TTT 3002
TTT 3002 is a potent and orally active FLT3 inhibitor. TTT 3002 potently inhibits FLT3 phosphorylation by activating mutations at residue D835, with an IC50 of 0.2 nM. TTT 3002 can be used for AML (acute myeloid leukemia) research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 871037-95-5
- 分子式: C27H23N5O3
- 分子量:465.50
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
<0.25 nM
Compound: TTT-3002
|
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell proliferation measured after 24 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell proliferation measured after 24 hrs by MTT assay
|
[PMID: 32659083] |
TTT 3002 downregulates FLT3 phosphorylation (pFLT3) in Molm14 and MV4-11 cells[1].
TTT 3002 induces cell cycle arrest followed by marked induction of apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Molm14 and MV4-11 cells
-
Concentration:0, 0.25, 0.5, 1, 2 nM
-
Incubation Time:1 h
-
Result:Downregulated FLT3 phosphorylation (pFLT3) in Molm14 and MV4-11 cells in a dose-dependent manner. The IC50 for FLT3 phosphorylation in both cell lines was six- to seven fold lower for TTT 3002 compared with Quizartinib (HY-13001) at 0.2 vs 1.3 nM, respectively.
-
Cell Line:Molm14 and MV4-11 cells
-
Concentration:0, 1, 2, 5, 10 nM
-
Incubation Time:24 h
-
Result:Showed cell cycle arrest followed by marked induction of apoptosis, along with concurrent activation of caspase 3 and poly ADP ribose polymerase cleavage.
TTT 3002 (6 mg/kg, Oral gavage, single) is rapidly absorbed with a biphasic maximum serum concentration (Cmax) followed by a monoexponential decay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/C mice (female, age 6 to 8 weeks, received Ba/F3-ITD Luc+ cells by tail vein injection on day 0)[1]
-
Dosage:6 mg/kg
-
Administration:Oral gavage, twice per day, for 2 to 4 weeks
-
Result:Showed no significant changes in animal weight and was sufficient to eliminate the presence of Ba/F3-ITD Luc+ cells by day 17 (10 days of treatment).
-
Animal Model:Leukemic engrafted mice (female, age 6 to 8 weeks)[1]
-
Dosage:6 mg/kg
-
Administration:Oral gavage, single (Pharmacokinetic Analysis)
-
Result:After oral administration, TTT 3002 was rapidly absorbed with a biphasic maximum serum concentration (Cmax) followed by a monoexponential decay. The Cmax and area under the concentration-time curve from time 0 to infinity (AUC0→∞) were 613 nM and 3127 nM⋅h, respectively. The half-life, apparent volume of distribution, and apparent clearance were 3.6 hours, 21 L/kg, and 4.1 L/h per kilogram, respectively.
化学情報
-
CAS 番号 871037-95-5
-
分子量 465.50
-
分子式 C27H23N5O3
-
SMILES
C[C@]12N3C4=C(C5=CC=CC=C53)C(CNC6=O)=C6C7=C4N([C@](C[C@]2(N)C(NC)=O)([H])O1)C8=CC=CC=C78
-
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
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TTT 3002 関連分類
HY-111249 関連分類
Powered by Bioz