TH9619 |
| Katalog-Nr.GC73599 |
TH9619 ist ein starker Inhibitor der Dedrogenase- und Cyclodrolase-Aktivitäten sowohl in MTHFD1 als auch in MTHFD2 mit einem IC50-Wert von 47 nM und tötet gezielt Krebszellen ab.
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Cas No.: 2379556-22-4
Sample solution is provided at 25 µL, 10mM.
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TH9619 is a potent inhibitor of dedrogenase and cyclodrolase activities in both MTHFD1 and MTHFD2 with a IC50 value of 47 nM, and selectively kills cancer cells. TH9619 induces apoptosis by blocking the S phase. TH9619 has antitumor activity.
TH9619 (7.8-1,000 nM, 420 s) displays high selectivity toward binding and stabilizing MTHFD2 over other common folate metabolism targets in intact HL-60 and LCL-889 cells[1].TH9619 (1 nM-1 μM, 96 h) shows overall strong antiproliferative efficacy in AML cells and T-ALL Jurkat cells[1].TH9619 (1-100 μM, 96 h) target MTHFD1(DC) but not mitochondrial MTHFD2 in SW620 cells[2].
TH9619 (30 mg/kg, s.c., twice daily for 50 days) impairs cancer progression and lowers systemic tmidine levels in HL-60 cells xenograft acute myeloid leukemia (AML) NOG mice model[1].Plasma concentration and pharmacokinetic (PK) evaluation of TH9619 following subcutaneous administration of 10 mg/kg in female NOG mice[1]
References:
[1]. Bonagas N, et al. Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing tmidine depletion and replication stress. Nat Cancer. 2022 Feb;3(2):156-172.
[2]. Green AC, et al. Formate overflow drives toxic folate trapping in MTHFD1 inhibited cancer cells. Nat Metab. 2023 Apr;5(4):642-659.
| Cas No. | 2379556-22-4 | SDF | |
| Formula | C17H18FN7O7 | M.Wt | 451.37 |
| Löslichkeit | DMSO : 100 mg/mL (221.55 mM; ultrasonic and warming and heat to 60°C) | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2155 mL | 11.0774 mL | 22.1548 mL |
| 5 mM | 0.4431 mL | 2.2155 mL | 4.431 mL |
| 10 mM | 0.2215 mL | 1.1077 mL | 2.2155 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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