| Identification | Back Directory | [Name]
Benzamide, 4-[(di-2-pyrazinylamino)methyl]-N-hydroxy- | [CAS]
1636894-46-6 | [Synonyms]
KA2507
Benzamide, 4-[(di-2-pyrazinylamino)methyl]-N-hydroxy-
modulatory,KA 2507,KA-2507,colorectal,Histone deacetylases,immune,cancer,antitumor,KA2507,Inhibitor,melanoma,HDAC,inhibit | [Molecular Formula]
C16H14N6O2 | [MDL Number]
MFCD34473324 | [MOL File]
1636894-46-6.mol | [Molecular Weight]
322.32 |
| Chemical Properties | Back Directory | [density ]
1.407±0.06 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 66.67 mg/mL (206.84 mM; Need ultrasonic) | [form ]
Solid | [pka]
8.77±0.10(Predicted) | [color ]
White to light brown |
| Hazard Information | Back Directory | [Uses]
KA2507 is a potent, orally active and selective HDAC6 inhibitor, with an IC50 of 2.5 nM. KA2507 shows antitumor activities and immune modulatory effects in preclinical models[1]. | [in vivo]
KA2507 (100-200 mg/kg; p.o.; daily; for 20 days) inhibits tumor growth in the syngeneic B16-F10 mouse melanoma model[1].
KA2507 also demonstrates antitumor efficacy in CT26 and MC38 colorectal cancer models[1].
Analysis of tumor samples also indicates modulation of biomarkers of antitumor immunity at efficacious dosing, with KA2507 administration resulting in reduced STAT3 activation (as measured by phospho-STAT3, an important suppressor of the antitumor immune response), reduced PD-L1 expression, and increased expression of MHC class I[1].
KA2507 exhibits poor oral bioavailability (mice 15%) and Cmax (mice 300 ng/mL) following oral administration (mice 200 mg/kg)[1].
| Animal Model: | Male C57BL/6 mice, B16-F10 melanoma model[1] | | Dosage: | 100 mg/kg, 200 mg/kg, 200 mg/kg | | Administration: | Oral gavage, daily, for 20 days | | Result: | Demonstrated antitumor efficacy. |
| Animal Model: | Male C57BL/6 mice[1] | | Dosage: | 200 mg/kg (Pharmacokinetic Analysis) | | Administration: | Oral administration | | Result: | Oral bioavailability (15%), Cmax (300 ng/mL). |
| [IC 50]
HDAC6: 2.5 nM (IC50); HDAC8: 621 (IC50) | [References]
[1] Apostolia M Tsimberidou, et al. Preclinical Development and First-in-Human Study of KA2507, a Selective and Potent Inhibitor of Histone Deacetylase 6, for Patients with Refractory Solid Tumors. Clin Cancer Res. 2021 May 4. DOI:10.1158/1078-0432.CCR-21-0238 |
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| Company Name: |
NewCan Biotech Limited
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| Telephone: |
+86-0571-86912261 +86-15658003402 |
| Website: |
https://www.newcanbio.com/ |
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