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Chemical Structure| 2169916-18-9 Chemical Structure| 2169916-18-9

Structure of VTP50469
CAS No.: 2169916-18-9

Chemical Structure| 2169916-18-9

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VTP-50469 is a novel, potent, selective, orally-available MeninMLL1 inhibitor, being effectively against MLL-rearranged and NPM1c+ leukemia, selectively killing cell lines with MLLrearrangements and NPM1c+ mutations.

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Product Details of VTP50469

CAS No. :2169916-18-9
Formula : C32H47FN6O4S
M.W : 630.82
SMILES Code : C(N1CCC2(CN(C2)C=3C(OC4=C(C(N(C(C)C)C(C)C)=O)C=C(F)C=C4)=CN=CN3)CC1)[C@@H]5CC[C@@H](NS(C)(=O)=O)CC5
MDL No. :MFCD32197139

Safety of VTP50469

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of VTP50469

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Mouse Npm1c/Dnmt3a mutant cell line 10nM Evaluate effect of VTP-50469 on mouse Npm1c/Dnmt3a mutant cell line, showing rapid loss of self-renewal capacity Science. 2020 Jan 31;367(6477):586-590.
OCI-AML3 cells 3nM 6 days Assess sensitivity of OCI-AML3 cells to VTP-50469, showing rapid downregulation of MEIS1 and PBX3 Science. 2020 Jan 31;367(6477):586-590.
Human placental fibroblasts (HPFs) 0.5 mmol/L 4-5 days To reprogram HPFs into chemically induced epithelioid-like cells (ciEP-Ls), results showed morphological changes and upregulation of epithelial markers. Nan Fang Yi Ke Da Xue Xue Bao. 2025 Feb 20;45(2):322-330.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice MV4;11 xenograft model Oral 15, 30 and 60 mg/kg Twice daily for 28 days To evaluate the therapeutic effect of VTP50469 in vivo. Treatment at all dosage levels significantly prolonged survival. Cancer Cell. 2019 Dec 9;36(6):660-673.e11
BALB/c nude mice PDX model Oral gavage 50 mg/kg Once daily To evaluate the therapeutic effect of VTP50469 alone or in combination with alpelisib, results showed that the drug combination synergistically inhibited tumor growth and induced tumor regression in CRC PDX models carrying PIK3CA mutations. Cell Rep Med. 2024 May 21;5(5):101510
Mouse Npm1c/Dnmt3a mutant knock-in mice Oral 0.1% VTP-50469 chow Continuous for 9 weeks Assess eradication of preleukemic cells in Npm1c/Dnmt3a mutant mice by VTP-50469, showing rapid decrease in engraftment and no relapse Science. 2020 Jan 31;367(6477):586-590.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.59mL

0.32mL

0.16mL

7.93mL

1.59mL

0.79mL

15.85mL

3.17mL

1.59mL

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