TH9619

Name: TH9619
Brand: MedChemExpress
SKU: HY-155950
Rating: 4.5 (1 reviews)

Cat. No.: HY-155950 Purity: 99.33%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

TH9619 is a potent inhibitor of dehydrogenase and cyclohydrolase 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.

For research use only. We do not sell to patients.

TH9619 Chemical Structure

CAS No. : 2379556-22-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Based on 1 publication(s) in Google Scholar

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Description

In Vitro

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].

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

In Vivo

TH9619 (30 mg/kg, s.c., twice daily for 50 days) impairs cancer progression and lowers systemic thymidine 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]

Parameters	C_max (μM)	T_max (h)	AUC_0-24 (μM*h)	AUC_0-inf (uM*h)	λz range (h)	T_1/2z (h)
TH9619	26.2	0.25	11.1	11.2	4-8	1.68

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

Animal Model:	HL-60 cells xenograft AML NOG mice model^[1]
Dosage:	30 mg/kg
Administration:	s.c., twice daily for 50 days
Result:	Significantly prolonged mouse survival combined with the low-folate diet by a median of 2weeks compared with vehicle without affecting body weight.

Molecular Weight

451.37

Formula

C₁₇H₁₈FN₇O₇

CAS No.

2379556-22-4

Appearance

Solid

Color

Off-white to light yellow

SMILES

NC(NC(N)=NC1=O)=C1CC(NC2=CN=C(C(N[C@H](C(O)=O)CCC(O)=O)=O)C(F)=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (221.55 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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	4.4310 mL
10 mM	0.2215 mL	1.1077 mL	2.2155 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.54 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.33%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (246 KB) HNMR (128 KB) RP-HPLC (255 KB) LCMS (228 KB)

Handling Instructions (2659 KB)

References

[1]. Bonagas N, et al. Pharmacological targeting of MTHFD2 suppresses acute myeloid leukemia by inducing thymidine depletion and replication stress. Nat Cancer. 2022 Feb;3(2):156-172. [Content Brief]

[2]. Green AC, et al. Formate overflow drives toxic folate trapping in MTHFD1 inhibited cancer cells. Nat Metab. 2023 Apr;5(4):642-659. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2155 mL	11.0774 mL	22.1548 mL	55.3869 mL
	5 mM	0.4431 mL	2.2155 mL	4.4310 mL	11.0774 mL
	10 mM	0.2215 mL	1.1077 mL	2.2155 mL	5.5387 mL
	15 mM	0.1477 mL	0.7385 mL	1.4770 mL	3.6925 mL
	20 mM	0.1108 mL	0.5539 mL	1.1077 mL	2.7693 mL
	25 mM	0.0886 mL	0.4431 mL	0.8862 mL	2.2155 mL
	30 mM	0.0738 mL	0.3692 mL	0.7385 mL	1.8462 mL
	40 mM	0.0554 mL	0.2769 mL	0.5539 mL	1.3847 mL
	50 mM	0.0443 mL	0.2215 mL	0.4431 mL	1.1077 mL
	60 mM	0.0369 mL	0.1846 mL	0.3692 mL	0.9231 mL
	80 mM	0.0277 mL	0.1385 mL	0.2769 mL	0.6923 mL
	100 mM	0.0222 mL	0.1108 mL	0.2215 mL	0.5539 mL

TH9619 Related Classifications

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:

TH96192379556-22-4TH 9619TH-9619Methylenetetrahydrofolate Dehydrogenase (MTHFD)ApoptosisMTHFD2InhibitorAntitumorHL-60inhibitorinhibit

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TH9619

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TH9619 Related Antibodies

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Complete Stock Solution Preparation Table

TH9619 Related Classifications

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