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製品番号: HY-151905

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D6808

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.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 3029240-84-1
分子式: C₃₀H₂₅F₃N₆O₂
分子量:558.55

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (278 KB)

D6808 構造式

CAS 番号: 3029240-84-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

IC50: 2.9 nM (c‑Met)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
AGS	IC₅₀	>10000 nM Compound: 14; D6808	Antiproliferative activity against human AGS cells assessed as inhibition of cell proliferation incubated for 5 days by CCK-8 assay Antiproliferative activity against human AGS cells assessed as inhibition of cell proliferation incubated for 5 days by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	>10000 nM Compound: 14; D6808	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein Y1230H mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein Y1230H mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	1 nM Compound: 14; D6808	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein H1094Y mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein H1094Y mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	3.2 nM Compound: 14; D6808	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein M1250T mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein M1250T mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	33.4 nM Compound: 14; D6808	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein L1195V mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein L1195V mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	39 nM Compound: 14; D6808	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein F1200I mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein F1200I mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	4.2 nM Compound: 14; D6808	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein F1200L mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein F1200L mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	4.3 nM Compound: 14; D6808	Antiproliferative activity against mouse BaF3 cells harboring wild type Tpr-Met fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring wild type Tpr-Met fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
BaF3	IC₅₀	>10000 nM Compound: 14; D6808	Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein D1228N mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse BaF3 cells harboring Tpr-Met fusion protein D1228N mutant assessed as inhibition of cell proliferation incubated for 72 hrs by CCK-8 assay	[PMID: 36355693]
Hs746T	IC₅₀	0.7 nM Compound: 14; D6808	Antiproliferative activity against human Hs746T cells harboring MET alterations assessed as inhibition of cell proliferation incubated for 5 days by CCK8 assay Antiproliferative activity against human Hs746T cells harboring MET alterations assessed as inhibition of cell proliferation incubated for 5 days by CCK8 assay	[PMID: 36355693]
SNU-16	IC₅₀	>10000 nM Compound: 14; D6808	Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell proliferation incubated for 5 days by CCK-8 assay Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell proliferation incubated for 5 days by CCK-8 assay	[PMID: 36355693]

体外実験

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-Met^F1200L, Ba/F3-Tpr-Met^M1250T, Ba/F3-Tpr-Met^H1094Y, Ba/F3-Tpr-Met^F1200I, Ba/F3-Tpr-Met^L1195V, 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].

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

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.

体内実験

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
T_1/2 (h)	0.57	2.49	4.63
T_max (h)	0.08	0.25	0.25
C_max (ng/mL)	1071.23	60.98	282.12
AUC_0-t (h×ng/mL)	483.84	48.89	820.38
V_z (mL/kg)	3470.78
CL (mL/h/kg)	4207.06
MRT_0-t (h)	0.36	1.71	3.40
F (%)		2.02	33.91

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

化学情報

CAS 番号 3029240-84-1
分子量 558.55
分子式 C₃₀H₂₅F₃N₆O₂
SMILES

O=C1NCCCCN2C=C(C3=CN=C4C=CC(CCN5N=C(C6=CC(C(F)(F)F)=C1C=C6)C=CC5=O)=CC4=C3)C=N2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (278 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Wang C, et al. Discovery of D6808, a Highly Selective and Potent Macrocyclic c-Met Inhibitor for Gastric Cancer Harboring MET Gene Alteration Treatment. J Med Chem. 2022 Nov 24;65(22):15140-15164. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

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体積体積

分子量分子量

希釈計算機

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濃度 _(終了) 濃度 _(終了)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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