HPK1-IN-7

未知

HPK1-IN-7

H648327-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

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 )

HPK1-IN-7 是一种强效的口服活性 HPK1（造血祖细胞激酶 1，MAP4K1）抑制剂（IC 50 =2.6 nM），具有出色的家族和激酶组选择性。HPK1-IN-7 对 IRAK4（59 nM）和 GLK（140 nM）具有选择性。HPK1-IN-7 对 IRAK4（59 nM）和 GLK（140 nM）具有很强的疗效。

2320462-65-3

C24H22N6O4

458.5 g/mol

142587219

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

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

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

RVSSNRBUPQUIEG-LJQANCHMSA-N

CC1(C2=C(C=CC(=C2)NC3=NC=C(C(=N3)NC(CO)C4=CC=CC=C4)C5=NN=CO5)C(=O)O1)C

142587219

DMSO : 125 mg/mL (272.65 mM; Need ultrasonic)

3

10

7

458.17 Da

458.17 Da

135.000 Ų

34

0

705.000

0

1

2.700