2. Protein Tyrosine Kinase/RTK
  3. c-Met/HGFR
  4. D6808

D6808 是高度选择性、强效的 c‑Met 抑制剂，IC50 值为 2.9 nM。D6808 诱导细胞凋亡以及细胞周期阻滞。D6808 可用于非小细胞肺癌和胃癌的研究。

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D6808 Chemical Structure

D6808 Chemical Structure

CAS No. : 3029240-84-1

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D6808 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

D6808 is a highly selective and potent c‑Met inhibitor with an IC50 value of 2.9 nM. D6808 induces cell apoptosis and cell cycle arrest. D6808 can be used for the research of NSCLC and gastric cancers[1].

IC50 & Target

IC50: 2.9 nM (c‑Met)[1]
体外研究
(In Vitro)

D6808 shows c-Met biochemical kinase inhibitory activity with an IC50 value of 2.9 nM[1].
D6808 (0.0001-10 μM; 5 d) shows cellular antiproliferative potency to Hs746T cancer cells with an IC50 value of 0.7 nM[1].
D6808 displays extraordinary kinome selectivity with IC50 values of 401.3, 437.2, 1386 and 203.9 nM for Axl, TrkA, TrkB and TrkC kinase, respectively[1].
D6808 (0-10 μM; 72 h) show antiproliferative potency to Tpr-Met fusion protein-transformed Ba/F3 cells with IC50 values of 4.3, 4.2, 3.2, 1.0, 39.0 and 33.4 nM for Ba/F3-Tpr-Met, Ba/F3-Tpr-MetF1200L, Ba/F3-Tpr-MetM1250T, Ba/F3-Tpr-MetH1094Y, Ba/F3-Tpr-MetF1200I, Ba/F3-Tpr-MetL1195V, respectively[1].
D6808 (0-30 nM; 12 h) affects activation of MET and dose-dependently decreases the protein levels of CDK2, CDK4, CDK6, cyclin D2, and cyclin E1 and the cleave activation of PARP and caspase-9 in Ba/F3-Tpr-Met cells[1].
D6808 (40 nM; 24 h) induces cell apoptosis and 87.37% G0/G1 phase arrest in Ba/F3-Tpr-Met cells[1].

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

D6808 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Hs746T cancer cell line
Concentration: 0.0001-10 μM
Incubation Time: 5 days
Result: Inhibited the cell proliferation of Hs746T cancer cells.

Western Blot Analysis[1]

Cell Line: Hs746T and Ba/F3-Tpr-Met cell lines
Concentration: 0, 0.37, 1.1, 3.3, 10 and 30 nM
Incubation Time: 12 hours
Result: Suppressed the activation of MET in Hs746T and Ba/F3-Tpr-Met cells.

Apoptosis Analysis[1]

Cell Line: Ba/F3-Tpr-Met cell line
Concentration: 40 nM
Incubation Time: 24 hours
Result: Induced 50.89% apoptosis after 48 h treatment.
体内研究
(In Vivo)

1.19 Pharmacokinetic Properties of D6808 in Rats[1].

Rats
IV 2.0 mg/kg		 Rats
PO 10.0 mg/kg		 Rats
IP 10.0 mg/kg
T1/2 (h) 0.57 2.49 4.63
Tmax (h) 0.08 0.25 0.25
Cmax (ng/mL) 1071.23 60.98 282.12
AUC0-t (h×ng/mL) 483.84 48.89 820.38
Vz (mL/kg) 3470.78
CL (mL/h/kg) 4207.06
MRT0-t (h) 0.36 1.71 3.40
F (%) 2.02 33.91

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

558.55

Formula

C30H25F3N6O2
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

D6808 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:

D68083029240-84-1D 6808D-6808c-Met/HGFRmacrocyclicNSCLCgastric cancertepotinibapoptosiscell cycle arrestInhibitorinhibitorinhibit

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