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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
12 Results for "
D816V
" in MedChemExpress (MCE) Product Catalog:
Products (12)
12 Results for "D816V" in MCE Product Catalog:
14
Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
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1 Cited Publications
Synonyms: CGT9486; PLX 9486
Bezuclastinib (CGT9486) is an orally active, highly selective tyrosine kinase inhibitor with potent activity against KIT D816V. Bezuclastinib can be used for the research of nonadvanced systemic mastocytosis (NonAdvSM) .
Synonyms: BLU-263
Elenestinib (BLU-263) is an orally active inhibitor of Tyrosine kinase with an IC50 value of 6 nM for KIT D816V. Elenestinib minimally penetrates the blood-brain barrier. Elenestinib can be used in the study of systemic mastocytosis .
Cat. No.: HY-E70736
KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT D816V is a mutant of KIT. KIT D816V Recombinant Human Active Protein Kinase is a recombinant KIT D816V protein that can be used to study KIT D816V-related functions .
Cat. No.: HY-171544
Synonyms: AGS-16M8F
Cat. No.: HY-152839A
CAS No.: 2832013-93-9
Synonyms: BLU-263 phosphate
Elenestinib (BLU-263) phosphate is an orally active inhibitor of Tyrosine kinase with an IC50 of 0.2 nM for KIT D816V. Elenestinib phosphate minimally penetrates the blood-brain barrier. Elenestinib phosphate can be used in the study of systemic mastocytosis .
Cat. No.: HY-101561R
CAS No.: 1703793-34-3
Synonyms: BLU-285 (Standard)
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Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
Cat. No.: HY-W754911
CAS No.: 2408934-57-4
Synonyms: BLU-285-d3
Cat. No.: HY-107458
CAS No.: 834894-21-2
AP23848 is an ATP-dependent kinase inhibitor that effectively and selectively targets the Kit activation loop mutation both in vitro and in vivo, showing anti-tumor activity. AP23848 can inhibit the phosphorylation of the activated Kit mutation and tumor growth in mice, making it suitable for targeting diseases with the D816V mutation, such as systemic mastocytosis (SM) and acute myeloid leukemia (AML) research .
Cat. No.: HY-121708
CAS No.: 930089-25-1
KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
Cat. No.: HY-10638
CAS No.: 845895-51-4
AP23464 is an ATP-based inhibitor for Kit, that inhibits the phosphorylation of Kit wildtype and mutants, with IC50 of 5-85 nM. AP23464 inhibits the proliferation of Kit mutated cells (IC50 is 3-20 nM), arrests the cell cycle at G0/G1 phase, and induces apoptosis in Kit mutated cells .
Cat. No.: HY-P706025
Purity: ≥ 85%, as determined by reducing SDS-PAGE.
Synonyms: Mast/stem cell growth factor receptor Kit; Piebald trait protein; PBT; Proto-oncogene c-Kit; Tyrosine-protein kinase Kit; p145 c-kit; v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog; SCFR
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
