WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H124831
CAS#: 2758339-04-5 (hydrate)
Description: HM43239 is an orally active small molecule inhibitor of FLT3 that selectively inhibits not only FLT3 wild type, ITD mutants or TKD mutations, but also FLT3 ITD/TKD double mutations. HM43239 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1/2 and TAK1, known to be involved in tumor cell proliferation and/or differentiation HM43239 monotherapy induced dose-dependent regression of tumor growth in FLT3 wild-type and FLT3 mutated leukemia cancer cell line.
Hodoodo Cat#: H124831
Name: Tuspetinib monohydrate
CAS#: 2758339-04-5 (hydrate)
Chemical Formula: C29H35ClN6O
Exact Mass: 518.26
Molecular Weight: 519.090
Elemental Analysis: C, 67.10; H, 6.80; Cl, 6.83; N, 16.19; O, 3.08
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Related CAS #: 2758339-04-5 (hydrate) 2569527-64-4
Synonym: HM43239 monohydrate; HM-43239 monohydrate; 1YT25M37WR; UNII-1YT25M37WR;
IUPAC/Chemical Name: 5-chloro-N-[3-cyclopropyl-5-[[(3R,5S)-3,5-dimethylpiperazin-1-yl]methyl]phenyl]-4-(6-methyl-1H-indol-3-yl)pyrimidin-2-amine;hydrate
InChi Key: ZBXHRUUVJWPXCW-AQDIUKAZSA-N
InChi Code: InChI=1S/C29H33ClN6.H2O/c1-17-4-7-24-25(12-31-27(24)8-17)28-26(30)13-32-29(35-28)34-23-10-20(9-22(11-23)21-5-6-21)16-36-14-18(2)33-19(3)15-36;/h4,7-13,18-19,21,31,33H,5-6,14-16H2,1-3H3,(H,32,34,35);1H2/t18-,19+;
SMILES Code: CC1=CC2=C(C=C1)C(C3=NC(NC4=CC(CN5C[C@@H](C)N[C@@H](C)C5)=CC(C6CC6)=C4)=NC=C3Cl)=CN2.[H]O[H]
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 519.09 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1. Kim J, Bae I, Choi J, Kim M, Byun J, Moon M, Lee E, Kim Y, Kang H, Kim E, Jung S, Ahn Y, Kim Y, Suh K. Abstract 1293: HM43239, a novel FLT3 inhibitor in overcoming resistance for acute myeloid leukemia. Cancer Res. 2019 July 1;79(13_Supplement):1293. doi: 10.1158/1538-7445.AM2019-1293.
2. Lee M, Young E, Moon M, Byun J, Yu H, Kang S, Lee J, Lee K, Kim E, Lee H, Kim Y, Ahn Y, Suh K, Kim S. Abstract 804: Antitumor activity of the potent and novel FLT3 inhibitor HM43239 in acute myeloid leukemia. Cancer Res. 2018 July 1;78(13_Supplement):804. doi: 10.1158/1538-7445.AM2018-804.
