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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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H648327-1mg | 1mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $166.90 | |
H648327-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $350.90 | |
H648327-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $580.90 | |
H648327-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,100.90 |
Specifications & Purity | ≥99% |
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Biochemical and Physiological Mechanisms | HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor ( IC 50 =2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust effic |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor ( IC 50 =2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1 In Vivo HPK1-IN-7 (100 mg/kg; p.o.; twice daily for 28 days) shows robust enhancement of anti-PD1 efficacy in a syngeneic tumor model of colorectal cancer . HPK1-IN-7 (compound 24) (1 mg/kg; intravenous; mice) is characterized by moderate plasma clearance (43 mL/min/kg) and a large volume of distribution (4.4 L/kg). After oral administration (20 mg/kg), the Cmax was 5.3 μM and the AUC 0-24h was 19 μM•h. The calculated oral bioavailability based on these pharmacokinetics studies is approximately 100% . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice (MC38 syngeneic tumor model) Dosage: 100 mg/kg Administration: Oral; twice daily for 28 days Result: Enhanced the efficacy of anti-PD1 treatment, garnering a 100% cure rate vs a 20% cure rate with anti-PD1 alone. Form:Solid IC50& Target:HPK1 2.6 nM (IC 50 ) GLK/MAP4K3 140 nM (IC 50 ) IRAK4 59 nM (IC 50 ) Fms/CSFR 3.2 nM (IC 50 ) FLT3 25.4 nM (IC 50 ) AMPKA1 44.3 nM (IC 50 ) cKIT 45.7 nM (IC 50 ) MST1 55.1 nM (IC 50 ) ICK 65.1 nM (IC 50 ) MST2 78.5 nM (IC 50 ) |
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IUPAC Name | 5-[[4-[[(1S)-2-hydroxy-1-phenylethyl]amino]-5-(1,3,4-oxadiazol-2-yl)pyrimidin-2-yl]amino]-3,3-dimethyl-2-benzofuran-1-one |
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INCHI | InChI=1S/C24H22N6O4/c1-24(2)18-10-15(8-9-16(18)22(32)34-24)27-23-25-11-17(21-30-26-13-33-21)20(29-23)28-19(12-31)14-6-4-3-5-7-14/h3-11,13,19,31H,12H2,1-2H3,(H2,25,27,28,29)/t19-/m1/s1 |
InChi Key | RVSSNRBUPQUIEG-LJQANCHMSA-N |
Canonical SMILES | CC1(C2=C(C=CC(=C2)NC3=NC=C(C(=N3)NC(CO)C4=CC=CC=C4)C5=NN=CO5)C(=O)O1)C |
Isomeric SMILES | CC1(C2=C(C=CC(=C2)NC3=NC=C(C(=N3)N[C@H](CO)C4=CC=CC=C4)C5=NN=CO5)C(=O)O1)C |
PubChem CID | 142587219 |
Molecular Weight | 458.5 |
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Solubility | DMSO : 125 mg/mL (272.65 mM; Need ultrasonic) |
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