Shopping Cart

Your shopping cart is currently empty

AS-99 TFA

Name: AS-99 TFA
Brand: TargetMol
SKU: T36978
Price: 536 USD
Availability: InStock
Rating: 5 (10 reviews)

Copy Product Info

😃Good

Catalog No. T36978Cas No. 3115178-55-4

AS-99 TFA is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. It blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo[1].

AS-99 TFA

Copy Product Info

😃Good

Catalog No. T36978Cas No. 3115178-55-4

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
5 mg	$536	-	In Stock
10 mg	$909	-	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Batch Information

Select Batch

Appearance:Solid

Color:Yellow

Resource Download

COA

Product Introduction

Bioactivity

Description	AS-99 TFA is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. It blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo[1].
In vitro	AS-99 TFA was tested against 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2, revealing no significant inhibition at 50 μM, indicating over 100-fold selectivity towards ASH1L[1]. AS-99 TFA affects the growth of MLL leukemia cells (MV4;11, MOLM13, KOPN8, RS4;11) with GI50 values ranging from 1.8 μM to 3.6 μM[1]. AS-99 TFA (1-8 μM; 7 days) also induces apoptosis in MLL leukemia cells, but not in K562 cells, as shown by Annexin V positive cell quantification, and it suppresses MLL fusion driven transcriptional programs[1].
In vivo	AS-99 (30 mg/kg; i.p.; q.d., treated for 14 consecutive days) TFA reduces leukemia burden in mice[1].AS-99 TFA is used for in vivo studies in mice, which reveals favorable exposure in plasma upon i.v. and i.p. administration (AUC = 9701 hr* ng/mL and 10,699 hr* ng/mL, respectively), suitable half-life (~5-6 h) and Cmax >10 μM[1].

Chemical Properties

Molecular Weight	707.71
Formula	C₂₉H₃₁F₆N₅O₅S₂
Cas No.	3115178-55-4
Smiles	O=C(O)C(F)(F)F.O=C(NCC=1C=CC=2C(=CN(C2C1)C3CCN(CC3)S(=O)(=O)C(F)(F)F)C=4C=CC=C(C4)C(=S)N)C5CN(C)C5

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250.00 mg/mL (353.25 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.30 mg/mL (4.66 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.4130 mL	7.0650 mL	14.1301 mL	70.6504 mL
5 mM	0.2826 mL	1.4130 mL	2.8260 mL	14.1301 mL
10 mM	0.1413 mL	0.7065 mL	1.4130 mL	7.0650 mL
20 mM	0.0707 mL	0.3533 mL	0.7065 mL	3.5325 mL
50 mM	0.0283 mL	0.1413 mL	0.2826 mL	1.4130 mL
100 mM	0.0141 mL	0.0707 mL	0.1413 mL	0.7065 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc