2. MAPK/ERK Pathway Protein Tyrosine Kinase/RTK Apoptosis
  3. Raf Src Apoptosis
  4. CCT241161

CCT241161 是一种口服有效的泛型 RAF 抑制剂，其对 LCK, CRAF, SRC, V600E-BRAF 和 BRAF 的 IC50 值分别为 3, 6, 10, 15 和 30 nM。CCT241161 对 BRAF 和 NRAS 突变的黑色素瘤具有良好的活性。CCT241161 还具有抗癌细胞增殖活性。

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CCT241161 Chemical Structure

CCT241161 Chemical Structure

CAS No. : 1163719-91-2

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规格 价格 是否有货 数量
1 mg ￥2785
1 - 2 周
5 mg   询价  
10 mg   询价  

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CCT241161 相关抗体

Top Publications Citing Use of Products

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Lck Fyn Blk

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity[1].

IC50 & Target

CRAF

6 nM (IC50)

Braf

30 nM (IC50)

BRafV600E

15 nM (IC50)

SRC

0.01 μM (IC50)

LCK

0.003 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 IC50
10 nM
Compound: 15; CCT241161
Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 72 hrs by CellTiter-Glo assay
Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 72 hrs by CellTiter-Glo assay
[PMID: 29461827]
体外研究
(In Vitro)

CCT241161 (1, 3, 10, 30, 100 nM; 24 h) inhibits MEK and ERK in WM266.4 cells[1].
CCT241161 (1, 10, 100 nM and 1, 10, 100 µM) inhibits BRAFV600E in Ba/F3 cells[1].
CCT241161 (0.5 µM; 20 days) inhibits A375 cell but not cause drug resistance[1].
CCT241161 (1 µM , 4 h) inhibits BRAF-inhibitor-resistant melanoma cells[1].
CCT241161 (0.1, 0.3, 1, 3, 10 µM; 24 h) inhibits MEK in NRAS mutant cells[1].
CCT241161 (0.1, 1, 10, 100 µM) shows anti-proliferative activity in D04 cells[1].

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

CCT241161 相关抗体:

Cell Viability Assay[1]

Cell Line: WM266.4 cells (BRAF mutant)
Concentration: 1, 3, 10, 30, 100 nM
Incubation Time: 24 h
Result: Exhibited effects of inhibiting MEK and ERK in WM266.4 cells.

Cell Viability Assay[1]

Cell Line: Ba/F3 cells
Concentration: 1, 10, 100 nM and 1, 10, 100 µM
Incubation Time:
Result: Inhibited BRAF-V600E and BRAF-T529N, V600E in Ba/F3 cells.

Cell Viability Assay[1]

Cell Line: A375 cell
Concentration: 0.5 µM
Incubation Time: 20 days
Result: Maintained inhibitory activity against A375 cell ,without drug resistance in 20 days.

Cell Proliferation Assay[1]

Cell Line: D04 cells
Concentration: 0.1, 1, 10, 100 µM
Incubation Time:
Result: Efficiently inhibited NRAS mutant cell growth.

Western Blot Analysis[1]

Cell Line: patient #2 (PLX4720-resistant cells from patient with vemurafenib-resistant melanoma)
Concentration: 1 µM
Incubation Time: 4 h
Result: Inhibited MEK, ERK, and SRC in the cells from patient #2.

Western Blot Analysis[1]

Cell Line: D04 cells
Concentration: 0.1, 0.3, 1, 3, 10 µM
Incubation Time: 24 h
Result: Showed activity of surpressing MEK in NRAS mutant cells.
体内研究
(In Vivo)

CCT241161 (10, 20 mg/kg; i.g; once a day for 7 days) inhibits the growth of BRAF mutant A375, PLX4720-resistant A375 and NRAS mutant DO4 tumor xenografts in mice[1].

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

Animal Model: Female nude mice (5 to 6- week-old)[1].
Dosage: 10, 20 mg/kg
Administration: Oral gavage; once a day for 7 days.
Result: Showed activity of tumor regression in nude mice with xenografts tumor of BRAF mutant A375, PLX4720-resistant A375 (A375/R) and NRAS mutant DO4, without causing any body weight loss to the mice.
分子量

541.62

Formula

C28H27N7O3S
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

CCT241161 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)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

CCT2411611163719-91-2CCT 241161CCT-241161RafSrcApoptosisRaf kinasesMalignant melanomaresistanceWM266.4Ba/F3A375D04Inhibitorinhibitorinhibit

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