2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. FGFR-IN-26

FGFR-IN-26 是一种具有口服活性的 FGFR 抑制剂。FGFR-IN-26 可抑制 FGFR2 野生型及临床相关耐药突变。FGFR-IN-26 可抑制 FGFR2 扩增的异种移植小鼠模型中的肿瘤生长。FGFR-IN-26 可用于癌症研究，例如胃癌。

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FGFR-IN-26

FGFR-IN-26 Chemical Structure

CAS No. : 2823290-68-0

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FGFR-IN-26 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FGFR-IN-26 is an orally active FGFR inhibitor. FGFR-IN-26 inhibits FGFR2 wild-type and clinically relevant resistance mutations. FGFR-IN-26 inhibits tumor growth in FGFR2-amplified xenograft mouse models. FGFR-IN-26 can be used for the research of cancer, suah as gastric carcinoma[1].

IC50 & Target[1]

FGFR3

0.2 nM (IC50)

FGFR2

2.1 nM (IC50)

FGFR1

3.8 nM (IC50)

FGFR4

49 nM (IC50)

体外研究
(In Vitro)

FGFR-IN-26 (Compound 13) 可强效抑制表达 FGFR1、FGFR2 (野生型及临床相关耐药突变体)、FGFR3 和 FGFR4 的 Ba/F3 细胞增殖，对 FGFR2K660E (IC50 = 0.6 nM) 和 FGFR3 (IC50 = 0.2 nM) 的抑制活性最强，且对 FGFR2 的选择性比对 FGFR4 高 23 倍[1]。
FGFR-IN-26 可强效结合 FGFR2 (Kd = 2.7 nM)、FGFR2 (N550K) (Kd = 10 nM)、FGFR1 (Kd = 21 nM) 和 FGFR3 (Kd = 3.5 nM)，对 FGFR2 的选择性是 FGFR4 的 85 倍；且与 FGFR2 (C491F) 的可逆结合作用较弱 (Kd = 956 nM)[1]。
FGFR-IN-26 (72-120 h) 可强效抑制由 FGFR2 驱动的 SNU-16 胃癌细胞 (IC50 = 7.5 nM) 和携带 FGFR2N550K 突变的 AN3CA 子宫内膜癌细胞 (IC50 = 13 nM) 的活力[1]。
FGFR-IN-26 (1 μM) 对人类激酶组具有高选择性，仅能抑制 13 种野生型激酶的活性达 90% 以上[1]。

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

FGFR-IN-26 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 AUClast Cmax F Vd CL
Rat[1] 2 mg/kg i.v. 0.7 h 1032 ng·h/mL / / 0.8 L/kg 32 mL/min/kg
Rat[1] 10 mg/kg p.o. 2.4 h 1069 ng·h/mL 352 ng/mL 21 % / /
体内研究
(In Vivo)

FGFR-IN-26 (Compound 13) (10 mg/kg；口服；每日 2 次；连续 21 天) 在裸鼠的 FGFR2 扩增型 SNU-16 胃癌异种移植模型中实现了 152% 的肿瘤生长抑制率，且未出现显著的体重下降[1]。

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

Animal Model: FGFR2-amplified SNU-16 gastric carcinoma xenograft model in nude mice (female, 6-8-week-old)[1]
Dosage: 10 mg/kg
Administration: p.o.; twice daily; 21 days
Result: Achieved 152% tumor growth inhibition (TGI) over 21 days.
Reached a terminal day 21 plasma level of 192 ng/mL (480 nM) 4 h after the final dose.
Caused no significant body weight loss after 21 days.
分子量

401.46

Formula

C22H23N7O
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

FGFR-IN-26 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

FGFR-IN-262823290-68-0FGFRFibroblast growth factor receptorFGFR3intrahepatic cholangiocarcinomagastric carcinomaFGFR1endometrial cancerFGFR4FGFR2SNU-16Ba/F3 cellsAN3CAInhibitorinhibitorinhibit

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