Share to

Details

Safety

Technical Documents

Articles

reviews

Consult

returns

Product details

名称

HPK1-IN-7

分子类型

未知

英文名称

HPK1-IN-7

货号

H648327-5mg

包装规格

5mg

浓度

≥99%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

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 )

生化机理

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。

CAS号

2320462-65-3

分子式

C24H22N6O4

分子量

458.5 g/mol

PubChem编号

142587219

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

IIUPAC 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

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

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

PubChem CID

142587219

溶解性

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

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

458.17 Da

单同位素质量Monoisotopic Mass

458.17 Da

拓扑极表面积Topological Polar Surface Area

135.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

705.000

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

2.700

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

user reviews

Consultation

Warm reminder：

Because the manufacturer may temporarily adjust product specifications, prices, inventory, parameters and other information without notice, and there are differences in each user's consultation time and procurement needs, the platform reply content is only of reference value within a certain period. Sorry for the inconvenience caused to you, and thank you for your understanding and support! Please consult the online customer service for the latest details. Everything is subject to the real-time reply of the customer service.！

After Sales Services

Please check the quantity, appearance and product information in time when you receive the goods. In case of damage, wrong delivery, abnormal quality and other problems, please feel free to contact us.

Service Hotline:400-6226-992 ，We will handle it for you as soon as possible, thank you for your support and trust.！