and light, under nitrogenPowder -80°C 2 years;-20°C 1 ye
SequenceShortening
RRFFGI{Aaa}LTN{Aaa}LKTEEGN (Covalent bridge:Aaa7-Aaa11)
Sequence
Arg-Arg-Phe-Phe-Gly-Ile-Aaa-Leu-Thr-Asn-Aaa-Leu-Lys-Thr-Glu-Glu-Gly-Asn (Covalent bridge:Aaa7-Aaa11)
参考文献
[1]. Leshchiner ES, et al. Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices. Proc Natl Acad Sci U S A. 2015;112(6):1761-1766.
溶解度数据
In Vitro: H2O : 33.33 mg/mL (14.48 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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