2. Protein Tyrosine Kinase/RTK
  3. Anaplastic lymphoma kinase (ALK)
  4. KRCA-0377

KRCA-0377 是一种具有口服活性的 ALK 抑制剂，其 IC50 为 0.001 μM。KRCA-0377 还可抑制突变型 ALK 酶，IC50 值 ≤0.01 μM。KRCA-0377 对癌细胞具有细胞毒性，并可抑制异种移植小鼠模型中的肿瘤生长。KRCA-0377 可用于 ALK 阳性非小细胞肺癌的研究。

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KRCA-0377

KRCA-0377 Chemical Structure

CAS No. : 1845711-03-6

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KRCA-0377 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

KRCA-0377 is an orally active ALK inhibitor with an IC50 of 0.001 μM. KRCA-0377 also inhibits mutant ALK enzyme with IC50 values ≤0.01 μM. KRCA-0377 shows cytotoxicity against cancer cells and inhibits tumor growth in xenograft mice models. KRCA-0377 can be used for the research of ALK-positive non-small-cell lung cancer[1].

体外研究
(In Vitro)

KRCA-0377 (Compound 8) (30 min) 可强效抑制野生型 ALK，其 IC50 为 0.001 μM；同时抑制 ALKL1196M 突变酶，其 IC50 为 0.01 μM[1]。
KRCA-0377 (30 min) 可强效抑制多种对 Crizotinib (HY-50878) 耐药的 ALK 突变酶，包括 ALKG1202R (IC50 = 0.0059 μM)、ALKG1269A (IC50 = 0.0017 μM)、ALKT1151-L1152 inst T (IC50 = 0.0023 μM)、ALKF1174L (IC50 = 0.0021 μM) 和 ALKC1156Y (IC50 = 0.0030 μM)[1]。
KRCA-0377 (72 h) 在孵育 72 h 后可诱导 ALK 阳性 H2228 (CC50 = 0.01 μM)、H3122 (CC50 = 0.008 μM) 和 Ba/F3 ALKL1196M (CC50 = 0.036 μM) 细胞产生细胞毒性[1]。
KRCA-0377 (1 μM) 可抑制一个包含 96 种激酶的激酶组中约三分之一的激酶，抑制率超过 90%[1]。

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

KRCA-0377 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: H2228, H3122, Ba/F3 L1196M cells (all harboring EML4-ALK fusion genes)
Concentration: /
Incubation Time: 72 h
Result: Induced cytotoxicity in H2228 cells with a CC50 of 0.01 μM.
Induced cytotoxicity in H3122 cells with a CC50 of 0.008 μM.
Induced cytotoxicity in Ba/F3 L1196M cells with a CC50 of 0.036 μM.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC
Rat[1] 20 mg/kg p.o. 1.120 μg/mL 15.900 μg·h/mL
体内研究
(In Vivo)

KRCA-0377 (Compound 8) (50 mg/kg；口服给药，每日 1 次，连续 14 天) 可在雌性裸鼠中对 H3122 异种移植瘤的生长产生具有统计学意义的抑制作用[1]。

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

Animal Model: nude mice with H3122 xenograft (female)[1]
Dosage: 50 mg/kg
Administration: p.o.; daily; 14 days
Result: Achieved significant tumor growth inhibition, with tumor volumes remaining suppressed near the initial ~200 mm3 over the 14-day treatment and observation period.
Demonstrated statistically significant efficacy relative to the control group on the final study day (p < 0.01).
Caused no significant body weight changes in treated mice.
分子量

488.00

Formula

C23H26ClN5O3S
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

KRCA-0377 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)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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:

KRCA-03771845711-03-6KRCA0377KRCA 0377Anaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246ALK kinase activityantineoplastic agentxenograft modelsALK L1196M mutant enzymeG1202R ALK mutantT1151-L1152 inst T ALK mutant enzymeF1174L ALK mutant enzymewild-type ALKG1269A ALK mutant enzymeALK-positive non-small-cell lung cancerInhibitorinhibitorinhibit

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目录号：
HY-116636
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