HM43239
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.
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Chemical Information
| Name | HM43239 |
|---|---|
| Iupac Chemical Name | rel-5-Chloro-N-[3-cyclopropyl-5-[[(3R,5S)-3,5-dimethyl-1-piperazinyl]methyl]phenyl]-4-(6-methyl-1H-indol-3-yl)-2-pyrimidinamine |
| Synonyms | HM43239; HM-43239; HM 43239; Tuspetinib |
| Molecular Formula | C29H33ClN6 |
| Molecular Weight | 501.07 |
| Smile | 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 |
| InChiKey | FZLSDZZNPXXBBB-KDURUIRLSA-N |
| InChi | InChI=1S/C29H33ClN6/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)/t18-,19+ |
| CAS Number | 2569527-64-4 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| 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. |
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| Mechanism | |
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| Clinical study |
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.
Chemical Structure
