1. Epigenetics
    Apoptosis
  2. Histone Methyltransferase
    Apoptosis
  3. AS-99 TFA

AS-99 TFA 

Cat. No.: HY-141429A Purity: 98.85%
Handling Instructions

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. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo.

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

AS-99 TFA Chemical Structure

AS-99 TFA Chemical Structure

Size Price Stock Quantity
5 mg USD 580 In-stock
Estimated Time of Arrival: December 31
10 mg USD 980 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1900 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 5000 Get quote
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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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. AS-99 TFA 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 is tested against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. NO significant inhibition is observed at 50 µM of AS-99 TFA on any of the tested histone methyltransferases, indicating over 100-fold selectivity towards ASH1L[1].
AS-99 TFA shows effect on the growth of the MLL leukemia cells (MV4;11, MOLM13, KOPN8, RS4;11) with the GI50 values ranging from 1.8 µM to 3.6 µM[1].
AS-99 (1-8 µM; 7 days) TFA also induces apoptosis in the MLL leukemia cells, but not in the K562 cells, as assessed by the quantification of the Annexin V positive cells[1].
AS-99 TFA suppresses MLL fusion driven transcriptional programs[1].

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

RT-PCR[1]

Cell Line: MOLM13 cells
Concentration: 2-6 µM
Incubation Time: 7 days
Result: Led to a dose-dependent downregulation of canonical MLL fusion target genes required for leukemogenesis including MEF2C, DLX2, FLT3, and HOXA9.
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].

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

Animal Model: 8- to 10-week old female NSG mice (bearing MV4;11 cells)[1]
Dosage: 30 mg/kg
Administration: I.p.; q.d., treated for 14 consecutive days
Result: Reduced the leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood counts in normal mice.
Molecular Weight

707.71

Formula

C₂₉H₃₁F₆N₅O₅S₂

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 : 250 mg/mL (353.25 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4130 mL 7.0650 mL 14.1301 mL
5 mM 0.2826 mL 1.4130 mL 2.8260 mL
10 mM 0.1413 mL 0.7065 mL 1.4130 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.94 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (2.94 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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AS-99 TFA
Cat. No.:
HY-141429A
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