2. GPCR/G Protein MAPK/ERK Pathway Stem Cell/Wnt
  3. Ras ERK
  4. (7R)-Eras-4001

(7R)-Eras-4001 是一种口服有效的 KRAS 突变体抑制剂，对 H-RAS 和 N-RAS 具有显著的选择性。(7R)-Eras-4001 通过阻断 RAF 家族蛋白介导的下游信号通路，抑制 KRASG12D-RAF1 RBD 复合物形成及 ERK1/2 磷酸化，从而有效遏制癌细胞活力。(7R)-Eras-4001 呈剂量依赖性地诱导肿瘤生长抑制与消退，还能降低血浆 ERK1/2 磷酸化水平。(7R)-Eras-4001 与抗 PD-1 Cetuximab (HY-P9905) 有协同作用。(7R)-Eras-4001 可用于非小细胞肺癌、胰腺癌、结直肠癌及卵巢癌的研究。

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(7R)-Eras-4001

(7R)-Eras-4001 Chemical Structure

CAS No. : 3024878-21-2

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Other Forms of (7R)-Eras-4001:

(7R)-Eras-4001 相关抗体

Top Publications Citing Use of Products

查看 Ras 亚型特异性产品:

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K-Ras H-Ras N-Ras Ras

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(7R)-Eras-4001 is an orally active KRAS mutant inhibitor with remarkable selectivity for H-RAS and N-RAS. (7R)-Eras-4001 effectively suppresses cancer cell viability by blocking downstream signaling pathways mediated by RAF family proteins, inhibiting the formation of the KRASG12D-RAF1 RBD complex and the phosphorylation of ERK1/2. (7R)-Eras-4001 induces tumor growth inhibition and regression in a dose-dependent manner, and also reduces plasma ERK1/2 phosphorylation levels. (7R)-Eras-4001 exerts a synergistic effect with anti-PD-1 Cetuximab (HY-P9905). (7R)-Eras-4001 can be used in research on non-small cell lung cancer, pancreatic cancer, colorectal cancer, and ovarian cancer[1][2].

IC50 & Target

KRAS(G12C)

 

KRas G12D

 

KRas G12V

 

体外研究
(In Vitro)

ERAS-4001 强效抑制 KRASG12C 和 KRASG13D 突变癌细胞系的 3D 细胞活力，4-7 天时的 IC50 为 0.7-56.0 nM，但在非 KRAS 依赖型 (A375、NCI-H226) 和 KRASQ61H 突变型 (NCI-H460) 细胞系中活性极低[1]。

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

(7R)-Eras-4001 相关抗体:

Cell Viability Assay[1]

Cell Line: SW620, LU99 and MKN-1
Concentration: IC50
Incubation Time: /
Result: Inhibited cell viability with IC50s of 12.6 nM, 3.6 nM and 2.7 nM, respectively.
体内研究
(In Vivo)

(7R)-Eras-4001 (100 mg/kg；口服；每日 2 次) 可延缓肿瘤生长，在 KRASG12D 胰腺癌同源模型中与抗 PD-1 联合使用时可实现肿瘤完全消退并产生持久的免疫记忆[1]。
(7R)-Eras-4001 (50-150 mg/kg；口服；每日 2 次) 可抑制肿瘤生长，且在 KRASG12D 结直肠癌 CDX 模型中与西妥昔单抗联用时能产生更强的抗肿瘤疗效[1]。
(7R)-Eras-4001 (30-300 mg/kg；口服；每日 2 次；持续 28 天) 在 KRASG12D 胰腺癌异种移植模型中经每日 2 次口服给药 28 天后，呈现出剂量依赖性的血浆暴露特征，并可抑制肿瘤 ERK1/2 信号通路[1]。
(7R)-Eras-4001 (100 mg/kg；口服；每日 2 次) 在 KRASG12D 和 KRASG12V 突变型皮下异种移植模型中可实现 77%至 83%的肿瘤消退或生长抑制[1]。

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

Animal Model: Pancreatic ductal adenocarcinoma tumor-bearing Mice[1]
Dosage: 100 mg/kg
Administration: p.o.; twice daily
Result: Delayed tumor growth relative to vehicle as monotherapy.
Enabled complete tumor regression with durable immune memory when combined with anti-PD-1, with all mice having no measurable tumors from day 50 through study end and no tumors forming after KPC cell rechallenge.
分子量

743.19

Formula

C36H39ClF4N8O3
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

(7R)-Eras-4001 相关分类

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  • 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:

(7R)-Eras-40013024878-21-2RasERKExtracellular signal regulated kinasesKRAS G12Xcolorectal cancerpancreatic cancerRAF1 RBDNRASERK1/2wild-type KRASnon-small cell lung cancerwild-type HRASRAF family proteinsInhibitorinhibitorinhibit

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