2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. KRASG12C IN-17

KRASG12C IN-17 是一种具有口服活性的共价性 KRASG12C 抑制剂，并在 KRASG12C 突变的癌细胞中表现出强效的抑制活性（NCI-H23 IC50 = 0.7 nM；NCI-H358 IC50 = 0.5 nM)。 KRASG12C IN-17 可在 GDP 结合态与 GMPPNP 结合态下高效且不可逆地与 KRASG12C 形成共价结合，修饰率超过 96%。 KRASG12C IN-17 可用于 KRAS 驱动的肿瘤研究，包括结直肠癌。

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KRASG12C IN-17

KRASG12C IN-17 Chemical Structure

CAS No. : 2966924-23-0

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KRASG12C IN-17 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KRASG12C IN-17 is an orally active covalent KRASG12C inhibitor, showing strong inhibitory activity in KRASG12C-mutant cancer cells (NCI-H23 IC50 = 0.7 nM; NCI-H358 IC50 = 0.5 nM). KRASG12C IN-17 covalently and irreversibly binds to KRASG12C with > 96% modification efficiency in both GDP-bound and GMPPNP-bound conformations. KRASG12C IN-17 can be used for studies of KRAS-driven cancers, including colorectal cancer[1].

IC50 & Target

KRas G12C

 

体外研究
(In Vitro)

KRASG12C IN-17 (compound 19) 可显著抑制 KRASG12C 突变的 NCI-H23 与 NCI-H358 细胞增殖，在 72-144 小时处理后，其 IC50 分别为 0.7 nM 和 0.5 nM[1]。
KRASG12C IN-17 可在 GDP 结合态与 GMPPNP 结合态下高效且不可逆地修饰 KRASG12C，其修饰率在 15 分钟内超过 96%[1]。
KRASG12C IN-17 可在 Ba/F3 模型中有效抑制多种耐药相关 KRASG12C 突变体，包括 R68S、H95Q、Y96C 和 Q99L[1]。
KRASG12C IN-17 在部分 KRASG12C 次级突变癌细胞株中表现出抗增殖活性，尤其在 Y96C 与 Q99L 突变中仍保持较强效力。

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

KRASG12C IN-17 相关抗体:

Cell Proliferation Assay[1]

Cell Line: NCI-H23 (KRASG12C), NCI-H358 (KRASG12C)
Concentration: 0.7 nM (NCI-H23), 0.5 nM (NCI-H358)
Incubation Time: 72 h
Result: Significantly inhibited proliferation of KRASG12C-mutant NCI-H23 and NCI-H358 cells.
体内研究
(In Vivo)

KRASG12C IN-17 (30 mg/kg，口服灌胃，QD，连续给药 28 天) 在 SW837 KRASG12C 异种移植模型中表现出显著的体内活性，可实现 103% 的肿瘤生长抑制[1]。
KRASG12C IN-17 (30 mg/kg，口服灌胃，QD，连续给药 21 天) 在 Ba/F3 KRASG12C/R68S 异种移植模型中可显著降低肿瘤体积，达到 65.9% 的肿瘤减少率[1]。

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

Animal Model: SW837 human rectal cancer xenograft (KRASG12C) female NOD SCID mice (6–7 weeks old, 20.5–23.7 g)
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); once daily (QD); 28 days
Result: Achieved 103% tumor growth inhibition and induced near-complete tumor stasis without significant body-weight loss in SW837 KRASG12C xenograft models.
Animal Model: Ba/F3 KRASG12C/R68S xenograft model female NOD SCID mice (6-8 weeks old, 18.6-23.3 g)
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); once daily (QD); 21 days
Result: Reduced tumor volume by 65.9% and demonstrated good tolerability in Ba/F3 KRASG12C/R68S xenograft models.
分子量

650.69

Formula

C37H33F3N6O2
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

KRASG12C IN-17 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

KRASG12C IN-172966924-23-0RasKRAS G12Ccovalent inhibitorcolorectal cancerNSCLCresistance mutationR68Sxenograftoral bioavailabilitytumor stasisInhibitorinhibitorinhibit

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