Fulzerasib 是一种不可逆的 KRAS G12C 抑制剂，与西妥昔单抗具有协同抗癌作用。
| 生物活性 |
Fulzerasib is an irreversible KRAS G12C inhibitor, has a synergistic anti-cancer effect with cetuximab. |
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| 体外研究 |
Fulzerasib covalently inhibits the exchange of GDP/GTP nucleotides on KRAS G12C (IC50: 29 nM), locking KRAS in its inactive GDP binding state (RAS-GTP IC50: 74 nM), thereby blocking the KRAS signaling pathway (pERK IC50: 37 nM). Fulzerasib inhibited the growth of tumor cell lines carrying KRAS G12C mutations (IC50: 2-20 nM). |
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| 体内研究 |
Fulzerasib has strong anti-tumor activity in xenotransplantation of MIA Paca-2 CDX, NCI-H358 CDX like lung adenocarcinoma, patient derived xenotransplantation of colon adenocarcinoma SW837 CDX, lung cancer LU2529 PDX models in pancreatic cancer cell lines. |
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| 分子式 |
C32H30ClFN6O4
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| 分子量 |
617.07
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| CAS号 |
2641747-54-6
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| 中文名称 |
Fulzerasib
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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| 溶解性数据 |
In Vitro:
DMSO: 116.67 mg/mL (189.07 mM; Need ultrasonic) 配制储备液
*
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。 |
纯度： 99%
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Data Sheet
