2. Epigenetics
  3. Histone Methyltransferase
  4. AMG-193

AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP.

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AMG-193 Chemical Structure

AMG-193 Chemical Structure

CAS No. : 2790567-82-5

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10 mM * 1 mL in DMSO USD 748 In-stock
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Based on 1 publication(s) in Google Scholar

AMG-193 Related Antibodies

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP[1][2].

In Vitro

AMG 193 (200 μM; 6 d) induces alternative splicing defects, cell cycle arrest, and DNA damage response in MTAP-deficient HCT116 cells[2].

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

AMG-193 Related Antibodies

Cell Cycle Analysis[2]

Cell Line: MTAP-deficient HCT116 cells
Concentration: 200 µM
Incubation Time: 6 d
Result: Reduced the S phase and increased the G2/M cell population in mtap-deficient cells.
In Vivo

AMG 193 (3-100 mg/kg; p.o.; once every 5 days for 4 doses) dose-dependently inhibits tumor growth in MTAP-deficient xenograft mice[2].
AMG 193 (100 mg/kg; p.o.; once daily for 11 days) slightly reduces body weight in mice implanted with DLBCL (DOHH-2) tumors and causes tumor regression in 70% of mice, with preservation of normal hematopoietic cell lineages[2].

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

Animal Model: HCT116 MTAP-deficient mice[2]
Dosage: 3、10、30、100 mg/kg
Administration: p.o.; The drug was administered on day 20 after mice were implanted with DLBCL (DOHH-2) tumor cells and was administered once every 5 days for a total of 4 doses.
Result: Inhibited SDMA signaling in mtap-deleted tumors at all doses.
Animal Model: Mice implanted with DLBCL (DOHH-2) tumors[2]
Dosage: 100 mg/kg
Administration: p.o.; Once daily for 11 days
Result: Caused a significant increase in the Sub-G1 population and induced tumor cell death.
Molecular Weight

444.41

Formula

C22H19F3N4O3
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(N1[C@@H](C2=CC=C(C=C2)C(F)(F)F)COCC1)C3=NC=C4N=C(N)C(COC5)=C5C4=C3
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
Purity & Documentation

Purity: 99.36%

COA (254 KB) HNMR (143 KB) RP-HPLC (233 KB) LCMS (227 KB)

Handling Instructions (2659 KB)
References
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AMG-193 Related Classifications

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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:

AMG-1932790567-82-5AMG193AMG 193Histone MethyltransferasePRMT5 InhibitorHCT116Inhibitorinhibitorinhibit

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