SAH-SOS1A TFA

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SAH-SOS1A TFA

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

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-basedSOS1/KRASprotein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC₅₀=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-drivencancercell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS^[1].

IC₅₀& Target

KRAS-SOS1

KRas G12C

140 nM (EC₅₀)

KRas G12D

109 nM (EC₅₀)

KRas G12V

154 nM (EC₅₀)

KRas G12S

155 nM (EC₅₀)

KRas Q61H

175 nM (EC₅₀)

K-Ras WT

106 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^[1].
SAH-SOS1A TFA (5-40 μM; 4 hours) dose-responsively inhibits MEK1/2, ERK1/2, and AKT phosphorylation^[1].

Cell Viability Assay^[1]

Cell Line:	Panc 10.05 cells bearing the KRAS G12D mutation
Concentration:	0.625-40 μM
Incubation Time:	24 hours
Result:	Dose-responsively impaired the viability of cancer cells bearing KRAS G12D.

Western Blot Analysis^[1]

Cell Line:	Panc 10.05 cells
Concentration:	5-40 μM
Incubation Time:	Indicated doses for 4 h, followed by 15-min stimulation with EGF
Result:	Dose-responsively inhibited MEK1/2, ERK1/2, and AKT phosphorylation.

体内研究
(In Vivo)

SAH-SOS1A (0.2 μL of 10 mM solution; injection; 48 hours; abdomens ofD. melanogasterRas85D^V12/ActinGS) treatment notably decreases the phosphorylation state of ERK1/2^[1].

分子量

2301.55

性状

Solid

Formula

C₁₀₂H₁₆₀N₂₇F₃O₃₀

Sequence

Arg-Arg-Phe-Phe-Gly-Ile-Aaa-Leu-Thr-Asn-Aaa-Leu-Lys-Thr-Glu-Glu-Gly-Asn (Covalent bridge:Aaa7-Aaa11)

Sequence Shortening

RRFFGI{Aaa}LTN{Aaa}LKTEEGN (Covalent bridge:Aaa7-Aaa11)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light, under nitrogen

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

溶解性数据

In Vitro:

H₂O : 33.33 mg/mL(14.48 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	0.4345 mL	2.1724 mL	4.3449 mL
5 mM	0.0869 mL	0.4345 mL	0.8690 mL
10 mM	0.0434 mL	0.2172 mL	0.4345 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light, under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。