2. GPCR/G Protein MAPK/ERK Pathway PI3K/Akt/mTOR Stem Cell/Wnt Apoptosis
  3. Ras PI3K ERK mTOR Apoptosis
  4. RMC-4998

RMC-4998 是一种口服有效的靶向活性或 GTP 结合状态的 KRASG12C 突变体抑制剂。RMC-4998 可以与细胞内 CYPA 和激活状态下的 KRASG12C 突变体形成三重复合物，IC50 值为 28 nM。RMC-4998 可以抑制 KRASG12C 突变癌细胞中的 ERK 信号传导并诱导细胞凋亡 (apoptosis)。RMC-4998 可用于肿瘤的研究。

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RMC-4998 Chemical Structure

RMC-4998 Chemical Structure

CAS No. : 2642037-07-6

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RMC-4998 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRASG12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRASG12C mutant, with an IC50 value of 28 nM. RMC-4998 can inhibit ERK signaling in KRASG12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research[1][2].
IC50 & Target

KRASG12C[1].
体外研究
(In Vitro)

RMC-4998 (100 nM, 120 h) 通过将亲环蛋白 A (CYPA) 募集到突变 KRAS 的活性状态从而破坏 KRASG12C 突变细胞中的致癌信号传导[1]。
RMC-4998 可以抑制 KRASG12C 突变癌细胞中 ERK 信号相关蛋白的表达和细胞增殖[1]。
RMC-4998 (0-1000 nM, 72 h) 通过抑制 PI3K/mTOR 和 ERK 信号通路来抑制肺癌细胞活力[2]。
RMC-4998 (30 nM, 96 h) 可以抑制 ERK 蛋白磷酸化并抑制 LU65 细胞活力[3]。

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

RMC-4998 相关抗体:

Cell Proliferation Assay[1].

Cell Line: KRASG12C mutant cancer cell LU65 and H358 models
Concentration: 100 nM
Incubation Time: 120 h
Result: Inhibited cell proliferation, with an IC50 value of 0.28 nM.

Western Blot Analysis[1].

Cell Line: KRASG12C mutant cancer cell models (H358, H23, H2030, SW873, MIA PaCa-2)
Concentration: 0-10000 nM
Incubation Time: 2 h
Result: Inhibited phosphorylation of ERK signaling related proteins, including PSK, ERK, and CRAF proteins.

Cell Viability Assay[2].

Cell Line: H358, LU65, H2122, LU99A, SW1573 cells
Concentration: 0-1000 nM
Incubation Time: 72 h
Result: Had the strongest inhibitory effect on H358, LU65, and H2122 cells, but its effect was weaker in cell lines that are most resistant to inactive KRASG12C inhibitors such as LU99A and SW1573.
体内研究
(In Vivo)

RMC-4998 (10-200 mg/kg; 每天 1 次; 28 天; 口服) 在携带 NCI-H358 异种移植物的小鼠中抑制肿瘤中 ERK 磷酸化并具有抗肿瘤活性[1]。
RMC-4998 (80 mg/kg; 每天 1 次; 4 周; 口服) 在非小细胞肺癌小鼠中可以促进肿瘤消退，具有抗肿瘤活性[2]。
RMC-4998 (100 mg/kg; 每天 1 次; 口服) 在 sotorasib-R LU65 异种移植小鼠中导致肿瘤消退并抑制肿瘤中 ERK 磷酸化表达[3]。

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

Animal Model: Mice model bearing H358 CDX tumors[1].
Dosage: 10-200 mg/kg
Administration: Oral gavage (p.o.); once daily; 28 days
Result: Inhibited ERK phosphorylation in tumors for about 24 hours and induced cell apoptosis, leading to tumor regression.
Animal Model: The cell-line derived H2122 KRASG12C lung adenocarcinoma xenograft model (CDX)[2].
Dosage: 80 mg/kg
Administration: Oral gavage (p.o.); once daily; 4 weeks
Result: Inhibited tumor growth for 30-35 days.
Animal Model: Sotorasib-R LU65 mice xenograft model[3].
Dosage: 100 mg/kg
Administration: Oral gavage (p.o.); once dailys
Result: Reduced tumor volume and lowered the expression of pERK protein in the tumor.
分子量

983.25

Formula

C57H74N8O7
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

纯度 & 产品资料
参考文献

RMC-4998 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:

RMC-49982642037-07-6RMC4998RMC 4998RasPI3KERKmTORApoptosisPhosphoinositide 3-kinaseExtracellular signal regulated kinasesMammalian target of RapamycinKRAS mutationLU65 cellNSCLCanti-tumor activityInhibitorinhibitorinhibit

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